680:, as it competes with the full agonist for receptor occupancy, thereby producing a net decrease in the receptor activation as compared to that observed with the full agonist alone. Clinically, their usefulness is derived from their ability to enhance deficient systems while simultaneously blocking excessive activity. Exposing a receptor to a high level of a partial agonist will ensure that it has a constant, weak level of activity, whether its normal agonist is present at high or low levels. In addition, it has been suggested that partial agonism prevents the adaptive regulatory mechanisms that frequently develop after repeated exposure to potent full agonists or antagonists. E.g.
346:
567:. While the mechanism of antagonism is different in both of these phenomena, they are both called "non-competitive" because the end-results of each are functionally very similar. Unlike competitive antagonists, which affect the amount of agonist necessary to achieve a maximal response but do not affect the magnitude of that maximal response, non-competitive antagonists reduce the magnitude of the maximum response that can be attained by any amount of agonist. This property earns them the name "non-competitive" because their effects cannot be negated, no matter how much agonist is present. In functional assays of non-competitive antagonists,
291:
615:
649:
474:(active site) as the endogenous ligand or agonist, but without activating the receptor. Agonists and antagonists "compete" for the same binding site on the receptor. Once bound, an antagonist will block agonist binding. Sufficient concentrations of an antagonist will displace the agonist from the binding sites, resulting in a lower frequency of receptor activation. The level of activity of the receptor will be determined by the relative
439:
780:. But, once irreversible bonding has taken place, the receptor is deactivated and degraded. As for non-competitive antagonists and irreversible antagonists in functional assays with irreversible competitive antagonist drugs, there may be a shift in the log concentration–effect curve to the right, but, in general, both a decrease in slope and a reduced maximum are obtained.
2370:
209:. Antagonists mediate their effects through receptor interactions by preventing agonist-induced responses. This may be accomplished by binding to the active site or the allosteric site. In addition, antagonists may interact at unique binding sites not normally involved in the biological regulation of the receptor's activity to exert their effects.
31:
771:
from binding. Inactivation of receptors normally results in a depression of the maximal response of agonist dose-response curves and a right shift in the curve occurs where there is a receptor reserve similar to non-competitive antagonists. A washout step in the assay will usually distinguish between
378:
determination is independent of the affinity, efficacy or concentration of the agonist used. However, it is important that equilibrium has been reached. The effects of receptor desensitization on reaching equilibrium must also be taken into account. The affinity constant of antagonists exhibiting two
627:
Uncompetitive antagonists differ from non-competitive antagonists in that they require receptor activation by an agonist before they can bind to a separate allosteric binding site. This type of antagonism produces a kinetic profile in which "the same amount of antagonist blocks higher concentrations
586:
site. These antagonists bind to a distinctly separate binding site from the agonist, exerting their action to that receptor via the other binding site. They do not compete with agonists for binding at the active site. The bound antagonists may prevent conformational changes in the receptor required
578:
An antagonist that binds to the active site of a receptor is said to be "non-competitive" if the bond between the active site and the antagonist is irreversible or nearly so. This usage of the term "non-competitive" may not be ideal, however, since the term "irreversible competitive antagonism" may
266:
and that ligand-specific receptor conformations occur and can affect interaction of receptors with different second messenger systems may mean that drugs can be designed to activate some of the downstream functions of a receptor but not others. This means efficacy may actually depend on where that
712:
that exhibit intrinsic or basal activity can have inverse agonists, which not only block the effects of binding agonists like a classical antagonist but also inhibit the basal activity of the receptor. Many drugs previously classified as antagonists are now beginning to be reclassified as inverse
117:
on a receptor, or they may interact at unique binding sites not normally involved in the biological regulation of the receptor's activity. Antagonist activity may be reversible or irreversible depending on the longevity of the antagonist–receptor complex, which, in turn, depends on the nature of
387:
in the presence of a competitive antagonist as determined on a dose response curve. Altering the amount of antagonist used in the assay can alter the dose ratio. In Schild regression, a plot is made of the log (dose ratio-1) versus the log concentration of antagonist for a range of antagonist
478:
of each molecule for the site and their relative concentrations. High concentrations of a competitive agonist will increase the proportion of receptors that the agonist occupies, higher concentrations of the antagonist will be required to obtain the same degree of binding site occupancy. In
775:
Irreversible competitive antagonists also involve competition between the agonist and antagonist of the receptor, but the rate of covalent bonding differs and depends on affinity and reactivity of the antagonist. For some antagonists, there may be a distinct period during which they behave
379:
or more effects, such as in competitive neuromuscular-blocking agents that also block ion channels as well as antagonising agonist binding, cannot be analyzed using Schild regression. Schild regression involves comparing the change in the dose ratio, the ratio of the EC
656:
Silent antagonists are competitive receptor antagonists that have zero intrinsic activity for activating a receptor. They are true antagonists, so to speak. The term was created to distinguish fully inactive antagonists from weak partial agonists or inverse agonists.
537:
targets. Reversible antagonists, which bind via noncovalent intermolecular forces, will eventually dissociate from the receptor, freeing the receptor to be bound again. Irreversible antagonists bind via covalent intermolecular forces. Because there is not enough
225:
cellular response by binding to the receptor, thus initiating a biochemical mechanism for change within a cell. Antagonists were thought to turn "off" that response by 'blocking' the receptor from the agonist. This definition also remains in use for
216:
was originally coined to describe different profiles of drug effects. The biochemical definition of a receptor antagonist was introduced by Ariens and
Stephenson in the 1950s. The current accepted definition of receptor antagonist is based on the
671:
Partial agonists are defined as drugs that, at a given receptor, might differ in the amplitude of the functional response that they elicit after maximal receptor occupancy. Although they are agonists, partial agonists can act as a
1962:
Parsons CG, Stöffler A, Danysz W (November 2007). "Memantine: a NMDA receptor antagonist that improves memory by restoration of homeostasis in the glutamatergic system—too little activation is bad, too much is even worse".
747:
bind to the receptor target and, in general, cannot be removed; inactivating the receptor for the duration of the antagonist effects is determined by the rate of receptor turnover, the rate of synthesis of new receptors.
542:
to break covalent bonds in the local environment, the bond is essentially "permanent", meaning the receptor-antagonist complex will never dissociate. The receptor will thereby remain permanently antagonized until it is
341:
the greater the potency of the antagonist, and the lower the concentration of drug that is required to inhibit the maximum biological response. Lower concentrations of drugs may be associated with fewer side-effects.
261:
and the biochemical definition of a receptor antagonist continues to evolve. The two-state model of receptor activation has given way to multistate models with intermediate conformational states. The discovery of
200:
on the receptor. A receptor may contain one or more binding sites for different ligands. Binding to the active site on the receptor regulates receptor activation directly. The activity of receptors can also be
333:
value). This can be calculated for a given antagonist by determining the concentration of antagonist needed to elicit half inhibition of the maximum biological response of an agonist. Elucidating an IC
1618:
Cheng Y, Prusoff WH (December 1973). "Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction".
396:
values from the Cheng-Prusoff equation, agonist concentrations are varied. Affinity for competitive agonists and antagonists is related by the Cheng-Prusoff factor used to calculate the K
118:
antagonist–receptor binding. The majority of drug antagonists achieve their potency by competing with endogenous ligands or substrates at structurally defined binding sites on receptors.
408:. The Cheng-Prusoff factor takes into account the effect of altering agonist concentration and agonist affinity for the receptor on inhibition produced by competitive antagonists.
1915:"Failures and successes of NMDA receptor antagonists: molecular basis for the use of open-channel blockers like memantine in the treatment of acute and chronic neurologic insults"
337:
value is useful for comparing the potency of drugs with similar efficacies, however the dose-response curves produced by both drug antagonists must be similar. The lower the IC
366:), i.e. its ability to bind to a receptor, will determine the duration of inhibition of agonist activity. The affinity of an antagonist can be determined experimentally using
1820:
D.E. Golan, A.H Tashjian Jr, E.J. Armstrong, A.W. Armstrong. (2007) Principles of
Pharmacology: The Pathophysiologic Basis of Drug Therapy Lippincott Williams & Wilkins
822:
1807:
479:
functional assays using competitive antagonists, a parallel rightward shift of agonist dose–response curves with no alteration of the maximal response is observed.
1664:"International Union of Pharmacology Committee on Receptor Nomenclature and Drug Classification. XXXVIII. Update on terms and symbols in quantitative pharmacology"
2203:
Greasley PJ, Clapham JC (December 2006). "Inverse agonism or neutral antagonism at G-protein coupled receptors: a medicinal chemistry challenge worth pursuing?".
221:. It narrows the definition of antagonism to consider only those compounds with opposing activities at a single receptor. Agonists were thought to turn "on" a
302:
to activate the receptors they bind. Antagonists do not maintain the ability to activate a receptor. Once bound, however, antagonists inhibit the function of
3230:
392:
is where the line cuts the x-axis on the regression plot. Whereas, with Schild regression, antagonist concentration is varied in experiments used to derive K
571:
of the maximal response of agonist dose-response curves, and in some cases, rightward shifts, is produced. The rightward shift will occur as a result of a
579:
also be used to describe the same phenomenon without the potential for confusion with the second meaning of "non-competitive antagonism" discussed below.
1055:
Bleicher KH, Green LG, Martin RE, Rogers-Evans M (June 2004). "Ligand identification for G-protein-coupled receptors: a lead generation perspective".
772:
non-competitive and irreversible antagonist drugs, as effects of non-competitive antagonists are reversible and activity of agonist will be restored.
3684:
349:
Agonists get its maximum effect reduced when in the presence of an
Irreversible Competitive Antagonist or a Reversible Non-Competitive Antagonist.
2402:
614:
1785:
1373:
2048:
Principles and
Practice of Pharmacology for Anaesthetists By Norton Elwy Williams, Thomas Norman Calvey Published 2001 Blackwell Publishing
2494:
2459:
2006:
Fletcher A, Cliffe IA, Dourish CT (December 1993). "Silent 5-HT1A receptor antagonists: utility as research tools and therapeutic agents".
1775:
482:
Competitive antagonists are used to prevent the activity of drugs, and to reverse the effects of drugs that have already been consumed.
345:
3837:
3781:
3188:
2281:
Leurs R, Church MK, Taglialatela M (April 2002). "H1-antihistamines: inverse agonism, anti-inflammatory actions and cardiac effects".
2092:
Bosier B, Hermans E (August 2007). "Versatility of GPCR recognition by drugs: from biological implications to therapeutic relevance".
1402:
Lees P, Cunningham FM, Elliott J (December 2004). "Principles of pharmacodynamics and their applications in veterinary pharmacology".
559:
site of the receptor, or by irreversibly binding to the active site of the receptor. The former meaning has been standardised by the
3490:
2053:
1825:
954:
592:
294:
Agonists require higher dose/concentration to achieve the same effect when in the presence of a reversible competitive antagonist.
3674:
3223:
3178:
794:
1774:
eds, David E. Golan, ed.-in-chief; Armen H. Tashjian Jr., deputy ed.; Ehrin J. Armstrong, April W. Armstrong, associate (2008).
819:
3856:
3770:
3118:
2611:
1839:"Cyclothiazide selectively inhibits mGluR1 receptors interacting with a common allosteric site for non-competitive antagonists"
1174:
Ariens EJ (September 1954). "Affinity and intrinsic activity in the theory of competitive inhibition. I. Problems and theory".
618:
Figure demonstrates the noncompetitive antagonistic behaviour of
Phenoxybenzamine on alpha-adrenergiv norepinephrine receptors.
2646:
374:. Schild regression can be used to determine the nature of antagonism as beginning either competitive or non-competitive and K
3842:
3173:
2869:
2780:
2374:
736:
Many antagonists are reversible antagonists that, like most agonists, will bind and unbind a receptor at rates determined by
290:
3922:
3664:
3318:
3312:
3098:
2723:
318:
measures the effect of the ability of a range of concentrations of antagonists to reverse the activity of an agonist. The
3927:
3831:
3603:
2651:
799:
607:, which in turn reduces the fraction of available receptors and reduces the maximal effect that can be produced by the
3746:
3519:
3216:
2841:
1012:
Christopoulos A (March 2002). "Allosteric binding sites on cell-surface receptors: novel targets for drug discovery".
776:
competitively (regardless of basal efficacy), and freely associate to and dissociate from the receptor, determined by
575:(also known as spare receptors) and inhibition of the agonist response will only occur when this reserve is depleted.
555:
A non-competitive antagonist is a type of insurmountable antagonist that may act in one of two ways: by binding to an
1090:
Rees S, Morrow D, Kenakin T (2002). "GPCR drug discovery through the exploitation of allosteric drug binding sites".
2326:"Phenoxybenzamine binding reveals the helical orientation of the third transmembrane domain of adrenergic receptors"
1717:
Vauquelin G, Van Liefde I, Birzbier BB, Vanderheyden PM (August 2002). "New insights in insurmountable antagonism".
3585:
3424:
3411:
3382:
3327:
2576:
2395:
708:
can have effects similar to those of an antagonist, but causes a distinct set of downstream biological responses.
3932:
3881:
3398:
3088:
2836:
2830:
918:
539:
251:
227:
193:
142:("to contend for a prize"). Antagonists were discovered in the 20th century by American biologist Bailey Edgren.
3775:
3721:
3706:
3678:
3459:
3454:
3445:
3153:
2855:
777:
737:
966:
May LT, Avlani VA, Sexton PM, Christopoulos A (2004). "Allosteric modulation of G protein-coupled receptors".
3876:
3847:
3815:
3645:
3450:
3406:
3357:
3288:
2904:
2666:
2661:
2571:
2489:
923:
889:
709:
568:
534:
475:
157:
151:
82:
62:
51:
39:
1127:"Some implications of receptor theory for in vivo assessment of agonists, antagonists and inverse agonists"
3757:
3563:
3040:
2801:
2776:
2711:
2600:
2484:
2238:
Kenakin T (January 2004). "Efficacy as a vector: the relative prevalence and paucity of inverse agonism".
1889:
673:
633:
428:
405:
371:
319:
263:
181:
3888:
3732:
3465:
3352:
3148:
2940:
2742:
2419:
2388:
721:
239:
206:
202:
177:
165:
114:
54:
1442:
Swinney DC (September 2004). "Biochemical mechanisms of drug action: what does it take for success?".
572:
69:. Antagonist drugs interfere in the natural operation of receptor proteins. They are sometimes called
3893:
3737:
3590:
3543:
3183:
3045:
2955:
2796:
2676:
2444:
101:
for their cognate receptors, and binding will disrupt the interaction and inhibit the function of an
230:, substances that have opposing physiological actions, but act at different receptors. For example,
3514:
3093:
2981:
2950:
2596:
2556:
760:
757:
604:
315:
450: with: information about irreversible/insurmountable competitive antagonists. You can help by
3741:
3710:
3441:
3337:
3063:
3013:
2914:
2727:
2706:
2606:
2527:
2439:
2306:
2263:
2031:
1988:
1801:
1742:
1694:
1467:
1341:
1287:
1037:
991:
949:
T. Kenakin (2006) A Pharmacology Primer: Theory, Applications, and
Methods. 2nd Edition Elsevier
871:
3810:
3715:
3538:
3331:
3058:
2919:
2909:
2737:
2731:
2566:
2347:
2298:
2255:
2220:
2185:
2144:
2109:
2049:
2023:
1980:
1944:
1868:
1821:
1781:
1734:
1686:
1663:
1635:
1600:
1551:
1516:
1459:
1419:
1379:
1369:
1333:
1279:
1237:
1183:
1156:
1107:
1072:
1029:
983:
950:
863:
367:
931:
652:
Chart demonstrating the difference between agonists, silent antagonists, and inverse agonists
3800:
3594:
3509:
3263:
3103:
2991:
2986:
2786:
2756:
2542:
2522:
2504:
2337:
2290:
2247:
2212:
2175:
2136:
2101:
2074:
2015:
1972:
1934:
1926:
1858:
1850:
1726:
1678:
1627:
1590:
1582:
1543:
1506:
1498:
1451:
1411:
1325:
1269:
1227:
1219:
1146:
1138:
1099:
1064:
1021:
975:
855:
789:
749:
685:
648:
596:
417:
280:
185:
94:
3728:
3640:
3478:
3473:
3343:
3307:
3297:
3280:
3143:
3018:
2846:
2806:
2791:
2499:
2449:
2127:
Pulvirenti L, Koob GF (April 2002). "Being partial to psychostimulant addiction therapy".
831:
826:
705:
666:
487:
307:
258:
218:
106:
3420:
3275:
3258:
3133:
3113:
3032:
2874:
2616:
2561:
1863:
1838:
1595:
1586:
1570:
1511:
1486:
1232:
1223:
1207:
1151:
1126:
511:
127:
2140:
2078:
1939:
1914:
912:
438:
3916:
3656:
3555:
3547:
3530:
3469:
3138:
2625:
2532:
2294:
2019:
1976:
1854:
1759:
Stevens, E. (2013) Medicinal
Chemistry: The Modern Drug Discovery Process. pg. 79, 84
1730:
1631:
1534:
Colquhoun D (December 2007). "Why the Schild method is better than Schild realised".
1415:
1313:
1274:
1257:
768:
753:
744:
714:
681:
637:
600:
588:
189:
74:
2310:
1780:(2nd ed.). Philadelphia, Pa., : Lippincott Williams & Wilkins. p. 25.
1471:
1308:
Urban JD, Clarke WP, von
Zastrow M, Nichols DE, Kobilka B, Weinstein H, Javitch JA,
1041:
995:
875:
17:
3635:
3501:
3484:
3239:
3108:
3068:
2969:
2893:
2771:
2454:
2411:
2035:
1992:
1746:
1698:
471:
359:
235:
197:
86:
78:
2267:
1345:
1291:
2216:
3792:
3765:
3698:
3391:
3271:
3193:
2680:
2656:
1312:, Christopoulos A, Sexton PM, Miller KJ, Spedding M, Mailman RB (January 2007).
110:
2105:
1547:
1068:
3618:
3433:
3073:
3005:
2897:
2672:
1383:
1309:
1142:
764:
583:
556:
507:
247:
979:
3627:
3577:
2851:
1930:
1837:
Surin A, Pshenichkin S, Grajkowska E, Surina E, Wroblewski JT (March 2007).
1329:
1314:"Functional selectivity and classical concepts of quantitative pharmacology"
718:
693:
689:
629:
544:
499:
231:
2351:
2342:
2325:
2302:
2259:
2224:
2189:
2148:
2113:
1984:
1948:
1872:
1738:
1690:
1555:
1520:
1502:
1463:
1423:
1337:
1283:
1187:
1160:
1111:
1103:
1076:
1033:
987:
867:
257:
Our understanding of the mechanism of drug-induced receptor activation and
2369:
2180:
2163:
2027:
1639:
1604:
1241:
61:
that blocks or dampens a biological response by binding to and blocking a
30:
3668:
2973:
2945:
2932:
2701:
2621:
2324:
Frang H, Cockcroft V, Karskela T, Scheinin M, Marjamäki A (August 2001).
1657:
1655:
1653:
1651:
1649:
495:
483:
299:
268:
98:
820:
Pharmacology Guide: In vitro pharmacology: concentration-response curves
370:
or for competitive antagonists in radioligand binding studies using the
134:, "opponent, competitor, villain, enemy, rival", which is derived from
42:
molecule, inhibiting the signal produced by a receptor–agonist coupling.
3292:
2434:
2251:
677:
608:
503:
311:
303:
169:
161:
102:
66:
35:
1777:
Principles of pharmacology: the pathophysiologic basis of drug therapy
1682:
688:, binds with weak morphine-like activity and is used clinically as an
3805:
3374:
3254:
3208:
560:
533:) competitive antagonists, depending on how they interact with their
491:
1455:
1364:
Ritter J, Flower R, Henderson G, Loke YK, MacEwan D, Rang H (2020).
713:
agonists because of the discovery of constitutive active receptors.
591:
has been shown to act as a reversible non-competitive antagonist of
1662:
Neubig RR, Spedding M, Kenakin T, Christopoulos A (December 2003).
1025:
859:
250:
raises arterial pressure through vasoconstriction mediated by alpha
126:
The
English word antagonist in pharmaceutical terms comes from the
647:
613:
344:
289:
109:
at receptors. Antagonists mediate their effects by binding to the
29:
2164:"Buprenorphine: a unique opioid with broad clinical applications"
205:
by the binding of a ligand to other sites on the receptor, as in
27:
Type of receptor ligand or drug that blocks a biological response
2826:
2719:
2715:
2517:
2065:
Patil PN (2002). "Everhardus J. Ariëns (1918–2002): a tribute".
327:
173:
58:
3212:
2384:
2380:
846:
Hopkins AL, Groom CR (September 2002). "The druggable genome".
432:
196:
between the receptor and its ligand, at locations called the
1258:"G protein-coupled receptors: a count of 1001 conformations"
582:
The second form of "non-competitive antagonists" act at an
1176:
400:(affinity constant for an antagonist) from the shift in IC
271:
at a receptor is receptor-independent property of a drug.
1318:
The Journal of Pharmacology and Experimental Therapeutics
628:
of agonist better than lower concentrations of agonist".
1890:"basic_principles_of_pharm [TUSOM | Pharmwiki]"
451:
563:, and is equivalent to the antagonist being called an
470:
Competitive antagonists bind to receptors at the same
164:
molecules that can be activated by the binding of a
3869:
3824:
3791:
3756:
3697:
3655:
3626:
3617:
3576:
3529:
3500:
3432:
3419:
3405:
3390:
3373:
3366:
3246:
3166:
3126:
3082:
3031:
3004:
2968:
2931:
2892:
2883:
2819:
2764:
2755:
2694:
2639:
2588:
2550:
2541:
2472:
2427:
2418:
1404:
Journal of Veterinary Pharmacology and Therapeutics
911:
587:for receptor activation after the agonist binds.
1487:"Taking the time to study competitive antagonism"
418:Enzyme inhibitor § Types of reversible inhibitors
1712:
1710:
1708:
1007:
1005:
1437:
1435:
1433:
517:Competitive antagonists are sub-classified as
267:receptor is expressed, altering the view that
3224:
2396:
1201:
1199:
1197:
945:
943:
941:
8:
1806:: CS1 maint: multiple names: authors list (
1303:
1301:
728:have been reclassified as inverse agonists.
692:in pain management and as an alternative to
1397:
1395:
1393:
1359:
1357:
1355:
1256:Vauquelin G, Van Liefde I (February 2005).
322:of an antagonist is usually defined by its
3623:
3429:
3416:
3370:
3231:
3217:
3209:
3163:
3123:
3028:
3001:
2965:
2928:
2889:
2816:
2761:
2691:
2636:
2585:
2547:
2469:
2424:
2403:
2389:
2381:
1769:
1767:
1765:
717:, originally classified as antagonists of
595:. Another example of a non-competitive is
486:(also known as Narcan) is used to reverse
2341:
2179:
1938:
1862:
1594:
1510:
1273:
1231:
1208:"A modification of receptor theory. 1956"
1150:
34:Antagonists will block the binding of an
636:, is an uncompetitive antagonist of the
1719:Fundamental & Clinical Pharmacology
1262:Fundamental & Clinical Pharmacology
811:
696:in the treatment of opioid dependence.
1799:
383:of an agonist alone compared to the EC
358:The affinity of an antagonist for its
298:By definition, antagonists display no
176:. Receptors can be membrane-bound, as
1884:
1882:
1218:(4 Suppl): 106–20, discussion 103–5.
324:half maximal inhibitory concentration
314:. In functional antagonist assays, a
7:
932:participating institution membership
2330:The Journal of Biological Chemistry
1368:(9 ed.). Edinburgh: Elsevier.
1057:Current Opinion in Chemical Biology
3838:Angiotensin II receptor antagonist
3782:Endocannabinoid reuptake inhibitor
3189:Minimum bactericidal concentration
2129:Trends in Pharmacological Sciences
2094:Trends in Pharmacological Sciences
2067:Trends in Pharmacological Sciences
2008:Trends in Pharmacological Sciences
1587:10.1111/j.1476-5381.1975.tb07365.x
1536:Trends in Pharmacological Sciences
1224:10.1111/j.1476-5381.1997.tb06784.x
526:
518:
65:rather than activating it like an
25:
3729:Acetylcholine receptor antagonist
3491:Norepinephrine reuptake inhibitor
2283:Clinical and Experimental Allergy
1571:"An ambiguity in receptor theory"
1485:Wyllie DJ, Chen PE (March 2007).
752:is an example of an irreversible
388:concentrations. The affinity or K
234:lowers arterial pressure through
3179:Minimum inhibitory concentration
2368:
2295:10.1046/j.0954-7894.2002.01314.x
2205:European Journal of Pharmacology
1977:10.1016/j.neuropharm.2007.07.013
1855:10.1016/j.neuropharm.2006.09.018
1731:10.1046/j.1472-8206.2002.00095.x
1416:10.1111/j.1365-2885.2004.00620.x
1275:10.1111/j.1472-8206.2005.00319.x
795:Growth factor receptor inhibitor
437:
192:. Binding occurs as a result of
3857:Vasopressin receptor antagonist
3771:Cannabinoid receptor antagonist
3119:WHO list of essential medicines
2612:Non-specific effect of vaccines
1575:British Journal of Pharmacology
1491:British Journal of Pharmacology
1212:British Journal of Pharmacology
1206:Stephenson RP (February 1997).
710:Constitutively active receptors
599:which binds irreversibly (with
3843:Endothelin receptor antagonist
3707:Acetylcholine receptor agonist
3466:Adrenergic receptor antagonist
3174:Antimicrobial pharmacodynamics
1444:Nature Reviews. Drug Discovery
1014:Nature Reviews. Drug Discovery
848:Nature Reviews. Drug Discovery
836:Retrieved on December 6, 2007.
1:
3675:Glutamate receptor antagonist
3591:Serotonin receptor antagonist
3544:Histamine receptor antagonist
3319:Negative allosteric modulator
3313:Positive allosteric modulator
3099:Functional analog (chemistry)
2162:Vadivelu N, Hines RL (2007).
2141:10.1016/S0165-6147(00)01991-X
2079:10.1016/S0165-6147(02)02068-0
968:Current Pharmaceutical Design
892:. Online Etymology Dictionary
3832:Adenosine reuptake inhibitor
3766:Cannabinoid receptor agonist
3685:Glutamate reuptake inhibitor
3604:Serotonin reuptake inhibitor
3515:Dopamine receptor antagonist
2652:Hill equation (biochemistry)
2217:10.1016/j.ejphar.2006.09.032
2168:Journal of Opioid Management
2020:10.1016/0165-6147(93)90185-m
1632:10.1016/0006-2952(73)90196-2
1366:Rang and Dale's pharmacology
800:Selective receptor modulator
3520:Dopamine reuptake inhibitor
3442:Adrenergic receptor agonist
1569:Schild HO (February 1975).
684:, a partial agonist of the
632:, used in the treatment of
3949:
3811:Opioid receptor antagonist
3665:Glutamate receptor agonist
3586:Serotonin receptor agonist
3539:Histamine receptor agonist
3167:Antimicrobial pharmacology
2647:Dose–response relationship
2577:Desensitization (medicine)
2106:10.1016/j.tips.2007.06.001
1913:Lipton SA (January 2004).
1548:10.1016/j.tips.2007.09.011
1069:10.1016/j.cbpa.2004.04.008
664:
426:
415:
278:
149:
3510:Dopamine receptor agonist
3089:Coinduction (anesthetics)
1143:10.1016/j.bcp.2005.12.038
919:Oxford English Dictionary
756:—it permanently binds to
743:Irreversible antagonists
228:physiological antagonists
194:non-covalent interactions
3776:Endocannabinoid enhancer
3722:Cholinesterase inhibitor
3641:GABA receptor antagonist
3154:Multiple drug resistance
3127:Tolerance and resistance
2495:Physiological antagonist
1620:Biochemical Pharmacology
1246:of the original article.
1131:Biochemical Pharmacology
1092:Receptors & Channels
980:10.2174/1381612043384303
778:receptor-ligand kinetics
738:receptor-ligand kinetics
490:caused by drugs such as
219:receptor occupancy model
207:allosteric binding sites
180:, or inside the cell as
83:calcium channel blockers
3816:Enkephalinase inhibitor
3806:Opioid receptor agonist
3646:GABA reuptake inhibitor
3351:♦ Miscellaneous:
2905:Neuropsychopharmacology
2667:Cheng-Prussoff Equation
2662:Del Castillo Katz model
2589:Other effects of ligand
2572:Receptor (biochemistry)
2490:Irreversible antagonist
1931:10.1602/neurorx.1.1.101
1671:Pharmacological Reviews
1330:10.1124/jpet.106.104463
924:Oxford University Press
188:including those of the
182:intracellular receptors
152:Receptor (biochemistry)
3399:Ion channel modulators
3041:Classical pharmacology
2802:Plasma protein binding
2777:Volume of distribution
2485:Competitive antagonist
2343:10.1074/jbc.M104167200
2240:Molecular Pharmacology
1503:10.1038/sj.bjp.0706997
1125:Negus SS (June 2006).
1104:10.1080/10606820214640
674:competitive antagonist
653:
619:
429:Competitive inhibition
406:competitive inhibition
372:Cheng-Prusoff equation
350:
295:
264:functional selectivity
178:cell surface receptors
43:
3636:GABA receptor agonist
3149:Antibiotic resistance
2941:Clinical pharmacology
2460:Physiological agonist
2420:Ligand (biochemistry)
2181:10.5055/jom.2007.0038
676:in the presence of a
651:
617:
565:allosteric antagonist
427:Further information:
348:
293:
33:
3923:Receptor antagonists
3046:Reverse pharmacology
2956:Pharmacoepidemiology
2797:Biological half-life
2677:Ligand binding assay
2551:Activity at receptor
2445:Irreversible agonist
2377:at Wikimedia Commons
2375:Receptor antagonists
761:adrenergic receptors
605:adrenergic receptors
547:and thus destroyed.
286:Efficacy and potency
252:-adrenergic receptor
18:Receptor antagonists
3928:Signal transduction
3852:receptor antagonist
3094:Combination therapy
2982:Pharmacoinformatics
2951:Medicinal chemistry
2557:Mechanism of action
922:(Online ed.).
634:Alzheimer's disease
404:that occurs during
316:dose-response curve
73:; examples include
48:receptor antagonist
3240:Pharmacomodulation
3064:Immunopharmacology
3014:Pharmacotoxicology
2915:Psychopharmacology
2707:Intrinsic activity
2607:Pleiotropy (drugs)
2528:Agonist-antagonist
2440:Endogenous agonist
2252:10.1124/mol.65.1.2
1894:tmedweb.tulane.edu
825:2019-07-26 at the
654:
644:Silent antagonists
620:
510:is an antidote to
502:is an antidote to
351:
296:
44:
3908:
3907:
3904:
3903:
3865:
3864:
3693:
3692:
3613:
3612:
3383:Enzyme inhibition
3206:
3205:
3202:
3201:
3162:
3161:
3059:Photopharmacology
3054:
3053:
3027:
3026:
3000:
2999:
2964:
2963:
2927:
2926:
2920:Electrophysiology
2910:Neuropharmacology
2865:
2864:
2815:
2814:
2751:
2750:
2738:Therapeutic index
2690:
2689:
2635:
2634:
2584:
2583:
2513:
2512:
2468:
2467:
2373:Media related to
1965:Neuropharmacology
1843:Neuropharmacology
1787:978-0-7817-8355-2
1683:10.1124/pr.55.4.4
1375:978-0-7020-8060-9
930:(Subscription or
686:μ-opioid receptor
468:
467:
368:Schild regression
186:nuclear receptors
16:(Redirected from
3940:
3933:Pharmacodynamics
3882:Enzyme cofactors
3801:Opioid modulator
3758:Cannabinoidergic
3624:
3430:
3417:
3371:
3233:
3226:
3219:
3210:
3164:
3124:
3104:Polypharmacology
3029:
3002:
2992:Pharmacogenomics
2987:Pharmacogenetics
2966:
2929:
2890:
2817:
2787:Rate of infusion
2762:
2757:Pharmacokinetics
2692:
2637:
2586:
2548:
2543:Pharmacodynamics
2523:Neurotransmitter
2505:Enzyme inhibitor
2470:
2425:
2405:
2398:
2391:
2382:
2372:
2356:
2355:
2345:
2336:(33): 31279–84.
2321:
2315:
2314:
2278:
2272:
2271:
2235:
2229:
2228:
2200:
2194:
2193:
2183:
2159:
2153:
2152:
2124:
2118:
2117:
2089:
2083:
2082:
2062:
2056:
2046:
2040:
2039:
2003:
1997:
1996:
1959:
1953:
1952:
1942:
1910:
1904:
1903:
1901:
1900:
1886:
1877:
1876:
1866:
1834:
1828:
1818:
1812:
1811:
1805:
1797:
1795:
1794:
1771:
1760:
1757:
1751:
1750:
1714:
1703:
1702:
1668:
1659:
1644:
1643:
1626:(23): 3099–108.
1615:
1609:
1608:
1598:
1566:
1560:
1559:
1531:
1525:
1524:
1514:
1482:
1476:
1475:
1439:
1428:
1427:
1399:
1388:
1387:
1361:
1350:
1349:
1305:
1296:
1295:
1277:
1253:
1247:
1245:
1235:
1203:
1192:
1191:
1171:
1165:
1164:
1154:
1122:
1116:
1115:
1087:
1081:
1080:
1052:
1046:
1045:
1009:
1000:
999:
963:
957:
947:
936:
935:
927:
915:
908:
902:
901:
899:
897:
886:
880:
879:
843:
837:
816:
790:Enzyme inhibitor
750:Phenoxybenzamine
700:Inverse agonists
661:Partial agonists
597:phenoxybenzamine
573:receptor reserve
535:receptor protein
463:
460:
441:
433:
312:partial agonists
308:inverse agonists
281:Pharmacodynamics
275:Pharmacodynamics
138:("against") and
21:
3948:
3947:
3943:
3942:
3941:
3939:
3938:
3937:
3913:
3912:
3909:
3900:
3861:
3851:
3820:
3787:
3752:
3689:
3651:
3609:
3598:
3572:
3567:
3559:
3551:
3525:
3496:
3410:
3401:
3386:
3362:
3308:Inverse agonist
3298:Partial agonist
3242:
3237:
3207:
3198:
3158:
3144:Drug resistance
3122:
3078:
3050:
3023:
3019:Neurotoxicology
2996:
2960:
2923:
2885:
2879:
2861:
2811:
2807:Bioavailability
2792:Onset of action
2747:
2686:
2631:
2580:
2537:
2509:
2500:Inverse agonist
2464:
2450:Partial agonist
2414:
2409:
2365:
2360:
2359:
2323:
2322:
2318:
2280:
2279:
2275:
2237:
2236:
2232:
2202:
2201:
2197:
2161:
2160:
2156:
2126:
2125:
2121:
2091:
2090:
2086:
2064:
2063:
2059:
2047:
2043:
2005:
2004:
2000:
1961:
1960:
1956:
1912:
1911:
1907:
1898:
1896:
1888:
1887:
1880:
1836:
1835:
1831:
1819:
1815:
1798:
1792:
1790:
1788:
1773:
1772:
1763:
1758:
1754:
1716:
1715:
1706:
1666:
1661:
1660:
1647:
1617:
1616:
1612:
1568:
1567:
1563:
1533:
1532:
1528:
1484:
1483:
1479:
1456:10.1038/nrd1500
1441:
1440:
1431:
1401:
1400:
1391:
1376:
1363:
1362:
1353:
1307:
1306:
1299:
1255:
1254:
1250:
1205:
1204:
1195:
1173:
1172:
1168:
1137:(12): 1663–70.
1124:
1123:
1119:
1089:
1088:
1084:
1054:
1053:
1049:
1011:
1010:
1003:
974:(17): 2003–13.
965:
964:
960:
948:
939:
929:
910:
909:
905:
895:
893:
888:
887:
883:
845:
844:
840:
827:Wayback Machine
817:
813:
808:
786:
734:
725:
706:inverse agonist
702:
669:
667:Partial agonist
663:
646:
625:
593:mGluR1 receptor
553:
551:Non-competitive
512:benzodiazepines
488:opioid overdose
464:
458:
455:
448:needs expansion
442:
431:
425:
420:
414:
403:
399:
395:
391:
386:
382:
377:
365:
356:
340:
336:
331:
288:
283:
277:
259:receptor theory
243:
154:
148:
130:ἀνταγωνιστής –
124:
115:allosteric site
107:inverse agonist
28:
23:
22:
15:
12:
11:
5:
3946:
3944:
3936:
3935:
3930:
3925:
3915:
3914:
3906:
3905:
3902:
3901:
3899:
3898:
3886:
3873:
3871:
3867:
3866:
3863:
3862:
3860:
3859:
3854:
3849:
3845:
3840:
3835:
3828:
3826:
3822:
3821:
3819:
3818:
3813:
3808:
3803:
3797:
3795:
3789:
3788:
3786:
3785:
3779:
3773:
3768:
3762:
3760:
3754:
3753:
3751:
3750:
3744:
3735:
3726:
3725:
3724:
3713:
3703:
3701:
3695:
3694:
3691:
3690:
3688:
3687:
3682:
3672:
3661:
3659:
3653:
3652:
3650:
3649:
3643:
3638:
3632:
3630:
3621:
3615:
3614:
3611:
3610:
3608:
3607:
3601:
3596:
3588:
3582:
3580:
3574:
3573:
3571:
3570:
3565:
3561:
3557:
3553:
3549:
3541:
3535:
3533:
3527:
3526:
3524:
3523:
3517:
3512:
3506:
3504:
3498:
3497:
3495:
3494:
3488:
3482:
3476:
3463:
3457:
3448:
3438:
3436:
3427:
3414:
3403:
3402:
3396:
3394:
3388:
3387:
3379:
3377:
3368:
3364:
3363:
3361:
3360:
3355:
3348:
3347:
3341:
3335:
3323:
3322:
3316:
3310:
3305:
3300:
3295:
3284:
3283:
3278:
3267:
3266:
3261:
3250:
3248:
3244:
3243:
3238:
3236:
3235:
3228:
3221:
3213:
3204:
3203:
3200:
3199:
3197:
3196:
3191:
3186:
3184:Bacteriostatic
3181:
3176:
3170:
3168:
3160:
3159:
3157:
3156:
3151:
3146:
3141:
3136:
3134:Drug tolerance
3130:
3128:
3121:
3116:
3114:Lists of drugs
3111:
3106:
3101:
3096:
3091:
3086:
3084:
3080:
3079:
3077:
3076:
3071:
3066:
3061:
3055:
3052:
3051:
3049:
3048:
3043:
3037:
3035:
3033:Drug discovery
3025:
3024:
3022:
3021:
3016:
3010:
3008:
2998:
2997:
2995:
2994:
2989:
2984:
2978:
2976:
2962:
2961:
2959:
2958:
2953:
2948:
2943:
2937:
2935:
2925:
2924:
2922:
2917:
2912:
2907:
2902:
2900:
2887:
2881:
2880:
2878:
2877:
2875:Bioequivalence
2872:
2866:
2863:
2862:
2860:
2859:
2849:
2844:
2839:
2834:
2823:
2821:
2813:
2812:
2810:
2809:
2804:
2799:
2794:
2789:
2784:
2774:
2768:
2766:
2759:
2753:
2752:
2749:
2748:
2746:
2745:
2740:
2735:
2709:
2704:
2698:
2696:
2688:
2687:
2685:
2684:
2669:
2664:
2659:
2654:
2649:
2643:
2641:
2633:
2632:
2630:
2629:
2619:
2617:Adverse effect
2614:
2609:
2604:
2592:
2590:
2582:
2581:
2579:
2574:
2569:
2564:
2562:Mode of action
2559:
2554:
2552:
2545:
2539:
2538:
2536:
2535:
2530:
2525:
2520:
2514:
2511:
2510:
2508:
2507:
2502:
2497:
2492:
2487:
2482:
2476:
2474:
2466:
2465:
2463:
2462:
2457:
2452:
2447:
2442:
2437:
2431:
2429:
2422:
2416:
2415:
2410:
2408:
2407:
2400:
2393:
2385:
2379:
2378:
2364:
2363:External links
2361:
2358:
2357:
2316:
2273:
2230:
2195:
2154:
2119:
2084:
2057:
2041:
1998:
1971:(6): 699–723.
1954:
1905:
1878:
1829:
1813:
1786:
1761:
1752:
1704:
1677:(4): 597–606.
1645:
1610:
1561:
1542:(12): 608–14.
1526:
1477:
1429:
1410:(6): 397–414.
1389:
1374:
1351:
1297:
1248:
1193:
1166:
1117:
1098:(5–6): 261–8.
1082:
1047:
1026:10.1038/nrd746
1020:(3): 198–210.
1001:
958:
937:
903:
881:
860:10.1038/nrd892
838:
810:
809:
807:
804:
803:
802:
797:
792:
785:
782:
733:
730:
723:
715:Antihistamines
701:
698:
665:Main article:
662:
659:
645:
642:
624:
621:
601:covalent bonds
552:
549:
531:insurmountable
466:
465:
445:
443:
436:
424:
421:
413:
410:
401:
397:
393:
389:
384:
380:
375:
363:
355:
352:
338:
334:
329:
287:
284:
279:Main article:
276:
273:
241:
150:Main article:
147:
144:
123:
120:
75:alpha blockers
50:is a type of
26:
24:
14:
13:
10:
9:
6:
4:
3:
2:
3945:
3934:
3931:
3929:
3926:
3924:
3921:
3920:
3918:
3911:
3896:
3895:
3890:
3887:
3884:
3883:
3878:
3875:
3874:
3872:
3870:Miscellaneous
3868:
3858:
3855:
3853:
3846:
3844:
3841:
3839:
3836:
3833:
3830:
3829:
3827:
3823:
3817:
3814:
3812:
3809:
3807:
3804:
3802:
3799:
3798:
3796:
3794:
3790:
3783:
3780:
3777:
3774:
3772:
3769:
3767:
3764:
3763:
3761:
3759:
3755:
3748:
3745:
3743:
3739:
3736:
3734:
3730:
3727:
3723:
3720:
3719:
3717:
3714:
3712:
3708:
3705:
3704:
3702:
3700:
3696:
3686:
3683:
3680:
3676:
3673:
3670:
3666:
3663:
3662:
3660:
3658:
3657:Glutamatergic
3654:
3647:
3644:
3642:
3639:
3637:
3634:
3633:
3631:
3629:
3625:
3622:
3620:
3616:
3605:
3602:
3599:
3592:
3589:
3587:
3584:
3583:
3581:
3579:
3575:
3568:
3562:
3560:
3554:
3552:
3545:
3542:
3540:
3537:
3536:
3534:
3532:
3531:Histaminergic
3528:
3521:
3518:
3516:
3513:
3511:
3508:
3507:
3505:
3503:
3499:
3492:
3489:
3486:
3483:
3480:
3477:
3475:
3471:
3467:
3464:
3461:
3458:
3456:
3452:
3449:
3447:
3443:
3440:
3439:
3437:
3435:
3431:
3428:
3426:
3422:
3418:
3415:
3413:
3408:
3404:
3400:
3395:
3393:
3389:
3385:
3384:
3378:
3376:
3372:
3369:
3365:
3359:
3356:
3354:
3350:
3349:
3345:
3342:
3339:
3336:
3333:
3329:
3325:
3324:
3320:
3317:
3314:
3311:
3309:
3306:
3304:
3301:
3299:
3296:
3294:
3290:
3286:
3285:
3282:
3279:
3277:
3273:
3269:
3268:
3265:
3262:
3260:
3256:
3252:
3251:
3249:
3245:
3241:
3234:
3229:
3227:
3222:
3220:
3215:
3214:
3211:
3195:
3192:
3190:
3187:
3185:
3182:
3180:
3177:
3175:
3172:
3171:
3169:
3165:
3155:
3152:
3150:
3147:
3145:
3142:
3140:
3139:Tachyphylaxis
3137:
3135:
3132:
3131:
3129:
3125:
3120:
3117:
3115:
3112:
3110:
3107:
3105:
3102:
3100:
3097:
3095:
3092:
3090:
3087:
3085:
3081:
3075:
3072:
3070:
3067:
3065:
3062:
3060:
3057:
3056:
3047:
3044:
3042:
3039:
3038:
3036:
3034:
3030:
3020:
3017:
3015:
3012:
3011:
3009:
3007:
3003:
2993:
2990:
2988:
2985:
2983:
2980:
2979:
2977:
2975:
2971:
2967:
2957:
2954:
2952:
2949:
2947:
2944:
2942:
2939:
2938:
2936:
2934:
2930:
2921:
2918:
2916:
2913:
2911:
2908:
2906:
2903:
2901:
2899:
2895:
2891:
2888:
2882:
2876:
2873:
2871:
2868:
2867:
2857:
2853:
2850:
2848:
2845:
2843:
2840:
2838:
2835:
2832:
2828:
2825:
2824:
2822:
2818:
2808:
2805:
2803:
2800:
2798:
2795:
2793:
2790:
2788:
2785:
2782:
2778:
2775:
2773:
2770:
2769:
2767:
2763:
2760:
2758:
2754:
2744:
2741:
2739:
2736:
2733:
2729:
2725:
2721:
2717:
2713:
2710:
2708:
2705:
2703:
2700:
2699:
2697:
2693:
2682:
2678:
2674:
2670:
2668:
2665:
2663:
2660:
2658:
2655:
2653:
2650:
2648:
2645:
2644:
2642:
2638:
2627:
2626:Neurotoxicity
2623:
2620:
2618:
2615:
2613:
2610:
2608:
2605:
2602:
2598:
2595:Selectivity (
2594:
2593:
2591:
2587:
2578:
2575:
2573:
2570:
2568:
2565:
2563:
2560:
2558:
2555:
2553:
2549:
2546:
2544:
2540:
2534:
2533:Pharmacophore
2531:
2529:
2526:
2524:
2521:
2519:
2516:
2515:
2506:
2503:
2501:
2498:
2496:
2493:
2491:
2488:
2486:
2483:
2481:
2478:
2477:
2475:
2471:
2461:
2458:
2456:
2453:
2451:
2448:
2446:
2443:
2441:
2438:
2436:
2433:
2432:
2430:
2426:
2423:
2421:
2417:
2413:
2406:
2401:
2399:
2394:
2392:
2387:
2386:
2383:
2376:
2371:
2367:
2366:
2362:
2353:
2349:
2344:
2339:
2335:
2331:
2327:
2320:
2317:
2312:
2308:
2304:
2300:
2296:
2292:
2289:(4): 489–98.
2288:
2284:
2277:
2274:
2269:
2265:
2261:
2257:
2253:
2249:
2245:
2241:
2234:
2231:
2226:
2222:
2218:
2214:
2210:
2206:
2199:
2196:
2191:
2187:
2182:
2177:
2173:
2169:
2165:
2158:
2155:
2150:
2146:
2142:
2138:
2134:
2130:
2123:
2120:
2115:
2111:
2107:
2103:
2100:(8): 438–46.
2099:
2095:
2088:
2085:
2080:
2076:
2072:
2068:
2061:
2058:
2055:
2054:0-632-05605-3
2051:
2045:
2042:
2037:
2033:
2029:
2025:
2021:
2017:
2014:(12): 41–48.
2013:
2009:
2002:
1999:
1994:
1990:
1986:
1982:
1978:
1974:
1970:
1966:
1958:
1955:
1950:
1946:
1941:
1936:
1932:
1928:
1925:(1): 101–10.
1924:
1920:
1916:
1909:
1906:
1895:
1891:
1885:
1883:
1879:
1874:
1870:
1865:
1860:
1856:
1852:
1849:(3): 744–54.
1848:
1844:
1840:
1833:
1830:
1827:
1826:0-7817-8355-0
1823:
1817:
1814:
1809:
1803:
1789:
1783:
1779:
1778:
1770:
1768:
1766:
1762:
1756:
1753:
1748:
1744:
1740:
1736:
1732:
1728:
1725:(4): 263–72.
1724:
1720:
1713:
1711:
1709:
1705:
1700:
1696:
1692:
1688:
1684:
1680:
1676:
1672:
1665:
1658:
1656:
1654:
1652:
1650:
1646:
1641:
1637:
1633:
1629:
1625:
1621:
1614:
1611:
1606:
1602:
1597:
1592:
1588:
1584:
1580:
1576:
1572:
1565:
1562:
1557:
1553:
1549:
1545:
1541:
1537:
1530:
1527:
1522:
1518:
1513:
1508:
1504:
1500:
1497:(5): 541–51.
1496:
1492:
1488:
1481:
1478:
1473:
1469:
1465:
1461:
1457:
1453:
1449:
1445:
1438:
1436:
1434:
1430:
1425:
1421:
1417:
1413:
1409:
1405:
1398:
1396:
1394:
1390:
1385:
1381:
1377:
1371:
1367:
1360:
1358:
1356:
1352:
1347:
1343:
1339:
1335:
1331:
1327:
1323:
1319:
1315:
1311:
1304:
1302:
1298:
1293:
1289:
1285:
1281:
1276:
1271:
1267:
1263:
1259:
1252:
1249:
1243:
1239:
1234:
1229:
1225:
1221:
1217:
1213:
1209:
1202:
1200:
1198:
1194:
1189:
1185:
1181:
1177:
1170:
1167:
1162:
1158:
1153:
1148:
1144:
1140:
1136:
1132:
1128:
1121:
1118:
1113:
1109:
1105:
1101:
1097:
1093:
1086:
1083:
1078:
1074:
1070:
1066:
1063:(3): 287–96.
1062:
1058:
1051:
1048:
1043:
1039:
1035:
1031:
1027:
1023:
1019:
1015:
1008:
1006:
1002:
997:
993:
989:
985:
981:
977:
973:
969:
962:
959:
956:
955:0-12-370599-1
952:
946:
944:
942:
938:
933:
925:
921:
920:
914:
907:
904:
891:
885:
882:
877:
873:
869:
865:
861:
857:
854:(9): 727–30.
853:
849:
842:
839:
835:
833:
832:GlaxoWellcome
828:
824:
821:
815:
812:
805:
801:
798:
796:
793:
791:
788:
787:
783:
781:
779:
773:
770:
769:noradrenaline
766:
763:, preventing
762:
759:
755:
754:alpha blocker
751:
746:
741:
739:
732:Reversibility
731:
729:
727:
720:
716:
711:
707:
699:
697:
695:
691:
687:
683:
682:Buprenorphine
679:
675:
668:
660:
658:
650:
643:
641:
639:
638:NMDA receptor
635:
631:
623:Uncompetitive
622:
616:
612:
610:
606:
602:
598:
594:
590:
589:Cyclothiazide
585:
580:
576:
574:
570:
566:
562:
558:
550:
548:
546:
545:ubiquitinated
541:
536:
532:
528:
524:
520:
515:
513:
509:
505:
501:
498:. Similarly,
497:
493:
489:
485:
480:
477:
473:
462:
459:November 2017
453:
449:
446:This section
444:
440:
435:
434:
430:
422:
419:
411:
409:
407:
373:
369:
361:
353:
347:
343:
332:
325:
321:
317:
313:
309:
305:
301:
292:
285:
282:
274:
272:
270:
265:
260:
255:
253:
249:
245:
237:
233:
229:
224:
220:
215:
210:
208:
204:
199:
195:
191:
190:mitochondrion
187:
183:
179:
175:
171:
167:
163:
159:
153:
145:
143:
141:
137:
133:
129:
121:
119:
116:
112:
108:
104:
100:
96:
92:
88:
84:
80:
79:beta blockers
76:
72:
68:
64:
60:
56:
53:
49:
41:
37:
32:
19:
3910:
3892:
3880:
3578:Serotonergic
3502:Dopaminergic
3381:
3302:
3109:Chemotherapy
3069:Cell biology
2970:Biochemistry
2894:Neuroscience
2842:Distribution
2772:Loading dose
2479:
2455:Superagonist
2412:Pharmacology
2333:
2329:
2319:
2286:
2282:
2276:
2243:
2239:
2233:
2211:(1–3): 1–9.
2208:
2204:
2198:
2174:(1): 49–58.
2171:
2167:
2157:
2135:(4): 151–3.
2132:
2128:
2122:
2097:
2093:
2087:
2073:(7): 344–5.
2070:
2066:
2060:
2044:
2011:
2007:
2001:
1968:
1964:
1957:
1922:
1918:
1908:
1897:. Retrieved
1893:
1846:
1842:
1832:
1816:
1791:. Retrieved
1776:
1755:
1722:
1718:
1674:
1670:
1623:
1619:
1613:
1578:
1574:
1564:
1539:
1535:
1529:
1494:
1490:
1480:
1450:(9): 801–8.
1447:
1443:
1407:
1403:
1365:
1321:
1317:
1268:(1): 45–56.
1265:
1261:
1251:
1215:
1211:
1182:(1): 32–49.
1179:
1175:
1169:
1134:
1130:
1120:
1095:
1091:
1085:
1060:
1056:
1050:
1017:
1013:
971:
967:
961:
917:
913:"antagonist"
906:
894:. Retrieved
890:"Antagonist"
884:
851:
847:
841:
830:
814:
774:
742:
735:
703:
678:full agonist
670:
655:
626:
581:
577:
564:
554:
530:
527:irreversible
523:surmountable
522:
516:
481:
472:binding site
469:
456:
452:adding to it
447:
360:binding site
357:
323:
297:
256:
254:activation.
236:vasodilation
222:
213:
211:
198:binding site
156:Biochemical
155:
140:agonizesthai
139:
135:
132:antagonistēs
131:
125:
90:
87:pharmacology
70:
47:
45:
3894:Amino acids
3793:Opioidergic
3699:Cholinergic
3412:transporter
3392:Ion channel
3328:Transporter
3272:Ion channel
3194:Bactericide
2870:Compartment
2681:Patch clamp
2657:Schild plot
2246:(1): 2–11.
1324:(1): 1–13.
896:28 November
603:) to alpha-
540:free energy
423:Competitive
240:histamine H
111:active site
91:antagonists
3917:Categories
3742:Ganglionic
3733:Muscarinic
3711:Muscarinic
3434:Adrenergic
3303:Antagonist
3074:Physiology
3006:Toxicology
2898:psychology
2847:Metabolism
2837:Absorption
2831:Liberation
2673:Organ bath
2601:Functional
2480:Antagonist
2473:Inhibitory
2428:Excitatory
1899:2023-07-21
1793:2012-02-05
1581:(2): 311.
1384:1081403059
934:required.)
806:References
765:adrenaline
745:covalently
584:allosteric
569:depression
557:allosteric
519:reversible
508:flumazenil
416:See also:
248:adrenaline
214:antagonist
184:, such as
168:such as a
160:are large
113:or to the
3889:Precursor
3738:Nicotinic
3716:Nicotinic
3628:GABAergic
3353:Precursor
3338:Inhibitor
3264:Inhibitor
2856:Clearance
2852:Excretion
2671:Methods (
1802:cite book
726:receptors
719:histamine
694:methadone
690:analgesic
630:Memantine
500:Ro15-4513
232:histamine
212:The term
203:regulated
158:receptors
146:Receptors
122:Etymology
3877:Cofactor
3747:Muscular
3407:Receptor
3358:Cofactor
3344:Releaser
3332:Enhancer
3326:♦
3289:Receptor
3287:♦
3270:♦
3253:♦
2974:genetics
2946:Pharmacy
2933:Medicine
2743:Affinity
2702:Efficacy
2640:Analysis
2622:Toxicity
2352:11395517
2311:11849647
2303:11972592
2260:14722230
2225:17081515
2190:17367094
2149:11931978
2114:17629964
1985:17904591
1949:15717010
1873:17095021
1739:12570014
1691:14657418
1556:18023486
1521:17245371
1472:28668800
1464:15340390
1424:15601436
1338:16803859
1284:15660959
1188:13229418
1161:16460689
1112:12690954
1077:15183327
1042:13230838
1034:12120504
996:36602982
988:15279541
876:13166282
868:12209152
823:Archived
784:See also
496:morphine
484:Naloxone
476:affinity
354:Affinity
304:agonists
300:efficacy
269:efficacy
246:, while
244:receptor
99:efficacy
95:affinity
71:blockers
63:receptor
52:receptor
40:receptor
3834:(AdoRI)
3784:(eCBRI)
3367:Classes
3293:Agonist
3281:Blocker
3259:Inducer
2884:Related
2827:(L)ADME
2781:Initial
2765:Metrics
2712:Potency
2695:Metrics
2597:Binding
2567:Binding
2435:Agonist
2036:4274320
2028:8122313
1993:6599658
1919:NeuroRx
1864:1876747
1747:6145796
1699:1729572
1640:4202581
1605:1148491
1596:1666289
1512:2189774
1310:Roth BL
1242:9142399
1233:3224279
1152:1866283
609:agonist
504:alcohol
326:(i.e.,
320:potency
238:at the
170:hormone
162:protein
103:agonist
97:but no
67:agonist
36:agonist
3778:(eCBE)
3375:Enzyme
3276:Opener
3255:Enzyme
2886:fields
2350:
2309:
2301:
2268:115140
2266:
2258:
2223:
2188:
2147:
2112:
2052:
2034:
2026:
1991:
1983:
1947:
1940:534915
1937:
1871:
1861:
1824:
1784:
1745:
1737:
1697:
1689:
1638:
1603:
1593:
1554:
1519:
1509:
1470:
1462:
1422:
1382:
1372:
1346:447937
1344:
1336:
1292:609867
1290:
1282:
1240:
1230:
1186:
1159:
1149:
1110:
1075:
1040:
1032:
994:
986:
953:
874:
866:
561:IUPHAR
492:heroin
310:, and
223:single
166:ligand
81:, and
55:ligand
3891:(see
3879:(see
3825:Other
3648:(GRI)
3606:(SRI)
3522:(DRI)
3493:(NRI)
3409:&
3321:(NAM)
3315:(PAM)
3247:Types
3083:Other
2820:LADME
2307:S2CID
2264:S2CID
2032:S2CID
1989:S2CID
1743:S2CID
1695:S2CID
1667:(PDF)
1468:S2CID
1342:S2CID
1288:S2CID
1038:S2CID
992:S2CID
928:
872:S2CID
525:) or
412:Types
172:or a
136:anti-
128:Greek
93:have
85:. In
38:at a
3679:NMDA
3669:AMPA
3595:5-HT
3397:See
3380:see
3346:(RA)
3340:(RI)
3334:(RE)
2972:and
2896:and
2732:TD50
2728:LD50
2724:ED50
2720:IC50
2716:EC50
2518:Drug
2348:PMID
2299:PMID
2256:PMID
2221:PMID
2186:PMID
2145:PMID
2110:PMID
2050:ISBN
2024:PMID
1981:PMID
1945:PMID
1869:PMID
1822:ISBN
1808:link
1782:ISBN
1735:PMID
1687:PMID
1636:PMID
1601:PMID
1552:PMID
1517:PMID
1460:PMID
1420:PMID
1380:OCLC
1370:ISBN
1334:PMID
1280:PMID
1238:PMID
1184:PMID
1157:PMID
1108:PMID
1073:PMID
1030:PMID
984:PMID
951:ISBN
898:2010
864:PMID
767:and
611:.
506:and
174:drug
59:drug
2829:: (
2338:doi
2334:276
2291:doi
2248:doi
2213:doi
2209:553
2176:doi
2137:doi
2102:doi
2075:doi
2016:doi
1973:doi
1935:PMC
1927:doi
1859:PMC
1851:doi
1727:doi
1679:doi
1628:doi
1591:PMC
1583:doi
1544:doi
1507:PMC
1499:doi
1495:150
1452:doi
1412:doi
1326:doi
1322:320
1270:doi
1228:PMC
1220:doi
1216:120
1147:PMC
1139:doi
1100:doi
1065:doi
1022:doi
976:doi
856:doi
829:."
704:An
494:or
454:.
105:or
57:or
3919::
3848:NK
3749:))
3718:)
3619:AA
3462:))
3421:BA
3330::
3291::
3274::
3257::
2730:,
2726:,
2722:,
2718:,
2679:,
2675:,
2599:,
2346:.
2332:.
2328:.
2305:.
2297:.
2287:32
2285:.
2262:.
2254:.
2244:65
2242:.
2219:.
2207:.
2184:.
2170:.
2166:.
2143:.
2133:23
2131:.
2108:.
2098:28
2096:.
2071:23
2069:.
2030:.
2022:.
2012:14
2010:.
1987:.
1979:.
1969:53
1967:.
1943:.
1933:.
1921:.
1917:.
1892:.
1881:^
1867:.
1857:.
1847:52
1845:.
1841:.
1804:}}
1800:{{
1764:^
1741:.
1733:.
1723:16
1721:.
1707:^
1693:.
1685:.
1675:55
1673:.
1669:.
1648:^
1634:.
1624:22
1622:.
1599:.
1589:.
1579:53
1577:.
1573:.
1550:.
1540:28
1538:.
1515:.
1505:.
1493:.
1489:.
1466:.
1458:.
1446:.
1432:^
1418:.
1408:27
1406:.
1392:^
1378:.
1354:^
1340:.
1332:.
1320:.
1316:.
1300:^
1286:.
1278:.
1266:19
1264:.
1260:.
1236:.
1226:.
1214:.
1210:.
1196:^
1180:99
1178:.
1155:.
1145:.
1135:71
1133:.
1129:.
1106:.
1094:.
1071:.
1059:.
1036:.
1028:.
1016:.
1004:^
990:.
982:.
972:10
970:.
940:^
916:.
870:.
862:.
850:.
740:.
640:.
514:.
402:50
385:50
381:50
362:(K
339:50
335:50
330:50
328:IC
306:,
89:,
77:,
46:A
3897:)
3885:)
3850:1
3740:(
3731:(
3709:(
3681:)
3677:(
3671:)
3667:(
3600:)
3597:3
3593:(
3569:)
3566:3
3564:H
3558:2
3556:H
3550:1
3548:H
3546:(
3487:)
3485:β
3481:)
3479:2
3474:1
3472:(
3470:α
3468:(
3460:2
3455:1
3453:(
3451:β
3446:α
3444:(
3425:M
3423:/
3232:e
3225:t
3218:v
2858:)
2854:(
2833:)
2783:)
2779:(
2734:)
2714:(
2683:)
2628:)
2624:(
2603:)
2404:e
2397:t
2390:v
2354:.
2340::
2313:.
2293::
2270:.
2250::
2227:.
2215::
2192:.
2178::
2172:3
2151:.
2139::
2116:.
2104::
2081:.
2077::
2038:.
2018::
1995:.
1975::
1951:.
1929::
1923:1
1902:.
1875:.
1853::
1810:)
1796:.
1749:.
1729::
1701:.
1681::
1642:.
1630::
1607:.
1585::
1558:.
1546::
1523:.
1501::
1474:.
1454::
1448:3
1426:.
1414::
1386:.
1348:.
1328::
1294:.
1272::
1244:.
1222::
1190:.
1163:.
1141::
1114:.
1102::
1096:8
1079:.
1067::
1061:8
1044:.
1024::
1018:1
998:.
978::
926:.
900:.
878:.
858::
852:1
834:.
818:"
758:α
724:1
722:H
529:(
521:(
461:)
457:(
398:i
394:i
390:i
376:i
364:i
242:1
20:)
Text is available under the Creative Commons Attribution-ShareAlike License. Additional terms may apply.
