669:, 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.
335:
556:. 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,
280:
604:
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463:(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
428:
769:. 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.
2359:
198:. 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.
20:
760:
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
367:
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
616:
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
575:
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
567:
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
255:
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
701:
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
106:
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
376:
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
467:
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
764:
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
368:
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
645:
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.
526:
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
214:
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
205:
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
660:
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
1951:
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".
736:
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.
531:
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
330:
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.
250:
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
189:
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
322:
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
1607:
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".
385:
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
107:
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.
397:. 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.
1904:"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"
326:
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
355:), 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
1809:
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
811:
1796:
468:
functional assays using competitive antagonists, a parallel rightward shift of agonist dose–response curves with no alteration of the maximal response is observed.
1653:"International Union of Pharmacology Committee on Receptor Nomenclature and Drug Classification. XXXVIII. Update on terms and symbols in quantitative pharmacology"
2192:
Greasley PJ, Clapham JC (December 2006). "Inverse agonism or neutral antagonism at G-protein coupled receptors: a medicinal chemistry challenge worth pursuing?".
210:. 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
291:
to activate the receptors they bind. Antagonists do not maintain the ability to activate a receptor. Once bound, however, antagonists inhibit the function of
3219:
381:
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
560:
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
568:
also be used to describe the same phenomenon without the potential for confusion with the second meaning of "non-competitive antagonism" discussed below.
1044:
Bleicher KH, Green LG, Martin RE, Rogers-Evans M (June 2004). "Ligand identification for G-protein-coupled receptors: a lead generation perspective".
761:
non-competitive and irreversible antagonist drugs, as effects of non-competitive antagonists are reversible and activity of agonist will be restored.
3673:
338:
Agonists get its maximum effect reduced when in the presence of an
Irreversible Competitive Antagonist or a Reversible Non-Competitive Antagonist.
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603:
1774:
1362:
2037:
Principles and
Practice of Pharmacology for Anaesthetists By Norton Elwy Williams, Thomas Norman Calvey Published 2001 Blackwell Publishing
2483:
2448:
1995:
Fletcher A, Cliffe IA, Dourish CT (December 1993). "Silent 5-HT1A receptor antagonists: utility as research tools and therapeutic agents".
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471:
Competitive antagonists are used to prevent the activity of drugs, and to reverse the effects of drugs that have already been consumed.
334:
3826:
3770:
3177:
2270:
Leurs R, Church MK, Taglialatela M (April 2002). "H1-antihistamines: inverse agonism, anti-inflammatory actions and cardiac effects".
2081:
Bosier B, Hermans E (August 2007). "Versatility of GPCR recognition by drugs: from biological implications to therapeutic relevance".
1391:
Lees P, Cunningham FM, Elliott J (December 2004). "Principles of pharmacodynamics and their applications in veterinary pharmacology".
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site of the receptor, or by irreversibly binding to the active site of the receptor. The former meaning has been standardised by the
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2042:
1814:
943:
581:
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Agonists require higher dose/concentration to achieve the same effect when in the presence of a reversible competitive antagonist.
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783:
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eds, David E. Golan, ed.-in-chief; Armen H. Tashjian Jr., deputy ed.; Ehrin J. Armstrong, April W. Armstrong, associate (2008).
808:
3845:
3759:
3107:
2600:
1828:"Cyclothiazide selectively inhibits mGluR1 receptors interacting with a common allosteric site for non-competitive antagonists"
1163:
Ariens EJ (September 1954). "Affinity and intrinsic activity in the theory of competitive inhibition. I. Problems and theory".
607:
Figure demonstrates the noncompetitive antagonistic behaviour of
Phenoxybenzamine on alpha-adrenergiv norepinephrine receptors.
2635:
363:. Schild regression can be used to determine the nature of antagonism as beginning either competitive or non-competitive and K
3831:
3162:
2858:
2769:
2363:
725:
Many antagonists are reversible antagonists that, like most agonists, will bind and unbind a receptor at rates determined by
279:
3911:
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measures the effect of the ability of a range of concentrations of antagonists to reverse the activity of an agonist. The
3916:
3820:
3592:
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788:
596:, which in turn reduces the fraction of available receptors and reduces the maximal effect that can be produced by the
3735:
3508:
3205:
2830:
1001:
Christopoulos A (March 2002). "Allosteric binding sites on cell-surface receptors: novel targets for drug discovery".
765:
competitively (regardless of basal efficacy), and freely associate to and dissociate from the receptor, determined by
564:(also known as spare receptors) and inhibition of the agonist response will only occur when this reserve is depleted.
544:
A non-competitive antagonist is a type of insurmountable antagonist that may act in one of two ways: by binding to an
1079:
Rees S, Morrow D, Kenakin T (2002). "GPCR drug discovery through the exploitation of allosteric drug binding sites".
2315:"Phenoxybenzamine binding reveals the helical orientation of the third transmembrane domain of adrenergic receptors"
1706:
Vauquelin G, Van Liefde I, Birzbier BB, Vanderheyden PM (August 2002). "New insights in insurmountable antagonism".
3574:
3413:
3400:
3371:
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can have effects similar to those of an antagonist, but causes a distinct set of downstream biological responses.
3921:
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3387:
3077:
2825:
2819:
907:
528:
240:
216:
182:
131:("to contend for a prize"). Antagonists were discovered in the 20th century by American biologist Bailey Edgren.
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3434:
3142:
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726:
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May LT, Avlani VA, Sexton PM, Christopoulos A (2004). "Allosteric modulation of G protein-coupled receptors".
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1116:"Some implications of receptor theory for in vivo assessment of agonists, antagonists and inverse agonists"
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Kenakin T (January 2004). "Efficacy as a vector: the relative prevalence and paucity of inverse agonism".
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Swinney DC (September 2004). "Biochemical mechanisms of drug action: what does it take for success?".
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58:. Antagonist drugs interfere in the natural operation of receptor proteins. They are sometimes called
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for their cognate receptors, and binding will disrupt the interaction and inhibit the function of an
219:, substances that have opposing physiological actions, but act at different receptors. For example,
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3082:
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439: with: information about irreversible/insurmountable competitive antagonists. You can help by
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2020:
1977:
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T. Kenakin (2006) A Pharmacology Primer: Theory, Applications, and
Methods. 2nd Edition Elsevier
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Chart demonstrating the difference between agonists, silent antagonists, and inverse agonists
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Pulvirenti L, Koob GF (April 2002). "Being partial to psychostimulant addiction therapy".
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Stevens, E. (2013) Medicinal
Chemistry: The Modern Drug Discovery Process. pg. 79, 84
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Colquhoun D (December 2007). "Why the Schild method is better than Schild realised".
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1769:(2nd ed.). Philadelphia, Pa., : Lippincott Williams & Wilkins. p. 25.
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Urban JD, Clarke WP, von
Zastrow M, Nichols DE, Kobilka B, Weinstein H, Javitch JA,
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1301:, Christopoulos A, Sexton PM, Miller KJ, Spedding M, Mailman RB (January 2007).
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Surin A, Pshenichkin S, Grajkowska E, Surina E, Wroblewski JT (March 2007).
1318:
1303:"Functional selectivity and classical concepts of quantitative pharmacology"
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Our understanding of the mechanism of drug-induced receptor activation and
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that blocks or dampens a biological response by binding to and blocking a
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Frang H, Cockcroft V, Karskela T, Scheinin M, Marjamäki A (August 2001).
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809:
Pharmacology Guide: In vitro pharmacology: concentration-response curves
359:
or for competitive antagonists in radioligand binding studies using the
123:, "opponent, competitor, villain, enemy, rival", which is derived from
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molecule, inhibiting the signal produced by a receptor–agonist coupling.
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2423:
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Principles of pharmacology: the pathophysiologic basis of drug therapy
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677:, binds with weak morphine-like activity and is used clinically as an
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3363:
3243:
3197:
549:
522:) competitive antagonists, depending on how they interact with their
480:
1444:
1353:
Ritter J, Flower R, Henderson G, Loke YK, MacEwan D, Rang H (2020).
702:
agonists because of the discovery of constitutive active receptors.
580:
has been shown to act as a reversible non-competitive antagonist of
1651:
Neubig RR, Spedding M, Kenakin T, Christopoulos A (December 2003).
1014:
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239:
raises arterial pressure through vasoconstriction mediated by alpha
115:
The
English word antagonist in pharmaceutical terms comes from the
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at receptors. Antagonists mediate their effects by binding to the
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2153:"Buprenorphine: a unique opioid with broad clinical applications"
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by the binding of a ligand to other sites on the receptor, as in
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Type of receptor ligand or drug that blocks a biological response
2815:
2708:
2704:
2506:
2054:
Patil PN (2002). "Everhardus J. Ariëns (1918–2002): a tribute".
316:
162:
47:
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2373:
2369:
835:
Hopkins AL, Groom CR (September 2002). "The druggable genome".
421:
185:
between the receptor and its ligand, at locations called the
1247:"G protein-coupled receptors: a count of 1001 conformations"
571:
The second form of "non-competitive antagonists" act at an
1165:
389:(affinity constant for an antagonist) from the shift in IC
260:
at a receptor is receptor-independent property of a drug.
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The Journal of Pharmacology and Experimental Therapeutics
617:
of agonist better than lower concentrations of agonist".
1879:"basic_principles_of_pharm [TUSOM | Pharmwiki]"
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552:, and is equivalent to the antagonist being called an
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Competitive antagonists bind to receptors at the same
153:
molecules that can be activated by the binding of a
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576:for receptor activation after the agonist binds.
1476:"Taking the time to study competitive antagonism"
407:Enzyme inhibitor § Types of reversible inhibitors
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1245:Vauquelin G, Van Liefde I (February 2005).
311:of an antagonist is usually defined by its
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1197:"A modification of receptor theory. 1956"
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23:Antagonists will block the binding of an
625:, is an uncompetitive antagonist of the
1708:Fundamental & Clinical Pharmacology
1251:Fundamental & Clinical Pharmacology
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685:in the treatment of opioid dependence.
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372:of an agonist alone compared to the EC
347:The affinity of an antagonist for its
287:By definition, antagonists display no
165:. Receptors can be membrane-bound, as
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1207:(4 Suppl): 106–20, discussion 103–5.
313:half maximal inhibitory concentration
303:. In functional antagonist assays, a
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921:participating institution membership
2319:The Journal of Biological Chemistry
1357:(9 ed.). Edinburgh: Elsevier.
1046:Current Opinion in Chemical Biology
3827:Angiotensin II receptor antagonist
3771:Endocannabinoid reuptake inhibitor
3178:Minimum bactericidal concentration
2118:Trends in Pharmacological Sciences
2083:Trends in Pharmacological Sciences
2056:Trends in Pharmacological Sciences
1997:Trends in Pharmacological Sciences
1576:10.1111/j.1476-5381.1975.tb07365.x
1525:Trends in Pharmacological Sciences
1213:10.1111/j.1476-5381.1997.tb06784.x
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3718:Acetylcholine receptor antagonist
3480:Norepinephrine reuptake inhibitor
2272:Clinical and Experimental Allergy
1560:"An ambiguity in receptor theory"
1474:Wyllie DJ, Chen PE (March 2007).
741:is an example of an irreversible
377:concentrations. The affinity or K
223:lowers arterial pressure through
3168:Minimum inhibitory concentration
2357:
2284:10.1046/j.0954-7894.2002.01314.x
2194:European Journal of Pharmacology
1966:10.1016/j.neuropharm.2007.07.013
1844:10.1016/j.neuropharm.2006.09.018
1720:10.1046/j.1472-8206.2002.00095.x
1405:10.1111/j.1365-2885.2004.00620.x
1264:10.1111/j.1472-8206.2005.00319.x
784:Growth factor receptor inhibitor
426:
181:. Binding occurs as a result of
3846:Vasopressin receptor antagonist
3760:Cannabinoid receptor antagonist
3108:WHO list of essential medicines
2601:Non-specific effect of vaccines
1564:British Journal of Pharmacology
1480:British Journal of Pharmacology
1201:British Journal of Pharmacology
1195:Stephenson RP (February 1997).
699:Constitutively active receptors
588:which binds irreversibly (with
3832:Endothelin receptor antagonist
3696:Acetylcholine receptor agonist
3455:Adrenergic receptor antagonist
3163:Antimicrobial pharmacodynamics
1433:Nature Reviews. Drug Discovery
1003:Nature Reviews. Drug Discovery
837:Nature Reviews. Drug Discovery
825:Retrieved on December 6, 2007.
1:
3664:Glutamate receptor antagonist
3580:Serotonin receptor antagonist
3533:Histamine receptor antagonist
3308:Negative allosteric modulator
3302:Positive allosteric modulator
3088:Functional analog (chemistry)
2151:Vadivelu N, Hines RL (2007).
2130:10.1016/S0165-6147(00)01991-X
2068:10.1016/S0165-6147(02)02068-0
957:Current Pharmaceutical Design
881:. Online Etymology Dictionary
3821:Adenosine reuptake inhibitor
3755:Cannabinoid receptor agonist
3674:Glutamate reuptake inhibitor
3593:Serotonin reuptake inhibitor
3504:Dopamine receptor antagonist
2641:Hill equation (biochemistry)
2206:10.1016/j.ejphar.2006.09.032
2157:Journal of Opioid Management
2009:10.1016/0165-6147(93)90185-m
1621:10.1016/0006-2952(73)90196-2
1355:Rang and Dale's pharmacology
789:Selective receptor modulator
3509:Dopamine reuptake inhibitor
3431:Adrenergic receptor agonist
1558:Schild HO (February 1975).
673:, a partial agonist of the
621:, used in the treatment of
3940:
3800:Opioid receptor antagonist
3654:Glutamate receptor agonist
3575:Serotonin receptor agonist
3528:Histamine receptor agonist
3156:Antimicrobial pharmacology
2636:Dose–response relationship
2566:Desensitization (medicine)
2095:10.1016/j.tips.2007.06.001
1902:Lipton SA (January 2004).
1537:10.1016/j.tips.2007.09.011
1058:10.1016/j.cbpa.2004.04.008
653:
415:
404:
267:
138:
3499:Dopamine receptor agonist
3078:Coinduction (anesthetics)
1132:10.1016/j.bcp.2005.12.038
908:Oxford English Dictionary
745:—it permanently binds to
732:Irreversible antagonists
217:physiological antagonists
183:non-covalent interactions
3765:Endocannabinoid enhancer
3711:Cholinesterase inhibitor
3630:GABA receptor antagonist
3143:Multiple drug resistance
3116:Tolerance and resistance
2484:Physiological antagonist
1609:Biochemical Pharmacology
1235:of the original article.
1120:Biochemical Pharmacology
1081:Receptors & Channels
969:10.2174/1381612043384303
767:receptor-ligand kinetics
727:receptor-ligand kinetics
479:caused by drugs such as
208:receptor occupancy model
196:allosteric binding sites
169:, or inside the cell as
72:calcium channel blockers
3805:Enkephalinase inhibitor
3795:Opioid receptor agonist
3635:GABA reuptake inhibitor
3340:♦ Miscellaneous:
2894:Neuropsychopharmacology
2656:Cheng-Prussoff Equation
2651:Del Castillo Katz model
2578:Other effects of ligand
2561:Receptor (biochemistry)
2479:Irreversible antagonist
1920:10.1602/neurorx.1.1.101
1660:Pharmacological Reviews
1319:10.1124/jpet.106.104463
913:Oxford University Press
177:including those of the
171:intracellular receptors
141:Receptor (biochemistry)
3388:Ion channel modulators
3030:Classical pharmacology
2791:Plasma protein binding
2766:Volume of distribution
2474:Competitive antagonist
2332:10.1074/jbc.M104167200
2229:Molecular Pharmacology
1492:10.1038/sj.bjp.0706997
1114:Negus SS (June 2006).
1093:10.1080/10606820214640
663:competitive antagonist
642:
608:
418:Competitive inhibition
395:competitive inhibition
361:Cheng-Prusoff equation
339:
284:
253:functional selectivity
167:cell surface receptors
32:
3625:GABA receptor agonist
3138:Antibiotic resistance
2930:Clinical pharmacology
2449:Physiological agonist
2409:Ligand (biochemistry)
2170:10.5055/jom.2007.0038
665:in the presence of a
640:
606:
554:allosteric antagonist
416:Further information:
337:
282:
22:
3912:Receptor antagonists
3035:Reverse pharmacology
2945:Pharmacoepidemiology
2786:Biological half-life
2666:Ligand binding assay
2540:Activity at receptor
2434:Irreversible agonist
2366:at Wikimedia Commons
2364:Receptor antagonists
750:adrenergic receptors
594:adrenergic receptors
536:and thus destroyed.
275:Efficacy and potency
241:-adrenergic receptor
3917:Signal transduction
3841:receptor antagonist
3083:Combination therapy
2971:Pharmacoinformatics
2940:Medicinal chemistry
2546:Mechanism of action
911:(Online ed.).
623:Alzheimer's disease
393:that occurs during
305:dose-response curve
62:; examples include
37:receptor antagonist
3229:Pharmacomodulation
3053:Immunopharmacology
3003:Pharmacotoxicology
2904:Psychopharmacology
2696:Intrinsic activity
2596:Pleiotropy (drugs)
2517:Agonist-antagonist
2429:Endogenous agonist
2241:10.1124/mol.65.1.2
1883:tmedweb.tulane.edu
814:2019-07-26 at the
643:
633:Silent antagonists
609:
499:is an antidote to
491:is an antidote to
340:
285:
33:
3897:
3896:
3893:
3892:
3854:
3853:
3682:
3681:
3602:
3601:
3372:Enzyme inhibition
3195:
3194:
3191:
3190:
3151:
3150:
3048:Photopharmacology
3043:
3042:
3016:
3015:
2989:
2988:
2953:
2952:
2916:
2915:
2909:Electrophysiology
2899:Neuropharmacology
2854:
2853:
2804:
2803:
2740:
2739:
2727:Therapeutic index
2679:
2678:
2624:
2623:
2573:
2572:
2502:
2501:
2457:
2456:
2362:Media related to
1954:Neuropharmacology
1832:Neuropharmacology
1776:978-0-7817-8355-2
1672:10.1124/pr.55.4.4
1364:978-0-7020-8060-9
919:(Subscription or
675:μ-opioid receptor
457:
456:
357:Schild regression
175:nuclear receptors
3929:
3922:Pharmacodynamics
3871:Enzyme cofactors
3790:Opioid modulator
3747:Cannabinoidergic
3613:
3419:
3406:
3360:
3222:
3215:
3208:
3199:
3153:
3113:
3093:Polypharmacology
3018:
2991:
2981:Pharmacogenomics
2976:Pharmacogenetics
2955:
2918:
2879:
2806:
2776:Rate of infusion
2751:
2746:Pharmacokinetics
2681:
2626:
2575:
2537:
2532:Pharmacodynamics
2512:Neurotransmitter
2494:Enzyme inhibitor
2459:
2414:
2394:
2387:
2380:
2371:
2361:
2345:
2344:
2334:
2325:(33): 31279–84.
2310:
2304:
2303:
2267:
2261:
2260:
2224:
2218:
2217:
2189:
2183:
2182:
2172:
2148:
2142:
2141:
2113:
2107:
2106:
2078:
2072:
2071:
2051:
2045:
2035:
2029:
2028:
1992:
1986:
1985:
1948:
1942:
1941:
1931:
1899:
1893:
1892:
1890:
1889:
1875:
1866:
1865:
1855:
1823:
1817:
1807:
1801:
1800:
1794:
1786:
1784:
1783:
1760:
1749:
1746:
1740:
1739:
1703:
1692:
1691:
1657:
1648:
1633:
1632:
1615:(23): 3099–108.
1604:
1598:
1597:
1587:
1555:
1549:
1548:
1520:
1514:
1513:
1503:
1471:
1465:
1464:
1428:
1417:
1416:
1388:
1377:
1376:
1350:
1339:
1338:
1294:
1285:
1284:
1266:
1242:
1236:
1234:
1224:
1192:
1181:
1180:
1160:
1154:
1153:
1143:
1111:
1105:
1104:
1076:
1070:
1069:
1041:
1035:
1034:
998:
989:
988:
952:
946:
936:
925:
924:
916:
904:
897:
891:
890:
888:
886:
875:
869:
868:
832:
826:
805:
779:Enzyme inhibitor
739:Phenoxybenzamine
689:Inverse agonists
650:Partial agonists
586:phenoxybenzamine
562:receptor reserve
524:receptor protein
452:
449:
430:
422:
301:partial agonists
297:inverse agonists
270:Pharmacodynamics
264:Pharmacodynamics
127:("against") and
3939:
3938:
3932:
3931:
3930:
3928:
3927:
3926:
3902:
3901:
3898:
3889:
3850:
3840:
3809:
3776:
3741:
3678:
3640:
3598:
3587:
3561:
3556:
3548:
3540:
3514:
3485:
3399:
3390:
3375:
3351:
3297:Inverse agonist
3287:Partial agonist
3231:
3226:
3196:
3187:
3147:
3133:Drug resistance
3111:
3067:
3039:
3012:
3008:Neurotoxicology
2985:
2949:
2912:
2874:
2868:
2850:
2800:
2796:Bioavailability
2781:Onset of action
2736:
2675:
2620:
2569:
2526:
2498:
2489:Inverse agonist
2453:
2439:Partial agonist
2403:
2398:
2354:
2349:
2348:
2312:
2311:
2307:
2269:
2268:
2264:
2226:
2225:
2221:
2191:
2190:
2186:
2150:
2149:
2145:
2115:
2114:
2110:
2080:
2079:
2075:
2053:
2052:
2048:
2036:
2032:
1994:
1993:
1989:
1950:
1949:
1945:
1901:
1900:
1896:
1887:
1885:
1877:
1876:
1869:
1825:
1824:
1820:
1808:
1804:
1787:
1781:
1779:
1777:
1762:
1761:
1752:
1747:
1743:
1705:
1704:
1695:
1655:
1650:
1649:
1636:
1606:
1605:
1601:
1557:
1556:
1552:
1522:
1521:
1517:
1473:
1472:
1468:
1445:10.1038/nrd1500
1430:
1429:
1420:
1390:
1389:
1380:
1365:
1352:
1351:
1342:
1296:
1295:
1288:
1244:
1243:
1239:
1194:
1193:
1184:
1162:
1161:
1157:
1126:(12): 1663–70.
1113:
1112:
1108:
1078:
1077:
1073:
1043:
1042:
1038:
1000:
999:
992:
963:(17): 2003–13.
954:
953:
949:
937:
928:
918:
899:
898:
894:
884:
882:
877:
876:
872:
834:
833:
829:
816:Wayback Machine
806:
802:
797:
775:
723:
714:
695:inverse agonist
691:
658:
656:Partial agonist
652:
635:
614:
582:mGluR1 receptor
542:
540:Non-competitive
501:benzodiazepines
477:opioid overdose
453:
447:
444:
437:needs expansion
431:
420:
414:
409:
403:
392:
388:
384:
380:
375:
371:
366:
354:
345:
329:
325:
320:
277:
272:
266:
248:receptor theory
232:
143:
137:
119:ἀνταγωνιστής –
113:
104:allosteric site
96:inverse agonist
17:
12:
11:
5:
3937:
3936:
3933:
3925:
3924:
3919:
3914:
3904:
3903:
3895:
3894:
3891:
3890:
3888:
3887:
3875:
3862:
3860:
3856:
3855:
3852:
3851:
3849:
3848:
3843:
3838:
3834:
3829:
3824:
3817:
3815:
3811:
3810:
3808:
3807:
3802:
3797:
3792:
3786:
3784:
3778:
3777:
3775:
3774:
3768:
3762:
3757:
3751:
3749:
3743:
3742:
3740:
3739:
3733:
3724:
3715:
3714:
3713:
3702:
3692:
3690:
3684:
3683:
3680:
3679:
3677:
3676:
3671:
3661:
3650:
3648:
3642:
3641:
3639:
3638:
3632:
3627:
3621:
3619:
3610:
3604:
3603:
3600:
3599:
3597:
3596:
3590:
3585:
3577:
3571:
3569:
3563:
3562:
3560:
3559:
3554:
3550:
3546:
3542:
3538:
3530:
3524:
3522:
3516:
3515:
3513:
3512:
3506:
3501:
3495:
3493:
3487:
3486:
3484:
3483:
3477:
3471:
3465:
3452:
3446:
3437:
3427:
3425:
3416:
3403:
3392:
3391:
3385:
3383:
3377:
3376:
3368:
3366:
3357:
3353:
3352:
3350:
3349:
3344:
3337:
3336:
3330:
3324:
3312:
3311:
3305:
3299:
3294:
3289:
3284:
3273:
3272:
3267:
3256:
3255:
3250:
3239:
3237:
3233:
3232:
3227:
3225:
3224:
3217:
3210:
3202:
3193:
3192:
3189:
3188:
3186:
3185:
3180:
3175:
3173:Bacteriostatic
3170:
3165:
3159:
3157:
3149:
3148:
3146:
3145:
3140:
3135:
3130:
3125:
3123:Drug tolerance
3119:
3117:
3110:
3105:
3103:Lists of drugs
3100:
3095:
3090:
3085:
3080:
3075:
3073:
3069:
3068:
3066:
3065:
3060:
3055:
3050:
3044:
3041:
3040:
3038:
3037:
3032:
3026:
3024:
3022:Drug discovery
3014:
3013:
3011:
3010:
3005:
2999:
2997:
2987:
2986:
2984:
2983:
2978:
2973:
2967:
2965:
2951:
2950:
2948:
2947:
2942:
2937:
2932:
2926:
2924:
2914:
2913:
2911:
2906:
2901:
2896:
2891:
2889:
2876:
2870:
2869:
2867:
2866:
2864:Bioequivalence
2861:
2855:
2852:
2851:
2849:
2848:
2838:
2833:
2828:
2823:
2812:
2810:
2802:
2801:
2799:
2798:
2793:
2788:
2783:
2778:
2773:
2763:
2757:
2755:
2748:
2742:
2741:
2738:
2737:
2735:
2734:
2729:
2724:
2698:
2693:
2687:
2685:
2677:
2676:
2674:
2673:
2658:
2653:
2648:
2643:
2638:
2632:
2630:
2622:
2621:
2619:
2618:
2608:
2606:Adverse effect
2603:
2598:
2593:
2581:
2579:
2571:
2570:
2568:
2563:
2558:
2553:
2551:Mode of action
2548:
2543:
2541:
2534:
2528:
2527:
2525:
2524:
2519:
2514:
2509:
2503:
2500:
2499:
2497:
2496:
2491:
2486:
2481:
2476:
2471:
2465:
2463:
2455:
2454:
2452:
2451:
2446:
2441:
2436:
2431:
2426:
2420:
2418:
2411:
2405:
2404:
2399:
2397:
2396:
2389:
2382:
2374:
2368:
2367:
2353:
2352:External links
2350:
2347:
2346:
2305:
2262:
2219:
2184:
2143:
2108:
2073:
2046:
2030:
1987:
1960:(6): 699–723.
1943:
1894:
1867:
1818:
1802:
1775:
1750:
1741:
1693:
1666:(4): 597–606.
1634:
1599:
1550:
1531:(12): 608–14.
1515:
1466:
1418:
1399:(6): 397–414.
1378:
1363:
1340:
1286:
1237:
1182:
1155:
1106:
1087:(5–6): 261–8.
1071:
1036:
1015:10.1038/nrd746
1009:(3): 198–210.
990:
947:
926:
892:
870:
849:10.1038/nrd892
827:
799:
798:
796:
793:
792:
791:
786:
781:
774:
771:
722:
719:
712:
704:Antihistamines
690:
687:
654:Main article:
651:
648:
634:
631:
613:
610:
590:covalent bonds
541:
538:
520:insurmountable
455:
454:
434:
432:
425:
413:
410:
402:
399:
390:
386:
382:
378:
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364:
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323:
318:
276:
273:
268:Main article:
265:
262:
230:
139:Main article:
136:
133:
112:
109:
64:alpha blockers
39:is a type of
15:
13:
10:
9:
6:
4:
3:
2:
3935:
3934:
3923:
3920:
3918:
3915:
3913:
3910:
3909:
3907:
3900:
3885:
3884:
3879:
3876:
3873:
3872:
3867:
3864:
3863:
3861:
3859:Miscellaneous
3857:
3847:
3844:
3842:
3835:
3833:
3830:
3828:
3825:
3822:
3819:
3818:
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3675:
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3659:
3655:
3652:
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3647:
3646:Glutamatergic
3643:
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3620:
3618:
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3551:
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3534:
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3529:
3526:
3525:
3523:
3521:
3520:Histaminergic
3517:
3510:
3507:
3505:
3502:
3500:
3497:
3496:
3494:
3492:
3488:
3481:
3478:
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3407:
3404:
3402:
3397:
3393:
3389:
3384:
3382:
3378:
3374:
3373:
3367:
3365:
3361:
3358:
3354:
3348:
3345:
3343:
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3328:
3325:
3322:
3318:
3314:
3313:
3309:
3306:
3303:
3300:
3298:
3295:
3293:
3290:
3288:
3285:
3283:
3279:
3275:
3274:
3271:
3268:
3266:
3262:
3258:
3257:
3254:
3251:
3249:
3245:
3241:
3240:
3238:
3234:
3230:
3223:
3218:
3216:
3211:
3209:
3204:
3203:
3200:
3184:
3181:
3179:
3176:
3174:
3171:
3169:
3166:
3164:
3161:
3160:
3158:
3154:
3144:
3141:
3139:
3136:
3134:
3131:
3129:
3128:Tachyphylaxis
3126:
3124:
3121:
3120:
3118:
3114:
3109:
3106:
3104:
3101:
3099:
3096:
3094:
3091:
3089:
3086:
3084:
3081:
3079:
3076:
3074:
3070:
3064:
3061:
3059:
3056:
3054:
3051:
3049:
3046:
3045:
3036:
3033:
3031:
3028:
3027:
3025:
3023:
3019:
3009:
3006:
3004:
3001:
3000:
2998:
2996:
2992:
2982:
2979:
2977:
2974:
2972:
2969:
2968:
2966:
2964:
2960:
2956:
2946:
2943:
2941:
2938:
2936:
2933:
2931:
2928:
2927:
2925:
2923:
2919:
2910:
2907:
2905:
2902:
2900:
2897:
2895:
2892:
2890:
2888:
2884:
2880:
2877:
2871:
2865:
2862:
2860:
2857:
2856:
2846:
2842:
2839:
2837:
2834:
2832:
2829:
2827:
2824:
2821:
2817:
2814:
2813:
2811:
2807:
2797:
2794:
2792:
2789:
2787:
2784:
2782:
2779:
2777:
2774:
2771:
2767:
2764:
2762:
2759:
2758:
2756:
2752:
2749:
2747:
2743:
2733:
2730:
2728:
2725:
2722:
2718:
2714:
2710:
2706:
2702:
2699:
2697:
2694:
2692:
2689:
2688:
2686:
2682:
2671:
2667:
2663:
2659:
2657:
2654:
2652:
2649:
2647:
2644:
2642:
2639:
2637:
2634:
2633:
2631:
2627:
2616:
2615:Neurotoxicity
2612:
2609:
2607:
2604:
2602:
2599:
2597:
2594:
2591:
2587:
2584:Selectivity (
2583:
2582:
2580:
2576:
2567:
2564:
2562:
2559:
2557:
2554:
2552:
2549:
2547:
2544:
2542:
2538:
2535:
2533:
2529:
2523:
2522:Pharmacophore
2520:
2518:
2515:
2513:
2510:
2508:
2505:
2504:
2495:
2492:
2490:
2487:
2485:
2482:
2480:
2477:
2475:
2472:
2470:
2467:
2466:
2464:
2460:
2450:
2447:
2445:
2442:
2440:
2437:
2435:
2432:
2430:
2427:
2425:
2422:
2421:
2419:
2415:
2412:
2410:
2406:
2402:
2395:
2390:
2388:
2383:
2381:
2376:
2375:
2372:
2365:
2360:
2356:
2355:
2351:
2342:
2338:
2333:
2328:
2324:
2320:
2316:
2309:
2306:
2301:
2297:
2293:
2289:
2285:
2281:
2278:(4): 489–98.
2277:
2273:
2266:
2263:
2258:
2254:
2250:
2246:
2242:
2238:
2234:
2230:
2223:
2220:
2215:
2211:
2207:
2203:
2199:
2195:
2188:
2185:
2180:
2176:
2171:
2166:
2162:
2158:
2154:
2147:
2144:
2139:
2135:
2131:
2127:
2123:
2119:
2112:
2109:
2104:
2100:
2096:
2092:
2089:(8): 438–46.
2088:
2084:
2077:
2074:
2069:
2065:
2061:
2057:
2050:
2047:
2044:
2043:0-632-05605-3
2040:
2034:
2031:
2026:
2022:
2018:
2014:
2010:
2006:
2003:(12): 41–48.
2002:
1998:
1991:
1988:
1983:
1979:
1975:
1971:
1967:
1963:
1959:
1955:
1947:
1944:
1939:
1935:
1930:
1925:
1921:
1917:
1914:(1): 101–10.
1913:
1909:
1905:
1898:
1895:
1884:
1880:
1874:
1872:
1868:
1863:
1859:
1854:
1849:
1845:
1841:
1838:(3): 744–54.
1837:
1833:
1829:
1822:
1819:
1816:
1815:0-7817-8355-0
1812:
1806:
1803:
1798:
1792:
1778:
1772:
1768:
1767:
1759:
1757:
1755:
1751:
1745:
1742:
1737:
1733:
1729:
1725:
1721:
1717:
1714:(4): 263–72.
1713:
1709:
1702:
1700:
1698:
1694:
1689:
1685:
1681:
1677:
1673:
1669:
1665:
1661:
1654:
1647:
1645:
1643:
1641:
1639:
1635:
1630:
1626:
1622:
1618:
1614:
1610:
1603:
1600:
1595:
1591:
1586:
1581:
1577:
1573:
1569:
1565:
1561:
1554:
1551:
1546:
1542:
1538:
1534:
1530:
1526:
1519:
1516:
1511:
1507:
1502:
1497:
1493:
1489:
1486:(5): 541–51.
1485:
1481:
1477:
1470:
1467:
1462:
1458:
1454:
1450:
1446:
1442:
1438:
1434:
1427:
1425:
1423:
1419:
1414:
1410:
1406:
1402:
1398:
1394:
1387:
1385:
1383:
1379:
1374:
1370:
1366:
1360:
1356:
1349:
1347:
1345:
1341:
1336:
1332:
1328:
1324:
1320:
1316:
1312:
1308:
1304:
1300:
1293:
1291:
1287:
1282:
1278:
1274:
1270:
1265:
1260:
1256:
1252:
1248:
1241:
1238:
1232:
1228:
1223:
1218:
1214:
1210:
1206:
1202:
1198:
1191:
1189:
1187:
1183:
1178:
1174:
1170:
1166:
1159:
1156:
1151:
1147:
1142:
1137:
1133:
1129:
1125:
1121:
1117:
1110:
1107:
1102:
1098:
1094:
1090:
1086:
1082:
1075:
1072:
1067:
1063:
1059:
1055:
1052:(3): 287–96.
1051:
1047:
1040:
1037:
1032:
1028:
1024:
1020:
1016:
1012:
1008:
1004:
997:
995:
991:
986:
982:
978:
974:
970:
966:
962:
958:
951:
948:
945:
944:0-12-370599-1
941:
935:
933:
931:
927:
922:
914:
910:
909:
903:
896:
893:
880:
874:
871:
866:
862:
858:
854:
850:
846:
843:(9): 727–30.
842:
838:
831:
828:
824:
822:
821:GlaxoWellcome
817:
813:
810:
804:
801:
794:
790:
787:
785:
782:
780:
777:
776:
772:
770:
768:
762:
759:
758:noradrenaline
755:
752:, preventing
751:
748:
744:
743:alpha blocker
740:
735:
730:
728:
721:Reversibility
720:
718:
716:
709:
705:
700:
696:
688:
686:
684:
680:
676:
672:
671:Buprenorphine
668:
664:
657:
649:
647:
639:
632:
630:
628:
627:NMDA receptor
624:
620:
612:Uncompetitive
611:
605:
601:
599:
595:
591:
587:
583:
579:
578:Cyclothiazide
574:
569:
565:
563:
559:
555:
551:
547:
539:
537:
535:
534:ubiquitinated
530:
525:
521:
517:
513:
509:
504:
502:
498:
494:
490:
487:. Similarly,
486:
482:
478:
474:
469:
466:
462:
451:
448:November 2017
442:
438:
435:This section
433:
429:
424:
423:
419:
411:
408:
400:
398:
396:
362:
358:
350:
342:
336:
332:
321:
314:
310:
306:
302:
298:
294:
290:
281:
274:
271:
263:
261:
259:
254:
249:
244:
242:
238:
234:
226:
222:
218:
213:
209:
204:
199:
197:
193:
188:
184:
180:
179:mitochondrion
176:
172:
168:
164:
160:
156:
152:
148:
142:
134:
132:
130:
126:
122:
118:
110:
108:
105:
101:
97:
93:
89:
85:
81:
77:
73:
69:
68:beta blockers
65:
61:
57:
53:
49:
45:
42:
38:
30:
26:
21:
3899:
3881:
3869:
3567:Serotonergic
3491:Dopaminergic
3370:
3291:
3098:Chemotherapy
3058:Cell biology
2959:Biochemistry
2883:Neuroscience
2831:Distribution
2761:Loading dose
2468:
2444:Superagonist
2401:Pharmacology
2322:
2318:
2308:
2275:
2271:
2265:
2232:
2228:
2222:
2200:(1–3): 1–9.
2197:
2193:
2187:
2163:(1): 49–58.
2160:
2156:
2146:
2124:(4): 151–3.
2121:
2117:
2111:
2086:
2082:
2076:
2062:(7): 344–5.
2059:
2055:
2049:
2033:
2000:
1996:
1990:
1957:
1953:
1946:
1911:
1907:
1897:
1886:. Retrieved
1882:
1835:
1831:
1821:
1805:
1780:. Retrieved
1765:
1744:
1711:
1707:
1663:
1659:
1612:
1608:
1602:
1567:
1563:
1553:
1528:
1524:
1518:
1483:
1479:
1469:
1439:(9): 801–8.
1436:
1432:
1396:
1392:
1354:
1310:
1306:
1257:(1): 45–56.
1254:
1250:
1240:
1204:
1200:
1171:(1): 32–49.
1168:
1164:
1158:
1123:
1119:
1109:
1084:
1080:
1074:
1049:
1045:
1039:
1006:
1002:
960:
956:
950:
906:
902:"antagonist"
895:
883:. Retrieved
879:"Antagonist"
873:
840:
836:
830:
819:
803:
763:
731:
724:
692:
667:full agonist
659:
644:
615:
570:
566:
553:
543:
519:
516:irreversible
512:surmountable
511:
505:
470:
461:binding site
458:
445:
441:adding to it
436:
349:binding site
346:
312:
286:
245:
243:activation.
225:vasodilation
211:
202:
200:
187:binding site
145:Biochemical
144:
129:agonizesthai
128:
124:
121:antagonistēs
120:
114:
79:
76:pharmacology
59:
36:
34:
3883:Amino acids
3782:Opioidergic
3688:Cholinergic
3401:transporter
3381:Ion channel
3317:Transporter
3261:Ion channel
3183:Bactericide
2859:Compartment
2670:Patch clamp
2646:Schild plot
2235:(1): 2–11.
1313:(1): 1–13.
885:28 November
592:) to alpha-
529:free energy
412:Competitive
229:histamine H
100:active site
80:antagonists
3906:Categories
3731:Ganglionic
3722:Muscarinic
3700:Muscarinic
3423:Adrenergic
3292:Antagonist
3063:Physiology
2995:Toxicology
2887:psychology
2836:Metabolism
2826:Absorption
2820:Liberation
2662:Organ bath
2590:Functional
2469:Antagonist
2462:Inhibitory
2417:Excitatory
1888:2023-07-21
1782:2012-02-05
1570:(2): 311.
1373:1081403059
923:required.)
795:References
754:adrenaline
734:covalently
573:allosteric
558:depression
546:allosteric
508:reversible
497:flumazenil
405:See also:
237:adrenaline
203:antagonist
173:, such as
157:such as a
149:are large
102:or to the
3878:Precursor
3727:Nicotinic
3705:Nicotinic
3617:GABAergic
3342:Precursor
3327:Inhibitor
3253:Inhibitor
2845:Clearance
2841:Excretion
2660:Methods (
1791:cite book
715:receptors
708:histamine
683:methadone
679:analgesic
619:Memantine
489:Ro15-4513
221:histamine
201:The term
192:regulated
147:receptors
135:Receptors
111:Etymology
3866:Cofactor
3736:Muscular
3396:Receptor
3347:Cofactor
3333:Releaser
3321:Enhancer
3315:♦
3278:Receptor
3276:♦
3259:♦
3242:♦
2963:genetics
2935:Pharmacy
2922:Medicine
2732:Affinity
2691:Efficacy
2629:Analysis
2611:Toxicity
2341:11395517
2300:11849647
2292:11972592
2249:14722230
2214:17081515
2179:17367094
2138:11931978
2103:17629964
1974:17904591
1938:15717010
1862:17095021
1728:12570014
1680:14657418
1545:18023486
1510:17245371
1461:28668800
1453:15340390
1413:15601436
1327:16803859
1273:15660959
1177:13229418
1150:16460689
1101:12690954
1066:15183327
1031:13230838
1023:12120504
985:36602982
977:15279541
865:13166282
857:12209152
812:Archived
773:See also
485:morphine
473:Naloxone
465:affinity
343:Affinity
293:agonists
289:efficacy
258:efficacy
235:, while
233:receptor
88:efficacy
84:affinity
60:blockers
52:receptor
41:receptor
29:receptor
3823:(AdoRI)
3773:(eCBRI)
3356:Classes
3282:Agonist
3270:Blocker
3248:Inducer
2873:Related
2816:(L)ADME
2770:Initial
2754:Metrics
2701:Potency
2684:Metrics
2586:Binding
2556:Binding
2424:Agonist
2025:4274320
2017:8122313
1982:6599658
1908:NeuroRx
1853:1876747
1736:6145796
1688:1729572
1629:4202581
1594:1148491
1585:1666289
1501:2189774
1299:Roth BL
1231:9142399
1222:3224279
1141:1866283
598:agonist
493:alcohol
315:(i.e.,
309:potency
227:at the
159:hormone
151:protein
92:agonist
86:but no
56:agonist
25:agonist
3767:(eCBE)
3364:Enzyme
3265:Opener
3244:Enzyme
2875:fields
2339:
2298:
2290:
2257:115140
2255:
2247:
2212:
2177:
2136:
2101:
2041:
2023:
2015:
1980:
1972:
1936:
1929:534915
1926:
1860:
1850:
1813:
1773:
1734:
1726:
1686:
1678:
1627:
1592:
1582:
1543:
1508:
1498:
1459:
1451:
1411:
1371:
1361:
1335:447937
1333:
1325:
1281:609867
1279:
1271:
1229:
1219:
1175:
1148:
1138:
1099:
1064:
1029:
1021:
983:
975:
942:
863:
855:
550:IUPHAR
481:heroin
299:, and
212:single
155:ligand
70:, and
44:ligand
3880:(see
3868:(see
3814:Other
3637:(GRI)
3595:(SRI)
3511:(DRI)
3482:(NRI)
3398:&
3310:(NAM)
3304:(PAM)
3236:Types
3072:Other
2809:LADME
2296:S2CID
2253:S2CID
2021:S2CID
1978:S2CID
1732:S2CID
1684:S2CID
1656:(PDF)
1457:S2CID
1331:S2CID
1277:S2CID
1027:S2CID
981:S2CID
917:
861:S2CID
514:) or
401:Types
161:or a
125:anti-
117:Greek
82:have
74:. In
27:at a
3668:NMDA
3658:AMPA
3584:5-HT
3386:See
3369:see
3335:(RA)
3329:(RI)
3323:(RE)
2961:and
2885:and
2721:TD50
2717:LD50
2713:ED50
2709:IC50
2705:EC50
2507:Drug
2337:PMID
2288:PMID
2245:PMID
2210:PMID
2175:PMID
2134:PMID
2099:PMID
2039:ISBN
2013:PMID
1970:PMID
1934:PMID
1858:PMID
1811:ISBN
1797:link
1771:ISBN
1724:PMID
1676:PMID
1625:PMID
1590:PMID
1541:PMID
1506:PMID
1449:PMID
1409:PMID
1369:OCLC
1359:ISBN
1323:PMID
1269:PMID
1227:PMID
1173:PMID
1146:PMID
1097:PMID
1062:PMID
1019:PMID
973:PMID
940:ISBN
887:2010
853:PMID
756:and
600:.
495:and
163:drug
48:drug
2818:: (
2327:doi
2323:276
2280:doi
2237:doi
2202:doi
2198:553
2165:doi
2126:doi
2091:doi
2064:doi
2005:doi
1962:doi
1924:PMC
1916:doi
1848:PMC
1840:doi
1716:doi
1668:doi
1617:doi
1580:PMC
1572:doi
1533:doi
1496:PMC
1488:doi
1484:150
1441:doi
1401:doi
1315:doi
1311:320
1259:doi
1217:PMC
1209:doi
1205:120
1136:PMC
1128:doi
1089:doi
1054:doi
1011:doi
965:doi
845:doi
818:."
693:An
483:or
443:.
94:or
46:or
3908::
3837:NK
3738:))
3707:)
3608:AA
3451:))
3410:BA
3319::
3280::
3263::
3246::
2719:,
2715:,
2711:,
2707:,
2668:,
2664:,
2588:,
2335:.
2321:.
2317:.
2294:.
2286:.
2276:32
2274:.
2251:.
2243:.
2233:65
2231:.
2208:.
2196:.
2173:.
2159:.
2155:.
2132:.
2122:23
2120:.
2097:.
2087:28
2085:.
2060:23
2058:.
2019:.
2011:.
2001:14
1999:.
1976:.
1968:.
1958:53
1956:.
1932:.
1922:.
1910:.
1906:.
1881:.
1870:^
1856:.
1846:.
1836:52
1834:.
1830:.
1793:}}
1789:{{
1753:^
1730:.
1722:.
1712:16
1710:.
1696:^
1682:.
1674:.
1664:55
1662:.
1658:.
1637:^
1623:.
1613:22
1611:.
1588:.
1578:.
1568:53
1566:.
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