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AMPA receptor positive allosteric modulator

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35: 24: 946: 862: 178:. For this reason, doubt has been cast on the feasibility of AMPAR activators for use in medicine. However, low doses of AMPAR activators may nonetheless be useful, and AMPAR PAMs, which, unlike agonists, show selectivity for AMPAR subpopulations of different subunit compositions, may hold greater potential for medical applications. 190:
on the AMPAR complex and potentiate the receptor. Unlike orthosteric (active/glutamate) site AMPAR activators, otherwise known as AMPAR agonists, AMPAR PAMs only potentiate AMPAR signaling in the presence of glutamate and hence do not activate the receptor directly/themselves. Moreover, whereas AMPAR
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Low-impact AMPAR PAMs decrease AMPAR deactivation (channel closing) alone to augment synaptic currents while high-impact AMPAR PAMs decrease both deactivation and desensitization together to enhance and prolong synaptic currents. Low-impact AMPAR PAMs have only slight effects on AMPAR currents,
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whereas high-impact AMPAR PAMs have effects more similar to those of AMPAR agonists and can produce strong enhancement. Similarly to AMPAR agonists, high-impact AMPAR PAMs can cause convulsions and neurotoxicity in sufficiently high doses. Conversely, low-impact AMPAR PAMs have few
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agonists activate all AMPARs, AMPAR PAMs can show selectivity for specific subpopulations of AMPARs. This is because the AMPAR is composed of different combinations of various subunits, and the allosteric sites differ depending on the different subunit combinations.
486:. All of the biarylpropylsulfonamides are high-impact AMPAR PAMs, whereas the majority of the ampakines are low-impact AMPAR potentiators. The biarylpropylsulfonamides are highly potent, on the order of 1,000-fold more potent than the ampakines and cyclothiazide. 694:
Ranganathan M, DeMartinis N, Huguenel B, Gaudreault F, Bednar MM, Shaffer CL, et al. (November 2017). "Attenuation of ketamine-induced impairment in verbal learning and memory in healthy volunteers by the AMPA receptor potentiator PF-04958242".
126:, and for other indications. They can broadly be divided into low-impact and high-impact potentiators, with high-impact potentiators able to produce comparatively more robust increases in AMPAR activation. However, high-impact AMPAR PAMs can cause 743:
Roberts BM, Holden DE, Shaffer CL, Seymour PA, Menniti FS, Schmidt CJ, et al. (September 2010). "Prevention of ketamine-induced working memory impairments by AMPA potentiators in a nonhuman primate model of cognitive dysfunction".
174:(CNS). Considering the broad impact of the AMPARs in the CNS, selectively targeting AMPARs involved in disease is difficult, and it is thought that global enhancement of AMPARs may be associated with an intolerable level of 1119: 941:, Simmons, Danielle & Lynch, Gary, "Treatment of female sexual dysfunction by compounds that positively modulate ampa-type glutamate receptors", published 2010-03-18, assigned to 194:
AMPAR PAMs can be broadly grouped into two types based on their binding site and impact on AMPAR activation: low-impact (type I) and high-impact (type II). Low-impact AMPAR PAMs have the following criteria:
1139: 3136: 1112: 857:, Carmichael, Stanley T & Clarkson, Andrew N, "Locally released growth factors to mediate motor recovery after stroke", issued 2017-06-21, assigned to 3158: 998:
Gudasheva TA, Grigoriev VV, Koliasnikova KN, Zamoyski VL, Seredenin SB (November 2016). "Neuropeptide cycloprolylglycine is an endogenous positive modulator of AMPA receptors".
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Black MD (April 2005). "Therapeutic potential of positive AMPA modulators and their relationship to AMPA receptor subunits. A review of preclinical data".
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Lee K, Goodman L, Fourie C, Schenk S, Leitch B, Montgomery JM (2016). "AMPA Receptors as Therapeutic Targets for Neurological Disorders".
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Froestl W, Muhs A, Pfeifer A (2012). "Cognitive enhancers (nootropics). Part 1: drugs interacting with receptors".
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Monti B, Contestabile A (June 2009). "Memory-enhancing drugs: a molecular perspective".
896: 632:. Advances in Protein Chemistry and Structural Biology. Vol. 103. pp. 203–61. 2917: 2897: 2662: 2597: 2517: 2497: 2293: 1765: 1694: 1481: 1400: 915: 880: 254: 237: 130: 91: 64: 3152: 3087: 3082: 3062: 2922: 2887: 2742: 2737: 2727: 2702: 2697: 2632: 2592: 2552: 2133: 1838: 1750: 1689: 1634: 1602: 1461: 1395: 1215: 1188: 1140: 354: 207: 138: 107: 103: 53: 1027: 34: 2877: 2707: 2677: 2582: 2547: 2482: 2467: 2245: 1746: 1719: 1674: 1471: 1457: 1425: 1375: 1330: 833: 773: 724: 23: 905: 637: 30:, one of the earliest and a prototypical AMPAR PAM. It is a low-impact AMPAR PAM. 3067: 3052: 3032: 3002: 2932: 2816: 2796: 2786: 2781: 2761: 2722: 2672: 2667: 2652: 2642: 2607: 2557: 2527: 2522: 2512: 2432: 2375: 2328: 2260: 2235: 2183: 2098: 1984: 1922: 1899: 1607: 1592: 1538: 1526: 1340: 1315: 1203: 1178: 573: 403: 309: 146: 38: 1080: 3105: 3077: 3027: 3012: 2989: 2984: 2979: 2912: 2882: 2872: 2811: 2747: 2732: 2712: 2657: 2627: 2612: 2587: 2572: 2537: 2532: 2492: 2487: 2457: 2442: 2402: 2380: 2343: 2313: 2298: 2278: 2036: 2006: 1989: 1979: 1734: 1724: 1699: 1654: 1531: 1516: 1511: 1491: 1450: 1440: 1430: 1410: 1405: 1365: 1360: 1320: 1310: 1295: 1235: 1210: 1011: 817: 757: 565: 557: 523: 499: 455: 440: 411: 391: 293: 134: 2902: 2892: 2850: 2776: 2766: 2692: 2687: 2647: 2622: 2617: 2567: 2542: 2472: 2447: 2437: 2412: 2407: 2397: 2273: 2158: 2143: 2123: 2108: 2103: 1994: 1819: 1814: 1760: 1649: 1644: 1639: 1597: 1506: 1501: 1476: 1385: 1325: 1305: 1300: 1290: 1280: 1255: 1183: 976: 561: 549: 531: 444: 399: 383: 358: 337: 261: 83: 54: 1088: 1019: 984: 924: 825: 765: 716: 655: 3047: 2845: 2752: 2577: 2562: 2477: 2392: 2308: 2198: 2080: 2011: 2001: 1863: 1729: 1627: 1435: 1046:
Investigation of the Functional Effects of Two Novel Ampakines in the CNS
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AMPAR PAMs can be broadly grouped by their impact on AMPAR activation:
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Substantially bind to the cyclothiazide site on the AMPAR complex; and
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Tooltip α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor
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Substantially alter/increase the half-width of the fEPSP; and/or
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While high-impact AMPAR PAMs have the following criteria:
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Uncompetitive pore blockers (mostly dizocilpine site):
41:(S-47445, CX-1632), a newer and high-impact AMPAR PAM. 1791: 1789: 1547: 1138: 470:These classes have divergent properties, including 199:Have little or no effect on the half-width of the 2043: 2028: 958: 956: 874: 872: 799: 797: 795: 793: 791: 789: 787: 785: 783: 738: 736: 734: 689: 687: 685: 623: 621: 619: 617: 615: 506:(Ampalex, BDP-12, BA-74, ORG-24292, SPD-420), 280:(Ampalex, BDP-12, BA-74, ORG-24292, SPD-420), 163:, and is responsible for the majority of fast 155:The AMPAR is one of the most highly expressed 1113: 1039: 1037: 879:Lorier AR, Funk GD, Greer JJ (January 2010). 8: 3159:AMPA receptor positive allosteric modulators 482:for AMPAR populations composed of different 46:AMPA receptor positive allosteric modulators 943:The Regents of the University of California 859:The Regents of the University of California 849: 847: 845: 843: 630:Ion Channels as Therapeutic Targets, Part A 3130:Metabotropic glutamate receptor modulators 1120: 1106: 1098: 1048:(Ph.D. thesis). Edinburgh Medical School. 3137:Glutamate metabolism/transport modulators 914: 904: 141:at sufficiently high doses, similarly to 1549: 611: 601:List of investigational antidepressants 201:field excitatory postsynaptic potential 2860:Alcohols/volatile anesthetics/related: 671: 661: 591:receptor positive allosteric modulator 478:, impact (i.e., low versus high), and 2016:Other positive allosteric modulators: 1796:Tooltip N-Methyl-D-aspartate receptor 264:and related compounds (also known as 7: 1000:Doklady. Biochemistry and Biophysics 439:and related compounds (very weak) – 2757:Ifenprodil (NR2B) site antagonists: 1069:Mini Reviews in Medicinal Chemistry 1321:Pesampator (BIIB-104, PF-04958242) 14: 526:(CX-691, ORG-24481, SCH-900460), 296:(CX-691, ORG-24481, SCH-900460), 215:brain-derived neurotrophic factor 206:Do not substantially bind to the 213:Do not induce the expression of 2797:Rislenemdaz (CERC-301, MK-0657) 1744:Negative allosteric modulators: 1632:Positive allosteric modulators: 1455:Negative allosteric modulators: 1208:Positive allosteric modulators: 186:AMPAR PAMs bind to one or more 2033:Tooltip Dehydroepiandrosterone 1341:Tulrampator (S-47445, CX-1632) 1236:Farampator (CX-691, ORG-24448) 965:Journal of Alzheimer's Disease 210:site on the AMPAR complex; and 50:positive allosteric modulators 1: 3123:Receptor/signaling modulators 2972:Unknown/unsorted antagonists: 1536:Unknown/unsorted antagonists: 1129:Ionotropic glutamate receptor 231:Induce the expression of BDNF 61:ionotropic glutamate receptor 906:10.1371/journal.pone.0008766 638:10.1016/bs.apcsb.2015.10.004 2821:NR2A-selective antagonists: 2353:Polyamine site antagonists: 1578:Acromelic acid (acromelate) 1164:Acromelic acid (acromelate) 3175: 1261:Hydrochlorothiazide (HCTZ) 1081:10.2174/138955709788452621 746:Behavioural Brain Research 15: 3114: 2203:Glycine site antagonists: 1012:10.1134/s160767291606003x 818:10.1007/s00213-004-2065-6 758:10.1016/j.bbr.2010.03.039 568:(BIIB-104; PF-04958242), 458:(BIIB-104; PF-04958242), 414:(BIIB-104; PF-04958242), 244:Classes and list of drugs 112:mild cognitive impairment 63:which mediates most fast 2091:Competitive antagonists: 1999:Polyamine site agonists: 1985:Neboglamine (nebostinel) 1554:Tooltip Kainate receptor 596:NMDA receptor antagonist 378:and related compounds – 376:Biarylpropylsulfonamides 268:or CX compounds; mostly 253:There are several major 145:AMPAR activators (i.e., 16:Not to be confused with 3073:Pentamidine isethionate 2817:Traxoprodil (CP-101606) 2056:Epipregnanolone sulfate 977:10.3233/JAD-2012-121186 536:High-impact (type II): 3103:Allosteric modulators: 3038:Ipenoxazone (MLV-6976) 2693:Pethidine (meperidine) 2314:Licostinel (ACEA-1021) 2236:Apimostinel (NRX-1074) 1900:Apimostinel (NRX-1074) 1868:Glycine site agonists: 1700:Licostinel (ACEA-1021) 1411:Licostinel (ACEA-1021) 1296:Mibampator (LY-451395) 172:central nervous system 72:central nervous system 42: 31: 2772:CO-101244 (PD-174494) 2488:Delucemine (NPS-1506) 2438:Alazocine (SKF-10047) 498:Low-impact (type I): 249:By chemical structure 165:excitatory amino acid 147:active/glutamate site 37: 26: 2792:Radiprodil (RGH-896) 2767:Buphenine (nylidrin) 2344:Rapastinel (GLYX-13) 2159:Midafotel (d-CPPene) 2066:Pregnenolone sulfate 1990:Rapastinel (GLYX-13) 1781:Pregnenolone sulfate 1522:Pregnenolone sulfate 697:Molecular Psychiatry 312:(S-47445, CX-1632), 100:cognitive impairment 78:Medical applications 2023:-Hydroxycholesterol 1834:Homoquinolinic acid 1807:Main site agonists: 1565:Main site agonists: 1159:5-Fluorowillardiine 1156:Main site agonists: 897:2010PLoSO...5.8766L 363:hydrochlorothiazide 270:benzoylpyrrolidines 120:Alzheimer's disease 2371:Diethylenetriamine 2050:prasterone sulfate 1825:Homocysteic acid ( 1568:5-Bromowillardiine 1044:Jordan GR (2007). 806:Psychopharmacology 576:(S-47445, CX-1632) 128:motor coordination 104:cognitive symptoms 96:preclinical models 59:(AMPR), a type of 43: 32: 3146: 3145: 2997: 2953:Trichloroethylene 2898:Ethanol (alcohol) 2263: 2206:4-Cl-KYN (AV-101) 1974: 1966: 1933: 1925: 1917: 1874: 1859:Tetrazolylglycine 1828: 1766:Ethanol (alcohol) 1755:sodium thiopental 1573:5-Iodowillardiine 1482:Ethanol (alcohol) 1466:sodium thiopental 709:10.1038/mp.2017.6 703:(11): 1633–1640. 347:Benzothiadiazides 168:neurotransmission 94:-like effects in 68:neurotransmission 3166: 2995: 2948:Trichloroethanol 2508:Dextromethorphan 2261: 2045: 2034: 2030: 1972: 1964: 1931: 1923: 1915: 1872: 1826: 1797: 1793: 1555: 1551: 1386:Fanapanel (MPQX) 1146: 1142: 1122: 1115: 1108: 1099: 1093: 1092: 1064: 1058: 1057: 1041: 1032: 1031: 995: 989: 988: 960: 951: 950: 949: 945: 935: 929: 928: 918: 908: 876: 867: 866: 865: 861: 851: 838: 837: 801: 778: 777: 740: 729: 728: 691: 680: 679: 673: 669: 667: 659: 625: 447:, various others 255:chemical classes 188:allosteric sites 82:AMPAR PAMs have 56: 3174: 3173: 3169: 3168: 3167: 3165: 3164: 3163: 3149: 3148: 3147: 3142: 3110: 3008:Flufenamic acid 2943:Trichloroethane 2718:Rhynchophylline 2638:Methoxphenidine 2603:Levomilnacipran 2503:Dextromethadone 2428:α-Endopsychosin 2032: 1944:Dimethylglycine 1854:Quinolinic acid 1795: 1785: 1623:Quisqualic acid 1553: 1543: 1199:Quisqualic acid 1144: 1134: 1126: 1096: 1066: 1065: 1061: 1043: 1042: 1035: 997: 996: 992: 962: 961: 954: 947: 937: 936: 932: 878: 877: 870: 863: 853: 852: 841: 803: 802: 781: 742: 741: 732: 693: 692: 683: 670: 660: 648: 627: 626: 613: 609: 590: 583: 492: 472:allosteric site 257:of AMPAR PAMs: 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2736: 2734: 2731: 2729: 2728:Rolicyclidine 2726: 2724: 2721: 2719: 2716: 2714: 2711: 2709: 2706: 2704: 2703:Phencyclidine 2701: 2699: 2698:Phencyclamine 2696: 2694: 2691: 2689: 2686: 2684: 2681: 2679: 2676: 2674: 2671: 2669: 2666: 2664: 2661: 2659: 2656: 2654: 2651: 2649: 2646: 2644: 2641: 2639: 2636: 2634: 2633:Methoxetamine 2631: 2629: 2626: 2624: 2621: 2619: 2616: 2614: 2611: 2609: 2606: 2604: 2601: 2599: 2596: 2594: 2593:Levomethadone 2591: 2589: 2586: 2584: 2581: 2579: 2576: 2574: 2571: 2569: 2566: 2564: 2561: 2559: 2556: 2554: 2553:Fluorolintane 2551: 2549: 2546: 2544: 2541: 2539: 2536: 2534: 2531: 2529: 2526: 2524: 2521: 2519: 2516: 2514: 2511: 2509: 2506: 2504: 2501: 2499: 2496: 2494: 2491: 2489: 2486: 2484: 2481: 2479: 2476: 2474: 2471: 2469: 2466: 2464: 2461: 2459: 2456: 2454: 2451: 2449: 2446: 2444: 2441: 2439: 2436: 2434: 2431: 2429: 2426: 2424: 2421: 2419: 2416: 2414: 2411: 2409: 2406: 2404: 2401: 2399: 2396: 2394: 2391: 2389: 2386: 2382: 2379: 2377: 2374: 2372: 2369: 2367: 2364: 2362: 2359: 2357: 2354: 2350: 2347: 2345: 2342: 2340: 2337: 2335: 2332: 2330: 2327: 2325: 2322: 2320: 2317: 2315: 2312: 2310: 2307: 2305: 2302: 2300: 2297: 2295: 2292: 2290: 2287: 2285: 2282: 2280: 2277: 2275: 2272: 2270: 2267: 2265: 2259: 2257: 2254: 2252: 2249: 2247: 2244: 2242: 2239: 2237: 2234: 2232: 2229: 2227: 2224: 2222: 2219: 2217: 2214: 2212: 2209: 2207: 2204: 2200: 2197: 2195: 2192: 2190: 2187: 2185: 2182: 2180: 2177: 2175: 2172: 2170: 2167: 2165: 2162: 2160: 2157: 2155: 2152: 2150: 2147: 2145: 2142: 2140: 2137: 2135: 2134:Kaitocephalin 2132: 2130: 2127: 2125: 2122: 2120: 2117: 2115: 2112: 2110: 2107: 2105: 2102: 2100: 2097: 2095: 2092: 2089: 2086: 2085: 2082: 2079: 2077: 2074: 2072: 2069: 2067: 2064: 2062: 2059: 2057: 2054: 2051: 2047: 2041: 2038: 2031: 2026: 2024: 2022: 2017: 2013: 2010: 2008: 2005: 2003: 2000: 1996: 1993: 1991: 1988: 1986: 1983: 1981: 1978: 1976: 1970: 1968: 1962: 1960: 1957: 1955: 1952: 1950: 1947: 1945: 1942: 1940: 1937: 1935: 1929: 1927: 1921: 1919: 1913: 1911: 1908: 1906: 1903: 1901: 1898: 1896: 1893: 1891: 1888: 1886: 1883: 1881: 1878: 1876: 1869: 1865: 1862: 1860: 1857: 1855: 1852: 1850: 1847: 1845: 1842: 1840: 1839:Ibotenic acid 1837: 1835: 1832: 1830: 1823: 1821: 1818: 1816: 1813: 1811: 1808: 1805: 1802: 1801: 1799: 1794: 1788: 1782: 1779: 1777: 1774: 1772: 1769: 1767: 1764: 1762: 1759: 1756: 1752: 1751:pentobarbital 1748: 1745: 1741: 1738: 1736: 1733: 1731: 1728: 1726: 1723: 1721: 1718: 1716: 1713: 1711: 1708: 1706: 1703: 1701: 1698: 1696: 1693: 1691: 1690:Kaitocephalin 1688: 1686: 1683: 1681: 1678: 1676: 1673: 1671: 1668: 1666: 1663: 1660: 1659: 1656: 1653: 1651: 1648: 1646: 1643: 1641: 1638: 1636: 1635:Cyclothiazide 1633: 1629: 1626: 1624: 1621: 1619: 1616: 1614: 1611: 1609: 1606: 1604: 1603:Ibotenic acid 1601: 1599: 1596: 1594: 1591: 1589: 1586: 1584: 1581: 1579: 1576: 1574: 1571: 1569: 1566: 1563: 1560: 1559: 1557: 1552: 1546: 1540: 1537: 1533: 1530: 1528: 1525: 1523: 1520: 1518: 1515: 1513: 1510: 1508: 1505: 1503: 1500: 1498: 1495: 1493: 1490: 1488: 1485: 1483: 1480: 1478: 1475: 1473: 1470: 1467: 1463: 1462:pentobarbital 1459: 1456: 1452: 1449: 1447: 1444: 1442: 1439: 1437: 1434: 1432: 1429: 1427: 1424: 1422: 1419: 1417: 1414: 1412: 1409: 1407: 1404: 1402: 1399: 1397: 1396:Kaitocephalin 1394: 1392: 1389: 1387: 1384: 1382: 1379: 1377: 1374: 1372: 1369: 1367: 1364: 1362: 1359: 1357: 1354: 1352: 1349: 1346: 1345: 1342: 1339: 1337: 1334: 1332: 1329: 1327: 1324: 1322: 1319: 1317: 1314: 1312: 1309: 1307: 1304: 1302: 1299: 1297: 1294: 1292: 1289: 1287: 1284: 1282: 1279: 1277: 1274: 1272: 1269: 1267: 1264: 1262: 1259: 1257: 1254: 1252: 1249: 1247: 1244: 1242: 1239: 1237: 1234: 1232: 1229: 1227: 1224: 1222: 1219: 1217: 1216:Cyclothiazide 1214: 1212: 1209: 1205: 1202: 1200: 1197: 1195: 1192: 1190: 1189:Ibotenic acid 1187: 1185: 1182: 1180: 1177: 1175: 1172: 1170: 1167: 1165: 1162: 1160: 1157: 1154: 1151: 1150: 1148: 1143: 1137: 1133: 1130: 1123: 1118: 1116: 1111: 1109: 1104: 1103: 1100: 1090: 1086: 1082: 1078: 1075:(7): 769–81. 1074: 1070: 1063: 1060: 1055: 1051: 1047: 1040: 1038: 1034: 1029: 1025: 1021: 1017: 1013: 1009: 1005: 1001: 994: 991: 986: 982: 978: 974: 970: 966: 959: 957: 953: 944: 940: 939:US 2010069377 934: 931: 926: 922: 917: 912: 907: 902: 898: 894: 890: 886: 882: 875: 873: 869: 860: 856: 850: 848: 846: 844: 840: 835: 831: 827: 823: 819: 815: 812:(1): 154–63. 811: 807: 800: 798: 796: 794: 792: 790: 788: 786: 784: 780: 775: 771: 767: 763: 759: 755: 751: 747: 739: 737: 735: 731: 726: 722: 718: 714: 710: 706: 702: 698: 690: 688: 686: 682: 677: 665: 657: 653: 649: 647:9780128047941 643: 639: 635: 631: 624: 622: 620: 618: 616: 612: 606: 602: 599: 597: 594: 592: 585: 584: 580: 575: 571: 567: 563: 560:(LY-451395), 559: 555: 551: 547: 543: 539: 535: 533: 529: 525: 521: 517: 513: 509: 505: 501: 497: 496: 495: 489: 487: 485: 481: 477: 474:specificity, 473: 465: 461: 457: 453: 449: 446: 442: 438: 435: 433: 431: 427: 421: 417: 413: 409: 405: 401: 397: 394:(LY-451395), 393: 389: 385: 381: 377: 374: 372: 368: 364: 360: 356: 355:cyclothiazide 352: 348: 345: 343: 339: 335: 331: 327: 323: 319: 315: 311: 307: 303: 299: 295: 291: 287: 283: 279: 275: 271: 267: 263: 260: 259: 258: 256: 248: 243: 241: 239: 230: 227: 224: 223: 222: 216: 212: 209: 208:cyclothiazide 205: 202: 198: 197: 196: 192: 189: 181: 179: 177: 173: 169: 166: 162: 158: 153: 151: 148: 144: 140: 139:neurotoxicity 136: 132: 129: 125: 121: 117: 113: 109: 108:schizophrenia 105: 101: 97: 93: 89: 85: 77: 75: 73: 69: 66: 62: 58: 51: 47: 40: 36: 29: 25: 19: 3135: 3128: 3119: 3118: 3102: 3099: 2971: 2878:Cyclopropane 2859: 2842: 2820: 2756: 2708:Propoxyphene 2678:Orphenadrine 2583:Ketobemidone 2548:Eticyclidine 2483:Coronaridine 2468:ARL-15896-AR 2384: 2352: 2264:-Cycloserine 2246:Carisoprodol 2202: 2090: 2088:Antagonists: 2087: 2020: 2015: 1998: 1926:-Cycloserine 1867: 1806: 1803: 1747:Barbiturates 1743: 1720:Selurampanel 1675:Dasolampanel 1662:Antagonists: 1661: 1631: 1564: 1561: 1535: 1472:Cyclopropane 1458:Barbiturates 1454: 1426:Selurampanel 1376:Dasolampanel 1348:Antagonists: 1347: 1331:Pramiracetam 1207: 1155: 1152: 1072: 1068: 1062: 1045: 1003: 999: 993: 968: 964: 933: 891:(1): e8766. 888: 884: 809: 805: 749: 745: 700: 696: 629: 493: 469: 429: 425: 252: 234: 220: 203:(fEPSP); and 193: 185: 182:Pharmacology 154: 81: 45: 44: 3068:Pentamidine 3053:Minocycline 3033:Hodgkinsine 3003:Dexanabinol 2933:Sevoflurane 2787:Isoxsuprine 2782:Haloperidol 2762:Besonprodil 2723:Rimantadine 2673:Norketamine 2668:Noribogaine 2643:Milnacipran 2608:Levorphanol 2558:Gacyclidine 2528:Dizocilpine 2523:Diphenidine 2513:Dextrorphan 2433:Alaproclate 2376:Huperzine A 2329:Meprobamate 2289:Harkoseride 2184:Perzinfotel 2061:Plazinemdor 1608:Kainic acid 1593:Domoic acid 1539:Minocycline 1527:Sevoflurane 1204:Willardiine 1179:Domoic acid 752:(1): 41–8. 574:tulrampator 480:selectivity 464:osavampator 452:PF-04701475 408:PF-04778574 310:tulrampator 143:orthosteric 135:convulsions 131:disruptions 39:Tulrampator 3106:AGN-241751 3078:Piretanide 3028:Furosemide 3013:Flupirtine 2990:Conantokin 2985:Caroverine 2980:Bumetanide 2913:Isoflurane 2883:Desflurane 2873:Chloroform 2812:Safaprodil 2807:Ro 25-6981 2748:Tiletamine 2733:Sabeluzole 2713:Remacemide 2658:Neramexane 2628:Methorphan 2613:Loperamide 2588:Lanicemine 2573:Indantadol 2538:Esketamine 2533:Ephenidine 2493:Dexoxadrol 2458:Arketamine 2443:Amantadine 2403:3-MeO-PCMo 2381:Putrescine 2324:MDL-105519 2299:Kynurenine 2279:Gavestinel 2194:SDZ-220581 2154:MDL-100453 2037:prasterone 2007:Spermidine 1980:Milacemide 1885:ACC (ACPC) 1771:Evans blue 1735:Topiramate 1725:Tezampanel 1655:Isoflurane 1532:Talampanel 1517:Perampanel 1512:Isoflurane 1497:GYKI-53655 1492:GYKI-52466 1487:Evans blue 1451:Zonampanel 1441:Topiramate 1431:Tezampanel 1406:Kynurenine 1366:Caroverine 1361:Becampanel 1311:Oxiracetam 1211:Aniracetam 1132:modulators 855:US 9700596 607:References 570:PF-4778574 566:pesampator 558:mibampator 524:farampator 500:aniracetam 466:(TAK-653). 456:pesampator 441:aniracetam 412:pesampator 396:LY-4516146 392:mibampator 294:farampator 288:(BDP-20), 124:depression 3120:See also: 3100:Unsorted: 3043:MDL-27266 3023:FR-115427 3018:FPL-12495 2975:ARR-15896 2903:Halothane 2893:Enflurane 2851:Magnesium 2802:Ro 8-4304 2777:Eliprodil 2688:PD-137889 2648:Morphanol 2623:Methadone 2618:Memantine 2568:Ibogamine 2543:Etoxadrol 2473:ARL-16247 2463:ARL-12495 2448:Aptiganel 2413:4-MeO-PCP 2408:3-MeO-PCP 2398:3-MeO-PCE 2361:Co 101676 2334:MRZ 2/576 2284:GV-196771 2274:Felbamate 2251:CGP-39653 2231:ACEA-1328 2226:ACEA-1011 2169:NPC-17742 2164:NPC-12626 2149:LY-274614 2144:LY-235959 2139:LY-233053 2124:CGS-19755 2119:CGP-40116 2114:CGP-39653 2109:CGP-39551 2104:CGP-37849 2094:AP5 (APV) 1995:Sarcosine 1871:β-Fluoro- 1820:Glutamate 1815:Aspartate 1804:Agonists: 1761:Enflurane 1705:LY-382884 1665:ACEA-1011 1650:Halothane 1645:Enflurane 1640:Diazoxide 1613:LY-339434 1598:Glutamate 1562:Agonists: 1507:Irampanel 1502:Halothane 1477:Enflurane 1351:ACEA-1011 1326:Piracetam 1306:ORG-26576 1301:Nooglutyl 1291:LY-503430 1286:LY-451646 1281:LY-404187 1276:LY-395153 1271:LY-392098 1256:Diazoxide 1184:Glutamate 1153:Agonists: 1054:1842/1946 674:ignored ( 664:cite book 562:ORG-26576 554:LY-451646 550:LY-404187 532:piracetam 528:ORG-24448 490:By impact 445:piracetam 400:LY-503430 388:LY-450108 384:LY-404187 380:LY-392098 359:diazoxide 338:ORG-26576 276:(BA-14), 266:ampakines 262:Benzamide 157:receptors 84:cognition 3153:Category 3048:Metaphit 2958:Urethane 2846:Hydrogen 2843:Cations: 2753:Tramadol 2578:Ketamine 2563:Ibogaine 2478:Budipine 2393:3-HO-PCP 2319:LU-73068 2309:L-701324 2304:L-689560 2211:5,7-DCKA 2199:Selfotel 2081:SAGE-718 2076:SAGE-301 2071:SAGE-201 2012:Spermine 2002:Neomycin 1967:-Alanine 1959:L-687414 1918:-Alanine 1875:-alanine 1864:Theanine 1730:Theanine 1628:SYM-2081 1436:Theanine 1089:19519502 1028:11453708 1020:28058675 985:22886028 925:20098731 885:PLOS ONE 826:15672275 766:20347881 717:28242871 656:26920691 581:See also 484:subunits 450:Others: 365:(HCTZ), 351:BIIR-777 176:toxicity 150:agonists 116:dementia 65:synaptic 57:receptor 18:Ampakine 3092:saffron 2938:Toluene 2928:Octanol 2908:Hexanol 2863:Benzene 2839:TCN-213 2834:TCN-201 2829:MPX-007 2824:MPX-004 2418:8A-PDHQ 2356:Arcaine 2349:ZD-9379 2046:sulfate 1975:-Serine 1949:Glycine 1934:-Serine 1849:Proline 1776:NS-3763 1749:(e.g., 1740:UBP-302 1618:Proline 1460:(e.g., 1336:S-18986 1266:IDRA-21 1251:CX-1942 1246:CX-1739 1194:Proline 916:2808240 893:Bibcode 834:5869366 774:9432930 725:3691566 546:CX-1846 542:CX-1837 520:CX-1739 476:potency 460:GVS-111 437:Racetam 432:)-PIMSD 371:S-18986 367:IDRA-21 342:S-70340 334:CX-2076 330:CX-2007 326:CX-1942 322:CX-1837 318:CX-1796 314:CX-1739 306:CX-1501 170:in the 159:in the 118:(e.g., 102:(e.g., 70:in the 2968:Xylene 2868:Butane 2241:AV-101 1954:HA-966 1241:CX-717 1231:CX-614 1226:CX-546 1221:CX-516 1087:  1026:  1018:  983:  948:  923:  913:  864:  832:  824:  772:  764:  723:  715:  654:  644:  538:CX-701 516:CX-929 512:CX-717 508:CX-614 504:CX-516 302:CX-929 298:CX-717 290:CX-614 286:CX-554 282:CX-546 278:CX-516 217:(BDNF) 137:, and 88:memory 86:- and 28:CX-516 2963:Xenon 2423:18-MC 2388:2-MDP 2216:7-CKA 2179:PEAQX 1905:B6B21 1895:AK-51 1829:-HCA) 1792:NMDAR 1715:NS102 1446:YM90K 1141:AMPAR 1024:S2CID 830:S2CID 770:S2CID 721:S2CID 420:CMPDB 416:CMPDA 274:1-BCP 161:brain 3058:MPEP 2998:-αAA 2856:Zinc 2683:PCPr 2653:NEFA 2339:PNQX 2269:DNQX 2256:CNQX 2189:PPDA 2174:PBPD 2044:DHEA 2029:DHEA 1939:DHPG 1890:ACPD 1880:ACBD 1844:NMDA 1810:AMAA 1710:NBQX 1685:GAMS 1680:DNQX 1670:CNQX 1588:ATPA 1583:AMPA 1421:PNQX 1416:NBQX 1391:GAMS 1381:DNQX 1371:CNQX 1356:ATPO 1316:PEPA 1174:BOAA 1169:AMPA 1085:PMID 1016:PMID 981:PMID 921:PMID 822:PMID 762:PMID 713:PMID 676:help 652:PMID 642:ISBN 587:GABA 404:PEPA 272:) – 55:AMPA 48:are 2221:ACC 2129:CPP 2099:AP7 1910:CCG 1550:KAR 1077:doi 1050:hdl 1008:doi 1004:471 973:doi 911:PMC 901:doi 814:doi 810:179 754:doi 750:212 705:doi 634:doi 152:). 122:), 114:), 106:in 3155:: 2970:; 2858:; 2841:; 2819:; 2755:; 2383:; 2351:; 2201:; 2019:24 2014:; 1997:; 1866:; 1753:, 1742:; 1630:; 1534:; 1464:, 1453:; 1206:; 1083:. 1071:. 1036:^ 1022:. 1014:. 1002:. 979:. 969:32 967:. 955:^ 919:. 909:. 899:. 887:. 883:. 871:^ 842:^ 828:. 820:. 808:. 782:^ 768:. 760:. 748:. 733:^ 719:. 711:. 701:22 699:. 684:^ 668:: 666:}} 662:{{ 650:. 640:. 614:^ 572:, 564:, 556:, 552:, 548:, 544:, 540:, 530:, 522:, 518:, 514:, 510:, 502:, 462:, 454:, 443:, 422:, 418:, 410:, 406:, 402:, 398:, 390:, 386:, 382:, 369:, 361:, 357:, 353:, 349:– 340:, 336:, 332:, 328:, 324:, 320:, 316:, 308:, 304:, 300:, 292:, 284:, 240:. 133:, 110:, 74:. 3094:) 3090:( 2996:D 2262:D 2052:) 2048:( 2039:) 2035:( 2021:S 1973:L 1965:L 1932:D 1924:D 1916:D 1873:D 1827:L 1757:) 1468:) 1121:e 1114:t 1107:v 1091:. 1079:: 1073:9 1056:. 1052:: 1030:. 1010:: 987:. 975:: 927:. 903:: 895:: 889:5 836:. 816:: 776:. 756:: 727:. 707:: 678:) 658:. 636:: 589:A 430:R 428:, 426:R 424:( 20:.

Index

Ampakine

CX-516

Tulrampator
positive allosteric modulators
AMPA receptor
ionotropic glutamate receptor
synaptic
neurotransmission
central nervous system
cognition
memory
antidepressant
preclinical models
cognitive impairment
cognitive symptoms
schizophrenia
mild cognitive impairment
dementia
Alzheimer's disease
depression
motor coordination
disruptions
convulsions
neurotoxicity
orthosteric
active/glutamate site
agonists
receptors

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