262:
efficiency of transformation of the inactive form of the drug-receptor complex to the active drug-receptor complex may not be high enough to evoke a maximal response. Since the observed response may be less than maximal in systems with no spare receptor reserve, some low efficacy agonists are referred to as partial agonists. However, it is worth bearing in mind that these terms are relative - even partial agonists may appear as full agonists in a different system/experimental setup, as when the number of receptors increases, there may be enough drug-receptor complexes for a maximum response to be produced, even with individually low efficacy of transducing the response. There are actually relatively few
274:) are in fact partial agonists or inverse agonists, but with very low efficacy (less than 10%). Compounds considered partial agonists tend to have efficacy in between this range. Another case is represented by silent agonists, which are ligands that can place a receptor, typically an ion channel, into a desensitized state with little or no apparent activation of it, forming a complex that can subsequently generate currents when treated with an allosteric modulator.
33:
46:
120:
vary in the response they produce, even when they occupy the same number of receptors. High efficacy agonists can produce the maximal response of the receptor system while occupying a relatively low proportion of the receptors in that system. There is a distinction between efficacy and intrinsic
261:
Agonists of lower efficacy are not as efficient at producing a response from the drug-bound receptor, by stabilizing the active form of the drug-bound receptor. Therefore, they may not be able to produce the same maximal response, even when they occupy the entire receptor population, as the
321:
331:
R. P. Stephenson (1925ā2004) was a
British pharmacologist. Efficacy has historically been treated as a proportionality constant between the binding of the drug and the generation of the biological response. Stephenson defined efficacy as:
538:
270:) are more accurately described as high efficacy partial agonists, as a partial agonist with efficacy over ā80-90% is indistinguishable from a full agonist in most assays. Similarly many antagonists (such as
288:
855:
759:"Identification of Ī±7 Nicotinic Acetylcholine Receptor Silent Agonists Based on the Spirocyclic Quinuclidine-Ī -Isoxazoline Scaffold: Synthesis and Electrophysiological Evaluation"
608:
679:
561:
116:
of the drug and which is proportional to both efficacy and affinity. This use of the word "efficacy" was introduced by
Stephenson (1956) to describe the way in which
438:
362:
409:
385:
613:
Stevenson and
Furchgott's models of efficacy have been criticised and many more have been developed. The models of efficacy are shown in Bindslev (2008).
469:
836:
1833:
2287:
17:
687:
1005:
963:
920:
885:
316:{\displaystyle \mathrm {IA} ={\frac {\text{maximal response to the test agonist}}{\text{maximal response to full agonist}}}}
1097:
1062:
938:"DrugāAcceptor InteractionsāModeling theoretical tools to test and evaluate experimental equilibrium effects (Book review)"
106:
2440:
2384:
1791:
62:
2093:
820:
1345:
876:
Linderman JJ (2000). "Kinetic
Modeling Approaches to Understanding Ligand Efficacy". In Kenakin T, Angus JA (eds.).
102:
2277:
1826:
1781:
2459:
2373:
1721:
1214:
267:
2445:
1776:
1472:
1383:
1249:
2267:
1921:
1915:
1701:
1326:
903:
Drug-Acceptor
Interactions: Modeling Theoretical Tools to Test and Evaluate Experimental Equilibrium Effects
214:
2434:
2206:
1254:
388:
2349:
2122:
1819:
1444:
710:"Synthesis and evaluation of a conditionally-silent agonist for the Ī±7 nicotinic acetylcholine receptor"
2188:
2027:
2014:
1985:
1930:
1179:
998:
570:
2523:
2484:
2001:
1691:
1439:
1433:
266:
full agonists or silent antagonists; many compounds usually considered to be full agonists (such as
2378:
2324:
2309:
2281:
2062:
2057:
2048:
1756:
1458:
757:
Quadri M, Matera C, SilnoviÄ A, Pismataro MC, Horenstein NA, Stokes C, et al. (August 2017).
546:
2479:
2450:
2418:
2248:
2053:
2009:
1960:
1891:
1507:
1269:
1264:
1174:
1092:
98:
2360:
2166:
1643:
1404:
1379:
1314:
1203:
1087:
113:
2491:
2335:
2068:
1955:
1751:
1543:
1022:
991:
810:
59:
There are mistakes in this article; efficacy and intrinsic activity are different properties.
444:. This model was arguably flawed in that it did not incorporate the equilibrium between the
2496:
2340:
2193:
2146:
1786:
1648:
1558:
1399:
1279:
1047:
411:
is the stimulus to the biological system. The response is generated by an unknown function
414:
338:
8:
2117:
1905:
1696:
1584:
1553:
1199:
1159:
1082:
460:
441:
105:, which is a measure of the ability of the drug to bind to its molecular target, and the
2344:
2313:
2044:
1940:
1666:
1616:
1517:
1330:
1209:
1130:
1042:
969:
783:
758:
734:
709:
656:
647:
631:
394:
370:
101:
complex to produce a maximum functional response. This must be distinguished from the
2413:
2318:
2141:
1934:
1661:
1522:
1512:
1340:
1334:
1169:
959:
916:
881:
816:
788:
739:
661:
973:
2403:
2197:
2112:
1866:
1706:
1594:
1589:
1389:
1359:
1145:
1125:
1107:
949:
906:
778:
770:
729:
721:
651:
643:
2331:
2243:
2081:
2076:
1946:
1910:
1900:
1883:
1746:
1621:
1449:
1409:
1394:
1102:
1052:
237:
189:
1304:
2023:
1878:
1861:
1736:
1716:
1635:
1477:
1219:
1164:
725:
954:
937:
2517:
2259:
2158:
2150:
2133:
2072:
1741:
1228:
1135:
878:
The
Pharmacology of Functional, Biochemical, and Recombinant Receptor Systems
463:
later improved on
Stephenson's model with the definition of efficacy, e, as
2238:
2104:
2087:
1842:
1711:
1671:
1572:
1496:
1374:
1057:
1014:
792:
774:
743:
665:
166:
143:
911:
2395:
2368:
2301:
1994:
1874:
1796:
1283:
1259:
533:{\displaystyle S=\underbrace {\varepsilon _{\mathrm {Tot} }} _{e}\cdot p}
2221:
2036:
1676:
1608:
1500:
1275:
2230:
2180:
1811:
1454:
452:
agonist-bound-receptor that is shown in the del
Castillo Katz model.
32:
2271:
1576:
1548:
1535:
1224:
672:
271:
1895:
1037:
117:
2408:
1977:
1857:
983:
857:
756:
1429:
1322:
1318:
1120:
387:
is the proportion of agonist-bound receptors (given by the
94:
1495:
1769:
1571:
707:
1729:
1191:
853:
680:"In vitro pharmacology: concentration-response curves"
573:
549:
472:
417:
397:
373:
341:
291:
282:
Intrinsic activity of a test agonist is defined as:
1153:
808:
708:Chojnacka K, Papke RL, Horenstein NA (July 2013).
602:
555:
532:
432:
403:
379:
356:
315:
2515:
901:Bindslev N (2008). "Chapter 1: Simple Agonism".
636:British Journal of Pharmacology and Chemotherapy
843:. British Pharmacological Society. 2 June 2016.
55:needs attention from an expert in pharmacology
1827:
1634:
999:
714:Bioorganic & Medicinal Chemistry Letters
148:Efficacy higher than the endogenous agonist
750:
701:
623:
1834:
1820:
1006:
992:
854:Brunton L, Chabner BA, Knollman B (2011).
629:
194:Efficacy less than the endogenous agonist
2035:
1607:
1075:
1030:
953:
910:
875:
871:
869:
867:
804:
802:
782:
733:
655:
610:is the total concentration of receptors.
171:Efficacy equal to the endogenous agonist
900:
809:Foreman JC, Johansen T, Gibb AJ (2009).
124:
31:
1534:
1242:
942:Microbial Ecology in Health and Disease
935:
455:
326:
14:
2516:
1841:
1367:
1297:
864:
799:
65:may be able to help recruit an expert.
36:Efficacy spectrum of receptor ligands.
27:Measure of relative response to a drug
1815:
987:
905:. London: CRC Press. pp. 19ā20.
277:
1422:
306:maximal response to the test agonist
39:
632:"A modification of receptor theory"
93:refer to the relative ability of a
24:
2441:Angiotensin II receptor antagonist
2385:Endocannabinoid reuptake inhibitor
1792:Minimum bactericidal concentration
648:10.1111/j.1476-5381.1956.tb00006.x
594:
591:
588:
506:
503:
500:
296:
293:
25:
2535:
2332:Acetylcholine receptor antagonist
2094:Norepinephrine reuptake inhibitor
880:. Berlin: Springer. p. 120.
812:Textbook of Receptor Pharmacology
684:Glaxo Wellcome pharmacology guide
603:{\displaystyle _{\mathrm {Tot} }}
1782:Minimum inhibitory concentration
1013:
309:maximal response to full agonist
44:
2460:Vasopressin receptor antagonist
2374:Cannabinoid receptor antagonist
1722:WHO list of essential medicines
1215:Non-specific effect of vaccines
929:
630:Stephenson RP (December 1956).
448:agonist-bound-receptor and the
2446:Endothelin receptor antagonist
2310:Acetylcholine receptor agonist
2069:Adrenergic receptor antagonist
1777:Antimicrobial pharmacodynamics
894:
847:
829:
815:(Second ed.). CRC Press.
583:
574:
495:
486:
427:
421:
13:
1:
2278:Glutamate receptor antagonist
2194:Serotonin receptor antagonist
2147:Histamine receptor antagonist
1922:Negative allosteric modulator
1916:Positive allosteric modulator
1702:Functional analog (chemistry)
948:(4). London: Routledge: 213.
616:
2435:Adenosine reuptake inhibitor
2369:Cannabinoid receptor agonist
2288:Glutamate reuptake inhibitor
2207:Serotonin reuptake inhibitor
2118:Dopamine receptor antagonist
1255:Hill equation (biochemistry)
860:(12th ed.). p. 46.
556:{\displaystyle \varepsilon }
112:, which is a measure of the
7:
2123:Dopamine reuptake inhibitor
2045:Adrenergic receptor agonist
128:
57:. The specific problem is:
10:
2540:
2414:Opioid receptor antagonist
2268:Glutamate receptor agonist
2189:Serotonin receptor agonist
2142:Histamine receptor agonist
1770:Antimicrobial pharmacology
1250:Doseāresponse relationship
1180:Desensitization (medicine)
837:"R P ('Steve') Stephenson"
726:10.1016/j.bmcl.2013.05.039
2472:
2427:
2394:
2359:
2300:
2258:
2229:
2220:
2179:
2132:
2113:Dopamine receptor agonist
2103:
2022:
2008:
1993:
1976:
1969:
1849:
1692:Coinduction (anesthetics)
1685:
1486:
1358:
1144:
1021:
955:10.1080/08910600802431931
841:Pharmacology Hall of Fame
440:, which is assumed to be
219:Affinity but no efficacy
137:
2379:Endocannabinoid enhancer
2325:Cholinesterase inhibitor
2244:GABA receptor antagonist
1757:Multiple drug resistance
1730:Tolerance and resistance
1098:Physiological antagonist
63:WikiProject Pharmacology
2419:Enkephalinase inhibitor
2409:Opioid receptor agonist
2249:GABA reuptake inhibitor
1954:♦ Miscellaneous:
1508:Neuropsychopharmacology
1270:Cheng-Prussoff Equation
1265:Del Castillo Katz model
1192:Other effects of ligand
1175:Receptor (biochemistry)
1093:Irreversible antagonist
18:Efficacy (pharmacology)
2002:Ion channel modulators
1644:Classical pharmacology
1405:Plasma protein binding
1380:Volume of distribution
1088:Competitive antagonist
775:10.1002/cmdc.201700162
604:
557:
534:
434:
405:
381:
358:
317:
37:
2239:GABA receptor agonist
1752:Antibiotic resistance
1544:Clinical pharmacology
1063:Physiological agonist
1023:Ligand (biochemistry)
912:10.4324/9781315159782
605:
558:
535:
435:
406:
382:
359:
318:
125:Mechanism of efficacy
35:
1649:Reverse pharmacology
1559:Pharmacoepidemiology
1400:Biological half-life
1280:Ligand binding assay
1154:Activity at receptor
1048:Irreversible agonist
571:
547:
470:
456:Furchgott's efficacy
433:{\displaystyle f(S)}
415:
395:
371:
357:{\displaystyle S=ep}
339:
327:Stevenson's efficacy
289:
2455:receptor antagonist
1697:Combination therapy
1585:Pharmacoinformatics
1554:Medicinal chemistry
1160:Mechanism of action
461:Robert F. Furchgott
1843:Pharmacomodulation
1667:Immunopharmacology
1617:Pharmacotoxicology
1518:Psychopharmacology
1310:Intrinsic activity
1210:Pleiotropy (drugs)
1131:Agonist-antagonist
1043:Endogenous agonist
936:Kirkeby H (2017).
600:
565:intrinsic efficacy
553:
530:
523:
516:
430:
401:
377:
354:
313:
278:Intrinsic activity
83:Intrinsic activity
38:
2511:
2510:
2507:
2506:
2468:
2467:
2296:
2295:
2216:
2215:
1986:Enzyme inhibition
1809:
1808:
1805:
1804:
1765:
1764:
1662:Photopharmacology
1657:
1656:
1630:
1629:
1603:
1602:
1567:
1566:
1530:
1529:
1523:Electrophysiology
1513:Neuropharmacology
1468:
1467:
1418:
1417:
1354:
1353:
1341:Therapeutic index
1293:
1292:
1238:
1237:
1187:
1186:
1116:
1115:
1071:
1070:
965:978-1-351-66057-0
922:978-91-977071-0-7
887:978-3-540-66124-5
769:(16): 1335ā1348.
720:(14): 4145ā4149.
580:
492:
481:
479:
404:{\displaystyle S}
380:{\displaystyle p}
311:
310:
307:
259:
258:
242:Inverse efficacy
215:Silent antagonist
80:
79:
16:(Redirected from
2531:
2524:Pharmacodynamics
2485:Enzyme cofactors
2404:Opioid modulator
2361:Cannabinoidergic
2227:
2226:
2033:
2032:
2020:
2019:
1974:
1973:
1836:
1829:
1822:
1813:
1812:
1767:
1766:
1727:
1726:
1707:Polypharmacology
1632:
1631:
1605:
1604:
1595:Pharmacogenomics
1590:Pharmacogenetics
1569:
1568:
1532:
1531:
1493:
1492:
1420:
1419:
1390:Rate of infusion
1365:
1364:
1360:Pharmacokinetics
1295:
1294:
1240:
1239:
1189:
1188:
1151:
1150:
1146:Pharmacodynamics
1126:Neurotransmitter
1108:Enzyme inhibitor
1073:
1072:
1028:
1027:
1008:
1001:
994:
985:
984:
978:
977:
957:
933:
927:
926:
914:
898:
892:
891:
873:
862:
861:
851:
845:
844:
833:
827:
826:
806:
797:
796:
786:
754:
748:
747:
737:
705:
699:
698:
696:
695:
686:. Archived from
676:
670:
669:
659:
627:
609:
607:
606:
601:
599:
598:
597:
581:
578:
562:
560:
559:
554:
539:
537:
536:
531:
522:
517:
512:
511:
510:
509:
493:
490:
439:
437:
436:
431:
410:
408:
407:
402:
386:
384:
383:
378:
363:
361:
360:
355:
322:
320:
319:
314:
312:
308:
305:
304:
299:
129:
75:
72:
66:
48:
47:
40:
21:
2539:
2538:
2534:
2533:
2532:
2530:
2529:
2528:
2514:
2513:
2512:
2503:
2464:
2454:
2423:
2390:
2355:
2292:
2254:
2212:
2201:
2175:
2170:
2162:
2154:
2128:
2099:
2013:
2004:
1989:
1965:
1911:Inverse agonist
1901:Partial agonist
1845:
1840:
1810:
1801:
1761:
1747:Drug resistance
1725:
1681:
1653:
1626:
1622:Neurotoxicology
1599:
1563:
1526:
1488:
1482:
1464:
1414:
1410:Bioavailability
1395:Onset of action
1350:
1289:
1234:
1183:
1140:
1112:
1103:Inverse agonist
1067:
1053:Partial agonist
1017:
1012:
982:
981:
966:
934:
930:
923:
899:
895:
888:
874:
865:
852:
848:
835:
834:
830:
823:
807:
800:
755:
751:
706:
702:
693:
691:
678:
677:
673:
628:
624:
619:
587:
586:
582:
577:
572:
569:
568:
548:
545:
544:
518:
499:
498:
494:
489:
482:
480:
471:
468:
467:
458:
416:
413:
412:
396:
393:
392:
372:
369:
368:
340:
337:
336:
329:
303:
292:
290:
287:
286:
280:
238:Inverse agonist
190:Partial agonist
138:% Efficacy (E)
127:
110:
76:
70:
67:
61:
49:
45:
28:
23:
22:
15:
12:
11:
5:
2537:
2527:
2526:
2509:
2508:
2505:
2504:
2502:
2501:
2489:
2476:
2474:
2470:
2469:
2466:
2465:
2463:
2462:
2457:
2452:
2448:
2443:
2438:
2431:
2429:
2425:
2424:
2422:
2421:
2416:
2411:
2406:
2400:
2398:
2392:
2391:
2389:
2388:
2382:
2376:
2371:
2365:
2363:
2357:
2356:
2354:
2353:
2347:
2338:
2329:
2328:
2327:
2316:
2306:
2304:
2298:
2297:
2294:
2293:
2291:
2290:
2285:
2275:
2264:
2262:
2256:
2255:
2253:
2252:
2246:
2241:
2235:
2233:
2224:
2218:
2217:
2214:
2213:
2211:
2210:
2204:
2199:
2191:
2185:
2183:
2177:
2176:
2174:
2173:
2168:
2164:
2160:
2156:
2152:
2144:
2138:
2136:
2130:
2129:
2127:
2126:
2120:
2115:
2109:
2107:
2101:
2100:
2098:
2097:
2091:
2085:
2079:
2066:
2060:
2051:
2041:
2039:
2030:
2017:
2006:
2005:
1999:
1997:
1991:
1990:
1982:
1980:
1971:
1967:
1966:
1964:
1963:
1958:
1951:
1950:
1944:
1938:
1926:
1925:
1919:
1913:
1908:
1903:
1898:
1887:
1886:
1881:
1870:
1869:
1864:
1853:
1851:
1847:
1846:
1839:
1838:
1831:
1824:
1816:
1807:
1806:
1803:
1802:
1800:
1799:
1794:
1789:
1787:Bacteriostatic
1784:
1779:
1773:
1771:
1763:
1762:
1760:
1759:
1754:
1749:
1744:
1739:
1737:Drug tolerance
1733:
1731:
1724:
1719:
1717:Lists of drugs
1714:
1709:
1704:
1699:
1694:
1689:
1687:
1683:
1682:
1680:
1679:
1674:
1669:
1664:
1658:
1655:
1654:
1652:
1651:
1646:
1640:
1638:
1636:Drug discovery
1628:
1627:
1625:
1624:
1619:
1613:
1611:
1601:
1600:
1598:
1597:
1592:
1587:
1581:
1579:
1565:
1564:
1562:
1561:
1556:
1551:
1546:
1540:
1538:
1528:
1527:
1525:
1520:
1515:
1510:
1505:
1503:
1490:
1484:
1483:
1481:
1480:
1478:Bioequivalence
1475:
1469:
1466:
1465:
1463:
1462:
1452:
1447:
1442:
1437:
1426:
1424:
1416:
1415:
1413:
1412:
1407:
1402:
1397:
1392:
1387:
1377:
1371:
1369:
1362:
1356:
1355:
1352:
1351:
1349:
1348:
1343:
1338:
1312:
1307:
1301:
1299:
1291:
1290:
1288:
1287:
1272:
1267:
1262:
1257:
1252:
1246:
1244:
1236:
1235:
1233:
1232:
1222:
1220:Adverse effect
1217:
1212:
1207:
1195:
1193:
1185:
1184:
1182:
1177:
1172:
1167:
1165:Mode of action
1162:
1157:
1155:
1148:
1142:
1141:
1139:
1138:
1133:
1128:
1123:
1117:
1114:
1113:
1111:
1110:
1105:
1100:
1095:
1090:
1085:
1079:
1077:
1069:
1068:
1066:
1065:
1060:
1055:
1050:
1045:
1040:
1034:
1032:
1025:
1019:
1018:
1011:
1010:
1003:
996:
988:
980:
979:
964:
928:
921:
893:
886:
863:
846:
828:
821:
798:
749:
700:
671:
642:(4): 379ā393.
621:
620:
618:
615:
596:
593:
590:
585:
576:
552:
541:
540:
529:
526:
521:
515:
508:
505:
502:
497:
488:
485:
478:
475:
457:
454:
429:
426:
423:
420:
400:
376:
365:
364:
353:
350:
347:
344:
328:
325:
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323:
302:
298:
295:
279:
276:
257:
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123:
108:
78:
77:
52:
50:
43:
26:
9:
6:
4:
3:
2:
2536:
2525:
2522:
2521:
2519:
2499:
2498:
2493:
2490:
2487:
2486:
2481:
2478:
2477:
2475:
2473:Miscellaneous
2471:
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2458:
2456:
2449:
2447:
2444:
2442:
2439:
2436:
2433:
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2333:
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2323:
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2320:
2317:
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2311:
2308:
2307:
2305:
2303:
2299:
2289:
2286:
2283:
2279:
2276:
2273:
2269:
2266:
2265:
2263:
2261:
2260:Glutamatergic
2257:
2250:
2247:
2245:
2242:
2240:
2237:
2236:
2234:
2232:
2228:
2225:
2223:
2219:
2208:
2205:
2202:
2195:
2192:
2190:
2187:
2186:
2184:
2182:
2178:
2171:
2165:
2163:
2157:
2155:
2148:
2145:
2143:
2140:
2139:
2137:
2135:
2134:Histaminergic
2131:
2124:
2121:
2119:
2116:
2114:
2111:
2110:
2108:
2106:
2102:
2095:
2092:
2089:
2086:
2083:
2080:
2078:
2074:
2070:
2067:
2064:
2061:
2059:
2055:
2052:
2050:
2046:
2043:
2042:
2040:
2038:
2034:
2031:
2029:
2025:
2021:
2018:
2016:
2011:
2007:
2003:
1998:
1996:
1992:
1988:
1987:
1981:
1979:
1975:
1972:
1968:
1962:
1959:
1957:
1953:
1952:
1948:
1945:
1942:
1939:
1936:
1932:
1928:
1927:
1923:
1920:
1917:
1914:
1912:
1909:
1907:
1904:
1902:
1899:
1897:
1893:
1889:
1888:
1885:
1882:
1880:
1876:
1872:
1871:
1868:
1865:
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1859:
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1848:
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1837:
1832:
1830:
1825:
1823:
1818:
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1814:
1798:
1795:
1793:
1790:
1788:
1785:
1783:
1780:
1778:
1775:
1774:
1772:
1768:
1758:
1755:
1753:
1750:
1748:
1745:
1743:
1742:Tachyphylaxis
1740:
1738:
1735:
1734:
1732:
1728:
1723:
1720:
1718:
1715:
1713:
1710:
1708:
1705:
1703:
1700:
1698:
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1690:
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1684:
1678:
1675:
1673:
1670:
1668:
1665:
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1660:
1659:
1650:
1647:
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1642:
1641:
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1633:
1623:
1620:
1618:
1615:
1614:
1612:
1610:
1606:
1596:
1593:
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1586:
1583:
1582:
1580:
1578:
1574:
1570:
1560:
1557:
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1547:
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1537:
1533:
1524:
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1516:
1514:
1511:
1509:
1506:
1504:
1502:
1498:
1494:
1491:
1485:
1479:
1476:
1474:
1471:
1470:
1460:
1456:
1453:
1451:
1448:
1446:
1443:
1441:
1438:
1435:
1431:
1428:
1427:
1425:
1421:
1411:
1408:
1406:
1403:
1401:
1398:
1396:
1393:
1391:
1388:
1385:
1381:
1378:
1376:
1373:
1372:
1370:
1366:
1363:
1361:
1357:
1347:
1344:
1342:
1339:
1336:
1332:
1328:
1324:
1320:
1316:
1313:
1311:
1308:
1306:
1303:
1302:
1300:
1296:
1285:
1281:
1277:
1273:
1271:
1268:
1266:
1263:
1261:
1258:
1256:
1253:
1251:
1248:
1247:
1245:
1241:
1230:
1229:Neurotoxicity
1226:
1223:
1221:
1218:
1216:
1213:
1211:
1208:
1205:
1201:
1198:Selectivity (
1197:
1196:
1194:
1190:
1181:
1178:
1176:
1173:
1171:
1168:
1166:
1163:
1161:
1158:
1156:
1152:
1149:
1147:
1143:
1137:
1136:Pharmacophore
1134:
1132:
1129:
1127:
1124:
1122:
1119:
1118:
1109:
1106:
1104:
1101:
1099:
1096:
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1089:
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1035:
1033:
1029:
1026:
1024:
1020:
1016:
1009:
1004:
1002:
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989:
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924:
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897:
889:
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850:
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838:
832:
824:
822:9781439887578
818:
814:
813:
805:
803:
794:
790:
785:
780:
776:
772:
768:
764:
760:
753:
745:
741:
736:
731:
727:
723:
719:
715:
711:
704:
690:on 2019-07-26
689:
685:
681:
675:
667:
663:
658:
653:
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633:
626:
622:
614:
611:
566:
550:
527:
524:
519:
513:
483:
476:
473:
466:
465:
464:
462:
453:
451:
447:
443:
424:
418:
398:
390:
389:Hill equation
374:
351:
348:
345:
342:
335:
334:
333:
300:
285:
284:
283:
275:
273:
269:
265:
255:
253:
250:
247:
244:
241:
239:
236:
235:
232:
230:
227:
224:
221:
218:
216:
213:
212:
208:
205:
202:
199:
196:
193:
191:
188:
187:
184:
182:
179:
176:
173:
170:
168:
165:
164:
161:
159:
156:
153:
150:
147:
145:
142:
141:
134:
131:
130:
122:
119:
115:
111:
104:
100:
96:
92:
88:
84:
74:
64:
60:
56:
53:This article
51:
42:
41:
34:
30:
19:
2495:
2483:
2181:Serotonergic
2105:Dopaminergic
1984:
1712:Chemotherapy
1672:Cell biology
1573:Biochemistry
1497:Neuroscience
1445:Distribution
1375:Loading dose
1309:
1058:Superagonist
1015:Pharmacology
945:
941:
931:
902:
896:
877:
856:
849:
840:
831:
811:
766:
762:
752:
717:
713:
703:
692:. Retrieved
688:the original
683:
674:
639:
635:
625:
612:
564:
542:
459:
449:
445:
366:
330:
281:
263:
260:
167:Full agonist
144:Superagonist
135:Description
90:
86:
82:
81:
68:
58:
54:
29:
2497:Amino acids
2396:Opioidergic
2302:Cholinergic
2015:transporter
1995:Ion channel
1931:Transporter
1875:Ion channel
1797:Bactericide
1473:Compartment
1284:Patch clamp
1260:Schild plot
763:ChemMedChem
446:inactivated
2345:Ganglionic
2336:Muscarinic
2314:Muscarinic
2037:Adrenergic
1906:Antagonist
1677:Physiology
1609:Toxicology
1501:psychology
1450:Metabolism
1440:Absorption
1434:Liberation
1276:Organ bath
1204:Functional
1083:Antagonist
1076:Inhibitory
1031:Excitatory
694:2009-07-11
617:References
442:hyperbolic
121:activity.
71:April 2019
2492:Precursor
2341:Nicotinic
2319:Nicotinic
2231:GABAergic
1956:Precursor
1941:Inhibitor
1867:Inhibitor
1459:Clearance
1455:Excretion
1274:Methods (
551:ε
525:⋅
514:⏟
484:ε
450:activated
2518:Category
2480:Cofactor
2350:Muscular
2010:Receptor
1961:Cofactor
1947:Releaser
1935:Enhancer
1929:♦
1892:Receptor
1890:♦
1873:♦
1856:♦
1577:genetics
1549:Pharmacy
1536:Medicine
1346:Affinity
1305:Efficacy
1243:Analysis
1225:Toxicity
974:83584731
793:28494140
744:23746476
666:13383117
272:naloxone
118:agonists
103:affinity
99:receptor
91:efficacy
2437:(AdoRI)
2387:(eCBRI)
1970:Classes
1896:Agonist
1884:Blocker
1862:Inducer
1487:Related
1430:(L)ADME
1384:Initial
1368:Metrics
1315:Potency
1298:Metrics
1200:Binding
1170:Binding
1038:Agonist
784:5573630
735:3882203
657:1510558
563:is the
132:Ligand
114:potency
2381:(eCBE)
1978:Enzyme
1879:Opener
1858:Enzyme
1489:fields
972:
962:
919:
884:
819:
791:
781:
742:
732:
664:
654:
543:where
391:) and
367:where
89:) and
2494:(see
2482:(see
2428:Other
2251:(GRI)
2209:(SRI)
2125:(DRI)
2096:(NRI)
2012:&
1924:(NAM)
1918:(PAM)
1850:Types
1686:Other
1423:LADME
970:S2CID
248:<
206:<
200:<
154:>
2282:NMDA
2272:AMPA
2198:5-HT
2000:See
1983:see
1949:(RA)
1943:(RI)
1937:(RE)
1575:and
1499:and
1335:TD50
1331:LD50
1327:ED50
1323:IC50
1319:EC50
1121:Drug
960:ISBN
917:ISBN
882:ISBN
817:ISBN
789:PMID
740:PMID
662:PMID
567:and
264:true
209:100
180:100
157:100
95:drug
1432:: (
950:doi
907:doi
779:PMC
771:doi
730:PMC
722:doi
652:PMC
644:doi
268:DOI
2520::
2451:NK
2352:))
2321:)
2222:AA
2065:))
2024:BA
1933::
1894::
1877::
1860::
1333:,
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968:.
958:.
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301:=
297:A
294:I
97:-
85:(
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69:(
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Text is available under the Creative Commons Attribution-ShareAlike License. Additional terms may apply.
