251:
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
263:) 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.
22:
35:
109:
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
250:
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
310:
320:
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:
527:
259:) 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
277:
844:
748:"Identification of Ī±7 Nicotinic Acetylcholine Receptor Silent Agonists Based on the Spirocyclic Quinuclidine-Ī -Isoxazoline Scaffold: Synthesis and Electrophysiological Evaluation"
597:
668:
550:
105:
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
427:
351:
398:
374:
602:
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).
458:
825:
1822:
2276:
676:
994:
952:
909:
874:
305:{\displaystyle \mathrm {IA} ={\frac {\text{maximal response to the test agonist}}{\text{maximal response to full agonist}}}}
1086:
1051:
927:"DrugāAcceptor InteractionsāModeling theoretical tools to test and evaluate experimental equilibrium effects (Book review)"
95:
2429:
2373:
1780:
51:
2082:
809:
1334:
865:
Linderman JJ (2000). "Kinetic
Modeling Approaches to Understanding Ligand Efficacy". In Kenakin T, Angus JA (eds.).
91:
2266:
1815:
1770:
2448:
2362:
1710:
1203:
256:
2434:
1765:
1461:
1372:
1238:
2256:
1910:
1904:
1690:
1315:
892:
Drug-Acceptor
Interactions: Modeling Theoretical Tools to Test and Evaluate Experimental Equilibrium Effects
203:
2423:
2195:
1243:
377:
2338:
2111:
1808:
1433:
699:"Synthesis and evaluation of a conditionally-silent agonist for the Ī±7 nicotinic acetylcholine receptor"
2177:
2016:
2003:
1974:
1919:
1168:
987:
559:
2512:
2473:
1990:
1680:
1428:
1422:
255:
full agonists or silent antagonists; many compounds usually considered to be full agonists (such as
2367:
2313:
2298:
2270:
2051:
2046:
2037:
1745:
1447:
746:
Quadri M, Matera C, SilnoviÄ A, Pismataro MC, Horenstein NA, Stokes C, et al. (August 2017).
535:
2468:
2439:
2407:
2237:
2042:
1998:
1949:
1880:
1496:
1258:
1253:
1163:
1081:
87:
2349:
2155:
1632:
1393:
1368:
1303:
1192:
1076:
102:
2480:
2324:
2057:
1944:
1740:
1532:
1011:
980:
799:
48:
There are mistakes in this article; efficacy and intrinsic activity are different properties.
433:. This model was arguably flawed in that it did not incorporate the equilibrium between the
2485:
2329:
2182:
2135:
1775:
1637:
1547:
1388:
1268:
1036:
400:
is the stimulus to the biological system. The response is generated by an unknown function
403:
327:
8:
2106:
1894:
1685:
1573:
1542:
1188:
1148:
1071:
449:
430:
94:, which is a measure of the ability of the drug to bind to its molecular target, and the
2333:
2302:
2033:
1929:
1655:
1605:
1506:
1319:
1198:
1119:
1031:
958:
772:
747:
723:
698:
645:
636:
620:
383:
359:
90:
complex to produce a maximum functional response. This must be distinguished from the
2402:
2307:
2130:
1923:
1650:
1511:
1501:
1329:
1323:
1158:
948:
905:
870:
805:
777:
728:
650:
962:
2392:
2186:
2101:
1855:
1695:
1583:
1578:
1378:
1348:
1134:
1114:
1096:
938:
895:
767:
759:
718:
710:
640:
632:
2320:
2232:
2070:
2065:
1935:
1899:
1889:
1872:
1735:
1610:
1438:
1398:
1383:
1091:
1041:
226:
178:
1293:
2012:
1867:
1850:
1725:
1705:
1624:
1466:
1208:
1153:
714:
943:
926:
2506:
2248:
2147:
2139:
2122:
2061:
1730:
1217:
1124:
867:
The
Pharmacology of Functional, Biochemical, and Recombinant Receptor Systems
452:
later improved on
Stephenson's model with the definition of efficacy, e, as
2227:
2093:
2076:
1831:
1700:
1660:
1561:
1485:
1363:
1046:
1003:
781:
763:
732:
654:
155:
132:
900:
2384:
2357:
2290:
1983:
1863:
1785:
1272:
1248:
522:{\displaystyle S=\underbrace {\varepsilon _{\mathrm {Tot} }} _{e}\cdot p}
2210:
2025:
1665:
1597:
1489:
1264:
2219:
2169:
1800:
1443:
441:
agonist-bound-receptor that is shown in the del
Castillo Katz model.
21:
2260:
1565:
1537:
1524:
1213:
661:
260:
1884:
1026:
106:
2397:
1966:
1846:
972:
846:
745:
1418:
1311:
1307:
1109:
376:
is the proportion of agonist-bound receptors (given by the
83:
1484:
1758:
1560:
696:
1718:
1180:
842:
669:"In vitro pharmacology: concentration-response curves"
562:
538:
461:
406:
386:
362:
330:
280:
271:
Intrinsic activity of a test agonist is defined as:
1142:
797:
697:Chojnacka K, Papke RL, Horenstein NA (July 2013).
591:
544:
521:
421:
392:
368:
345:
304:
2504:
890:Bindslev N (2008). "Chapter 1: Simple Agonism".
625:British Journal of Pharmacology and Chemotherapy
832:. British Pharmacological Society. 2 June 2016.
44:needs attention from an expert in pharmacology
1816:
1623:
988:
703:Bioorganic & Medicinal Chemistry Letters
137:Efficacy higher than the endogenous agonist
739:
690:
612:
1823:
1809:
995:
981:
843:Brunton L, Chabner BA, Knollman B (2011).
618:
183:Efficacy less than the endogenous agonist
2024:
1596:
1064:
1019:
942:
899:
864:
860:
858:
856:
793:
791:
771:
722:
644:
599:is the total concentration of receptors.
160:Efficacy equal to the endogenous agonist
889:
798:Foreman JC, Johansen T, Gibb AJ (2009).
113:
20:
1523:
1231:
931:Microbial Ecology in Health and Disease
924:
444:
315:
2505:
1830:
1356:
1286:
853:
788:
54:may be able to help recruit an expert.
25:Efficacy spectrum of receptor ligands.
16:Measure of relative response to a drug
1804:
976:
894:. London: CRC Press. pp. 19ā20.
266:
1411:
295:maximal response to the test agonist
28:
621:"A modification of receptor theory"
82:refer to the relative ability of a
13:
2430:Angiotensin II receptor antagonist
2374:Endocannabinoid reuptake inhibitor
1781:Minimum bactericidal concentration
637:10.1111/j.1476-5381.1956.tb00006.x
583:
580:
577:
495:
492:
489:
285:
282:
14:
2524:
2321:Acetylcholine receptor antagonist
2083:Norepinephrine reuptake inhibitor
869:. Berlin: Springer. p. 120.
801:Textbook of Receptor Pharmacology
673:Glaxo Wellcome pharmacology guide
592:{\displaystyle _{\mathrm {Tot} }}
1771:Minimum inhibitory concentration
1002:
298:maximal response to full agonist
33:
2449:Vasopressin receptor antagonist
2363:Cannabinoid receptor antagonist
1711:WHO list of essential medicines
1204:Non-specific effect of vaccines
918:
619:Stephenson RP (December 1956).
437:agonist-bound-receptor and the
2435:Endothelin receptor antagonist
2299:Acetylcholine receptor agonist
2058:Adrenergic receptor antagonist
1766:Antimicrobial pharmacodynamics
883:
836:
818:
804:(Second ed.). CRC Press.
572:
563:
484:
475:
416:
410:
1:
2267:Glutamate receptor antagonist
2183:Serotonin receptor antagonist
2136:Histamine receptor antagonist
1911:Negative allosteric modulator
1905:Positive allosteric modulator
1691:Functional analog (chemistry)
937:(4). London: Routledge: 213.
605:
2424:Adenosine reuptake inhibitor
2358:Cannabinoid receptor agonist
2277:Glutamate reuptake inhibitor
2196:Serotonin reuptake inhibitor
2107:Dopamine receptor antagonist
1244:Hill equation (biochemistry)
849:(12th ed.). p. 46.
545:{\displaystyle \varepsilon }
101:, which is a measure of the
7:
2112:Dopamine reuptake inhibitor
2034:Adrenergic receptor agonist
117:
46:. The specific problem is:
10:
2529:
2403:Opioid receptor antagonist
2257:Glutamate receptor agonist
2178:Serotonin receptor agonist
2131:Histamine receptor agonist
1759:Antimicrobial pharmacology
1239:Doseāresponse relationship
1169:Desensitization (medicine)
826:"R P ('Steve') Stephenson"
715:10.1016/j.bmcl.2013.05.039
2461:
2416:
2383:
2348:
2289:
2247:
2218:
2209:
2168:
2121:
2102:Dopamine receptor agonist
2092:
2011:
1997:
1982:
1965:
1958:
1838:
1681:Coinduction (anesthetics)
1674:
1475:
1347:
1133:
1010:
944:10.1080/08910600802431931
830:Pharmacology Hall of Fame
429:, which is assumed to be
208:Affinity but no efficacy
126:
2368:Endocannabinoid enhancer
2314:Cholinesterase inhibitor
2233:GABA receptor antagonist
1746:Multiple drug resistance
1719:Tolerance and resistance
1087:Physiological antagonist
52:WikiProject Pharmacology
2408:Enkephalinase inhibitor
2398:Opioid receptor agonist
2238:GABA reuptake inhibitor
1943:♦ Miscellaneous:
1497:Neuropsychopharmacology
1259:Cheng-Prussoff Equation
1254:Del Castillo Katz model
1181:Other effects of ligand
1164:Receptor (biochemistry)
1082:Irreversible antagonist
1991:Ion channel modulators
1633:Classical pharmacology
1394:Plasma protein binding
1369:Volume of distribution
1077:Competitive antagonist
764:10.1002/cmdc.201700162
593:
546:
523:
423:
394:
370:
347:
306:
26:
2228:GABA receptor agonist
1741:Antibiotic resistance
1533:Clinical pharmacology
1052:Physiological agonist
1012:Ligand (biochemistry)
901:10.4324/9781315159782
594:
547:
524:
424:
395:
371:
348:
307:
114:Mechanism of efficacy
24:
1638:Reverse pharmacology
1548:Pharmacoepidemiology
1389:Biological half-life
1269:Ligand binding assay
1143:Activity at receptor
1037:Irreversible agonist
560:
536:
459:
445:Furchgott's efficacy
422:{\displaystyle f(S)}
404:
384:
360:
346:{\displaystyle S=ep}
328:
316:Stevenson's efficacy
278:
2444:receptor antagonist
1686:Combination therapy
1574:Pharmacoinformatics
1543:Medicinal chemistry
1149:Mechanism of action
450:Robert F. Furchgott
1832:Pharmacomodulation
1656:Immunopharmacology
1606:Pharmacotoxicology
1507:Psychopharmacology
1299:Intrinsic activity
1199:Pleiotropy (drugs)
1120:Agonist-antagonist
1032:Endogenous agonist
925:Kirkeby H (2017).
589:
554:intrinsic efficacy
542:
519:
512:
505:
419:
390:
366:
343:
302:
267:Intrinsic activity
72:Intrinsic activity
27:
2500:
2499:
2496:
2495:
2457:
2456:
2285:
2284:
2205:
2204:
1975:Enzyme inhibition
1798:
1797:
1794:
1793:
1754:
1753:
1651:Photopharmacology
1646:
1645:
1619:
1618:
1592:
1591:
1556:
1555:
1519:
1518:
1512:Electrophysiology
1502:Neuropharmacology
1457:
1456:
1407:
1406:
1343:
1342:
1330:Therapeutic index
1282:
1281:
1227:
1226:
1176:
1175:
1105:
1104:
1060:
1059:
954:978-1-351-66057-0
911:978-91-977071-0-7
876:978-3-540-66124-5
758:(16): 1335ā1348.
709:(14): 4145ā4149.
569:
481:
470:
468:
393:{\displaystyle S}
369:{\displaystyle p}
300:
299:
296:
248:
247:
231:Inverse efficacy
204:Silent antagonist
69:
68:
2520:
2513:Pharmacodynamics
2474:Enzyme cofactors
2393:Opioid modulator
2350:Cannabinoidergic
2216:
2215:
2022:
2021:
2009:
2008:
1963:
1962:
1825:
1818:
1811:
1802:
1801:
1756:
1755:
1716:
1715:
1696:Polypharmacology
1621:
1620:
1594:
1593:
1584:Pharmacogenomics
1579:Pharmacogenetics
1558:
1557:
1521:
1520:
1482:
1481:
1409:
1408:
1379:Rate of infusion
1354:
1353:
1349:Pharmacokinetics
1284:
1283:
1229:
1228:
1178:
1177:
1140:
1139:
1135:Pharmacodynamics
1115:Neurotransmitter
1097:Enzyme inhibitor
1062:
1061:
1017:
1016:
997:
990:
983:
974:
973:
967:
966:
946:
922:
916:
915:
903:
887:
881:
880:
862:
851:
850:
840:
834:
833:
822:
816:
815:
795:
786:
785:
775:
743:
737:
736:
726:
694:
688:
687:
685:
684:
675:. Archived from
665:
659:
658:
648:
616:
598:
596:
595:
590:
588:
587:
586:
570:
567:
551:
549:
548:
543:
528:
526:
525:
520:
511:
506:
501:
500:
499:
498:
482:
479:
428:
426:
425:
420:
399:
397:
396:
391:
375:
373:
372:
367:
352:
350:
349:
344:
311:
309:
308:
303:
301:
297:
294:
293:
288:
118:
64:
61:
55:
37:
36:
29:
2528:
2527:
2523:
2522:
2521:
2519:
2518:
2517:
2503:
2502:
2501:
2492:
2453:
2443:
2412:
2379:
2344:
2281:
2243:
2201:
2190:
2164:
2159:
2151:
2143:
2117:
2088:
2002:
1993:
1978:
1954:
1900:Inverse agonist
1890:Partial agonist
1834:
1829:
1799:
1790:
1750:
1736:Drug resistance
1714:
1670:
1642:
1615:
1611:Neurotoxicology
1588:
1552:
1515:
1477:
1471:
1453:
1403:
1399:Bioavailability
1384:Onset of action
1339:
1278:
1223:
1172:
1129:
1101:
1092:Inverse agonist
1056:
1042:Partial agonist
1006:
1001:
971:
970:
955:
923:
919:
912:
888:
884:
877:
863:
854:
841:
837:
824:
823:
819:
812:
796:
789:
744:
740:
695:
691:
682:
680:
667:
666:
662:
617:
613:
608:
576:
575:
571:
566:
561:
558:
557:
537:
534:
533:
507:
488:
487:
483:
478:
471:
469:
460:
457:
456:
447:
405:
402:
401:
385:
382:
381:
361:
358:
357:
329:
326:
325:
318:
292:
281:
279:
276:
275:
269:
227:Inverse agonist
179:Partial agonist
127:% Efficacy (E)
116:
99:
65:
59:
56:
50:
38:
34:
17:
12:
11:
5:
2526:
2516:
2515:
2498:
2497:
2494:
2493:
2491:
2490:
2478:
2465:
2463:
2459:
2458:
2455:
2454:
2452:
2451:
2446:
2441:
2437:
2432:
2427:
2420:
2418:
2414:
2413:
2411:
2410:
2405:
2400:
2395:
2389:
2387:
2381:
2380:
2378:
2377:
2371:
2365:
2360:
2354:
2352:
2346:
2345:
2343:
2342:
2336:
2327:
2318:
2317:
2316:
2305:
2295:
2293:
2287:
2286:
2283:
2282:
2280:
2279:
2274:
2264:
2253:
2251:
2245:
2244:
2242:
2241:
2235:
2230:
2224:
2222:
2213:
2207:
2206:
2203:
2202:
2200:
2199:
2193:
2188:
2180:
2174:
2172:
2166:
2165:
2163:
2162:
2157:
2153:
2149:
2145:
2141:
2133:
2127:
2125:
2119:
2118:
2116:
2115:
2109:
2104:
2098:
2096:
2090:
2089:
2087:
2086:
2080:
2074:
2068:
2055:
2049:
2040:
2030:
2028:
2019:
2006:
1995:
1994:
1988:
1986:
1980:
1979:
1971:
1969:
1960:
1956:
1955:
1953:
1952:
1947:
1940:
1939:
1933:
1927:
1915:
1914:
1908:
1902:
1897:
1892:
1887:
1876:
1875:
1870:
1859:
1858:
1853:
1842:
1840:
1836:
1835:
1828:
1827:
1820:
1813:
1805:
1796:
1795:
1792:
1791:
1789:
1788:
1783:
1778:
1776:Bacteriostatic
1773:
1768:
1762:
1760:
1752:
1751:
1749:
1748:
1743:
1738:
1733:
1728:
1726:Drug tolerance
1722:
1720:
1713:
1708:
1706:Lists of drugs
1703:
1698:
1693:
1688:
1683:
1678:
1676:
1672:
1671:
1669:
1668:
1663:
1658:
1653:
1647:
1644:
1643:
1641:
1640:
1635:
1629:
1627:
1625:Drug discovery
1617:
1616:
1614:
1613:
1608:
1602:
1600:
1590:
1589:
1587:
1586:
1581:
1576:
1570:
1568:
1554:
1553:
1551:
1550:
1545:
1540:
1535:
1529:
1527:
1517:
1516:
1514:
1509:
1504:
1499:
1494:
1492:
1479:
1473:
1472:
1470:
1469:
1467:Bioequivalence
1464:
1458:
1455:
1454:
1452:
1451:
1441:
1436:
1431:
1426:
1415:
1413:
1405:
1404:
1402:
1401:
1396:
1391:
1386:
1381:
1376:
1366:
1360:
1358:
1351:
1345:
1344:
1341:
1340:
1338:
1337:
1332:
1327:
1301:
1296:
1290:
1288:
1280:
1279:
1277:
1276:
1261:
1256:
1251:
1246:
1241:
1235:
1233:
1225:
1224:
1222:
1221:
1211:
1209:Adverse effect
1206:
1201:
1196:
1184:
1182:
1174:
1173:
1171:
1166:
1161:
1156:
1154:Mode of action
1151:
1146:
1144:
1137:
1131:
1130:
1128:
1127:
1122:
1117:
1112:
1106:
1103:
1102:
1100:
1099:
1094:
1089:
1084:
1079:
1074:
1068:
1066:
1058:
1057:
1055:
1054:
1049:
1044:
1039:
1034:
1029:
1023:
1021:
1014:
1008:
1007:
1000:
999:
992:
985:
977:
969:
968:
953:
917:
910:
882:
875:
852:
835:
817:
810:
787:
738:
689:
660:
631:(4): 379ā393.
610:
609:
607:
604:
585:
582:
579:
574:
565:
541:
530:
529:
518:
515:
510:
504:
497:
494:
491:
486:
477:
474:
467:
464:
446:
443:
418:
415:
412:
409:
389:
365:
354:
353:
342:
339:
336:
333:
317:
314:
313:
312:
291:
287:
284:
268:
265:
246:
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115:
112:
97:
67:
66:
41:
39:
32:
15:
9:
6:
4:
3:
2:
2525:
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2510:
2508:
2488:
2487:
2482:
2479:
2476:
2475:
2470:
2467:
2466:
2464:
2462:Miscellaneous
2460:
2450:
2447:
2445:
2438:
2436:
2433:
2431:
2428:
2425:
2422:
2421:
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2328:
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2319:
2315:
2312:
2311:
2309:
2306:
2304:
2300:
2297:
2296:
2294:
2292:
2288:
2278:
2275:
2272:
2268:
2265:
2262:
2258:
2255:
2254:
2252:
2250:
2249:Glutamatergic
2246:
2239:
2236:
2234:
2231:
2229:
2226:
2225:
2223:
2221:
2217:
2214:
2212:
2208:
2197:
2194:
2191:
2184:
2181:
2179:
2176:
2175:
2173:
2171:
2167:
2160:
2154:
2152:
2146:
2144:
2137:
2134:
2132:
2129:
2128:
2126:
2124:
2123:Histaminergic
2120:
2113:
2110:
2108:
2105:
2103:
2100:
2099:
2097:
2095:
2091:
2084:
2081:
2078:
2075:
2072:
2069:
2067:
2063:
2059:
2056:
2053:
2050:
2048:
2044:
2041:
2039:
2035:
2032:
2031:
2029:
2027:
2023:
2020:
2018:
2014:
2010:
2007:
2005:
2000:
1996:
1992:
1987:
1985:
1981:
1977:
1976:
1970:
1968:
1964:
1961:
1957:
1951:
1948:
1946:
1942:
1941:
1937:
1934:
1931:
1928:
1925:
1921:
1917:
1916:
1912:
1909:
1906:
1903:
1901:
1898:
1896:
1893:
1891:
1888:
1886:
1882:
1878:
1877:
1874:
1871:
1869:
1865:
1861:
1860:
1857:
1854:
1852:
1848:
1844:
1843:
1841:
1837:
1833:
1826:
1821:
1819:
1814:
1812:
1807:
1806:
1803:
1787:
1784:
1782:
1779:
1777:
1774:
1772:
1769:
1767:
1764:
1763:
1761:
1757:
1747:
1744:
1742:
1739:
1737:
1734:
1732:
1731:Tachyphylaxis
1729:
1727:
1724:
1723:
1721:
1717:
1712:
1709:
1707:
1704:
1702:
1699:
1697:
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1689:
1687:
1684:
1682:
1679:
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1601:
1599:
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1580:
1577:
1575:
1572:
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1567:
1563:
1559:
1549:
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1539:
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1534:
1531:
1530:
1528:
1526:
1522:
1513:
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1500:
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1487:
1483:
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1459:
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1427:
1424:
1420:
1417:
1416:
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1390:
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1382:
1380:
1377:
1374:
1370:
1367:
1365:
1362:
1361:
1359:
1355:
1352:
1350:
1346:
1336:
1333:
1331:
1328:
1325:
1321:
1317:
1313:
1309:
1305:
1302:
1300:
1297:
1295:
1292:
1291:
1289:
1285:
1274:
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1266:
1262:
1260:
1257:
1255:
1252:
1250:
1247:
1245:
1242:
1240:
1237:
1236:
1234:
1230:
1219:
1218:Neurotoxicity
1215:
1212:
1210:
1207:
1205:
1202:
1200:
1197:
1194:
1190:
1187:Selectivity (
1186:
1185:
1183:
1179:
1170:
1167:
1165:
1162:
1160:
1157:
1155:
1152:
1150:
1147:
1145:
1141:
1138:
1136:
1132:
1126:
1125:Pharmacophore
1123:
1121:
1118:
1116:
1113:
1111:
1108:
1107:
1098:
1095:
1093:
1090:
1088:
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1005:
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813:
811:9781439887578
807:
803:
802:
794:
792:
783:
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769:
765:
761:
757:
753:
749:
742:
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730:
725:
720:
716:
712:
708:
704:
700:
693:
679:on 2019-07-26
678:
674:
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664:
656:
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634:
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626:
622:
615:
611:
603:
600:
555:
539:
516:
513:
508:
502:
472:
465:
462:
455:
454:
453:
451:
442:
440:
436:
432:
413:
407:
387:
379:
378:Hill equation
363:
340:
337:
334:
331:
324:
323:
322:
289:
274:
273:
272:
264:
262:
258:
254:
244:
242:
239:
236:
233:
230:
228:
225:
224:
221:
219:
216:
213:
210:
207:
205:
202:
201:
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194:
191:
188:
185:
182:
180:
177:
176:
173:
171:
168:
165:
162:
159:
157:
154:
153:
150:
148:
145:
142:
139:
136:
134:
131:
130:
123:
120:
119:
111:
108:
104:
100:
93:
89:
85:
81:
77:
73:
63:
53:
49:
45:
42:This article
40:
31:
30:
23:
19:
2484:
2472:
2170:Serotonergic
2094:Dopaminergic
1973:
1701:Chemotherapy
1661:Cell biology
1562:Biochemistry
1486:Neuroscience
1434:Distribution
1364:Loading dose
1298:
1047:Superagonist
1004:Pharmacology
934:
930:
920:
891:
885:
866:
845:
838:
829:
820:
800:
755:
751:
741:
706:
702:
692:
681:. Retrieved
677:the original
672:
663:
628:
624:
614:
601:
553:
531:
448:
438:
434:
355:
319:
270:
252:
249:
156:Full agonist
133:Superagonist
124:Description
79:
75:
71:
70:
57:
47:
43:
18:
2486:Amino acids
2385:Opioidergic
2291:Cholinergic
2004:transporter
1984:Ion channel
1920:Transporter
1864:Ion channel
1786:Bactericide
1462:Compartment
1273:Patch clamp
1249:Schild plot
752:ChemMedChem
435:inactivated
2334:Ganglionic
2325:Muscarinic
2303:Muscarinic
2026:Adrenergic
1895:Antagonist
1666:Physiology
1598:Toxicology
1490:psychology
1439:Metabolism
1429:Absorption
1423:Liberation
1265:Organ bath
1193:Functional
1072:Antagonist
1065:Inhibitory
1020:Excitatory
683:2009-07-11
606:References
431:hyperbolic
110:activity.
60:April 2019
2481:Precursor
2330:Nicotinic
2308:Nicotinic
2220:GABAergic
1945:Precursor
1930:Inhibitor
1856:Inhibitor
1448:Clearance
1444:Excretion
1263:Methods (
540:ε
514:⋅
503:⏟
473:ε
439:activated
2507:Category
2469:Cofactor
2339:Muscular
1999:Receptor
1950:Cofactor
1936:Releaser
1924:Enhancer
1918:♦
1881:Receptor
1879:♦
1862:♦
1845:♦
1566:genetics
1538:Pharmacy
1525:Medicine
1335:Affinity
1294:Efficacy
1232:Analysis
1214:Toxicity
963:83584731
782:28494140
733:23746476
655:13383117
261:naloxone
107:agonists
92:affinity
88:receptor
80:efficacy
2426:(AdoRI)
2376:(eCBRI)
1959:Classes
1885:Agonist
1873:Blocker
1851:Inducer
1476:Related
1419:(L)ADME
1373:Initial
1357:Metrics
1304:Potency
1287:Metrics
1189:Binding
1159:Binding
1027:Agonist
773:5573630
724:3882203
646:1510558
552:is the
121:Ligand
103:potency
2370:(eCBE)
1967:Enzyme
1868:Opener
1847:Enzyme
1478:fields
961:
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873:
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780:
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532:where
380:) and
356:where
78:) and
2483:(see
2471:(see
2417:Other
2240:(GRI)
2198:(SRI)
2114:(DRI)
2085:(NRI)
2001:&
1913:(NAM)
1907:(PAM)
1839:Types
1675:Other
1412:LADME
959:S2CID
237:<
195:<
189:<
143:>
2271:NMDA
2261:AMPA
2187:5-HT
1989:See
1972:see
1938:(RA)
1932:(RI)
1926:(RE)
1564:and
1488:and
1324:TD50
1320:LD50
1316:ED50
1312:IC50
1308:EC50
1110:Drug
949:ISBN
906:ISBN
871:ISBN
806:ISBN
778:PMID
729:PMID
651:PMID
556:and
253:true
198:100
169:100
146:100
84:drug
1421:: (
939:doi
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768:PMC
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711:doi
641:PMC
633:doi
257:DOI
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2440:NK
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2211:AA
2054:))
2013:BA
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Text is available under the Creative Commons Attribution-ShareAlike License. Additional terms may apply.
