Knowledge (XXG)

Seltorexant

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Muehlan C, Vaillant C, Zenklusen I, Kraehenbuehl S, Dingemanse J (November 2020). "Clinical pharmacology, efficacy, and safety of orexin receptor antagonists for the treatment of insomnia disorders".
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InChI=1S/C21H22FN7O/c1-13-8-14(2)26-21(25-13)28-11-15-9-27(10-16(15)12-28)20(30)19-17(22)4-3-5-18(19)29-23-6-7-24-29/h3-8,15-16H,9-12H2,1-2H3/t15-,16+
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Jacobson LH, Hoyer D, de Lecea L (January 2022). "Hypocretins (orexins): The ultimate translational neuropeptides".
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mg. In the early clinical trials conducted so far, seltorexant has been found to improve depression scores on the
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related to other clinically used orexin receptor antagonists. Seltorexant shows over 100-fold greater
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trials for treatment of insomnia. It was also under investigation for the treatment of
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Christopher JA (2014). "Small-molecule antagonists of the orexin receptors".
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List of investigational antidepressants § Orexin receptor antagonists
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in people with MDD and/or insomnia. Seltorexant is reported to be
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List of investigational sleep drugs § Orexin receptor antagonists
674:– another investigational short-acting orexin receptor antagonist 1575: 1228: 638:
of seltorexant observed in clinical trials so far have included
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hours. No residual effects of the medication were observed 4
709:"Hypocretin/Orexin Receptor Pharmacology and Sleep Phases" 172:
pyrrol-2-yl]-(2-fluoro-6-triazol-2-ylphenyl)methanone
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c4c(C)nc(nc4C)N5CC2CN(CC2C5)C(=O)c1c(cccc1F)-n3nccn3
1949: 1796: 1486: 1458: 1420: 1286: 1001: 336: 323: 290: 285: 265: 245: 225: 200: 180: 155: 142: 130: 122: 97: 92: 76: 64: 50: 42: 37: 602:Seltorexant is being explored at doses of 5 to 80 423:which is under development for the treatment of 214: 788: 786: 784: 189: 872: 870: 868: 866: 864: 862: 860: 782: 780: 778: 776: 774: 772: 770: 768: 766: 764: 702: 700: 698: 498:of seltorexant are considered to be ideal for 1771: 979: 838: 836: 834: 832: 408:, also known by its developmental code names 8: 1535: 21: 1644: 1632: 715:. Frontiers of Neurology and Neuroscience. 1778: 1764: 1756: 986: 972: 964: 234: 744: 724: 254: 494:hours after daytime administration. The 694: 572:As of February 2022, seltorexant is in 387: 367: 169: 707:Sun Y, Tisdale RK, Kilduff TS (2021). 20: 7: 274: 205: 610:in people with MDD and to improve 449:(2-SORA). The medication is taken 14: 478:hours and has a relatively short 608:Hamilton Depression Rating Scale 562:dual orexin receptor antagonists 311: 308: 302: 29: 395:Key:SQOCEMCKYDVLMM-IYBDPMFKSA-N 16:Experimental anti-insomnia drug 2130:Drugs not assigned an ATC code 2109:Vornorexant (ORN-0829, TS-142) 1941:Vornorexant (ORN-0829, TS-142) 1936:Tebideutorexant (JNJ-61393215) 795:Expert Opin Drug Metab Toxicol 317: 296: 46:MIN-202; JNJ-42847922; JNJ-922 1: 922:Pharmaceutical Patent Analyst 807:10.1080/17425255.2020.1817380 2140:Experimental antidepressants 620:time awake after sleep onset 1698:Tetracyclic antidepressants 1637:Tooltip 5-hydroxytryptophan 1460:Melatonin receptor agonists 1422:Orexin receptor antagonists 1402:Tetracyclic antidepressants 2186: 286:Chemical and physical data 1906:Nivasorexant (ACT-539313) 1716: 1680:Tricyclic antidepressants 1384:Tricyclic antidepressants 959:Seltorexant — AdisInsight 846:. AdisInsight. 2022-02-28 581:major depressive disorder 378: 358: 160: 28: 114:Investigational New Drug 2049:Fazamorexant (YZJ-1139) 2014:Suntinorexton (TAK-861) 1886:Fazamorexant (YZJ-1139) 597:Janssen Pharmaceuticals 2059:GSK-649868 (SB-649868) 1985:Firazorexton (TAK-994) 1975:Danavorexton (TAK-925) 1896:GSK-649868 (SB-649868) 713:Front Neurol Neurosci 593:Johnson & Johnson 484:elimination half-life 466:Seltorexant has fast 1866:C4X-3256 (INDV-2000) 1624:Serotonin precursors 995:Insomnia medications 656:abdominal discomfort 474:levels of 0.3 to 1.5 1586:Menthyl isovalerate 1009:positive modulators 520:Mechanism of action 25: 2160:Orexin antagonists 1743:Never to phase III 1121:Nonbenzodiazepines 891:10.1111/joim.13406 540:receptor over the 2117: 2116: 1753: 1752: 1199:potassium bromide 934:10.4155/ppa.14.46 801:(11): 1063–1078. 736:978-3-318-06843-6 726:10.1159/000514963 579:for treatment of 502:. Seltorexant is 418:orexin antagonist 403: 402: 349:Interactive image 111: 71:Orexin antagonist 2177: 2135:Aminopyrimidines 1780: 1773: 1766: 1757: 1646: 1643:Sodium oxybate ( 1638: 1634: 1537: 1359:Phenyltoloxamine 1300:inverse agonists 1253:Piperidinediones 988: 981: 974: 965: 946: 945: 917: 911: 910: 874: 855: 854: 852: 851: 840: 827: 826: 790: 759: 758: 748: 728: 704: 624:sleep efficiency 616:total sleep time 605: 560:, which are all 534:binding affinity 528:compound and is 496:pharmacokinetics 493: 489: 477: 462:Pharmacokinetics 351: 331: 319: 313: 310: 304: 298: 278: 258: 238: 218: 208: 207: 193: 147: 109: 106: 33: 26: 24: 2185: 2184: 2180: 2179: 2178: 2176: 2175: 2174: 2120: 2119: 2118: 2113: 1954: 1945: 1801: 1792: 1787:Orexin receptor 1784: 1754: 1749: 1748: 1733:Clinical trials 1712: 1636: 1482: 1454: 1416: 1324:Diphenhydramine 1298: 1295: 1282: 1219:Chloral hydrate 1163:amylene hydrate 1018:Benzodiazepines 1008: 1006: 997: 992: 955: 950: 949: 919: 918: 914: 876: 875: 858: 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1016: 925: 921: 915: 882: 879:J Intern Med 878: 848:. Retrieved 798: 794: 716: 712: 636:Side effects 601: 571: 558:daridorexant 530:structurally 523: 472:time to peak 465: 457:Pharmacology 414:JNJ-42847922 413: 409: 405: 404: 191:1293281-49-8 144:Elimination 99:Legal status 93:Legal status 18: 2089:Seltorexant 2069:Lemborexant 2004:Oveporexton 1901:Lemborexant 1729:from market 1702:mirtazapine 1619:Scopolamine 1600:hydrocodone 1553:Fenadiazole 1516:Ashwagandha 1506:risperidone 1478:Tasimelteon 1450:Vornorexant 1440:Seltorexant 1435:Lemborexant 1406:mirtazapine 1364:Pimethixene 1354:Pheniramine 1339:Hydroxyzine 1309:Alimemazine 1248:Paraldehyde 1213:meprobamate 1177:amobarbital 1130:Eszopiclone 1093:Nimetazepam 1073:Haloxazolam 1043:Doxefazepam 1038:Clorazepate 1028:Cinolazepam 672:Vornorexant 612:sleep onset 589:sleep apnea 554:lemborexant 504:metabolized 406:Seltorexant 332: g·mol 156:Identifiers 43:Other names 23:Seltorexant 2124:Categories 2104:TCS-OX2-29 2094:Suvorexant 2054:Filorexant 2034:Almorexant 2029:ACT-462206 2024:ACT-335827 1926:Suvorexant 1891:Filorexant 1856:Almorexant 1851:ACT-462206 1846:ACT-335827 1790:modulators 1660:guanfacine 1628:tryptophan 1591:Niaprazine 1566:pregabalin 1562:gabapentin 1502:olanzapine 1498:quetiapine 1445:Suvorexant 1379:Pyrilamine 1329:Doxylamine 1314:Captodiame 1242:zuranolone 1209:Carbamates 1098:Nitrazepam 1078:Loprazolam 1063:Flurazepam 1033:Climazolam 1023:Brotizolam 850:2022-04-05 689:References 660:nightmares 640:somnolence 583:(MDD) and 564:(DORAs). 550:suvorexant 536:for the OX 468:absorption 436:antagonist 431:. It is a 425:depression 421:medication 337:3D model ( 325:Molar mass 256:AIS8N3O50B 227:ChemSpider 182:CAS Number 165:IUPAC name 132:Metabolism 66:Drug class 2170:Triazoles 2150:Hypnotics 2009:SB-668875 1970:ALKS-2680 1962:Agonists: 1921:SB-408124 1916:SB-334867 1911:RTIOX-276 1809:Agonists: 1739:Phase III 1727:Withdrawn 1675:Trazodone 1656:clonidine 1604:oxycodone 1548:Chamomile 1473:Ramelteon 1468:Melatonin 1344:Meclizine 1145:Zopiclone 1113:Triazolam 1108:Temazepam 1088:Midazolam 1048:Estazolam 907:248119793 823:221572078 719:: 22–37. 648:dizziness 433:selective 151:2–3 hours 146:half-life 52:Routes of 2165:Pyrroles 2099:TCS-1102 1931:TCS-1102 1861:AZD-4041 1670:Theanine 1664:prazosin 1608:morphine 1581:Lavender 1570:phenibut 1542:nabilone 1530:cannabis 1296:receptor 1278:Valerian 1195:Bromides 1155:Alcohols 1140:Zolpidem 1135:Zaleplon 1103:Quazepam 1053:Etizolam 1007:receptor 942:25489915 899:35043499 815:32901578 755:34052813 666:See also 652:headache 546:receptor 524:It is a 482:with an 480:duration 451:by mouth 447:receptor 429:insomnia 416:, is an 236:34989176 216:67116280 78:ATC code 59:By mouth 2155:Ketones 2084:MK-8133 2079:MK-3697 2074:MK-1064 1876:CVN-766 1871:CR-5542 1700:(e.g., 1688:doxepin 1682:(e.g., 1654:(e.g., 1598:(e.g., 1596:Opioids 1560:(e.g., 1528:(e.g., 1496:(e.g., 1404:(e.g., 1392:doxepin 1386:(e.g., 1265:(e.g., 1255:(e.g., 1236:(e.g., 1211:(e.g., 1197:(e.g., 1175:(e.g., 1167:ethanol 1157:(e.g., 1152:Others: 1125:Z-drugs 746:8171809 644:fatigue 585:phase 2 574:phase 3 506:by the 470:with a 438:of the 410:MIN-202 330:407.453 292:Formula 202:PubChem 1990:Orexin 1980:E-2086 1965:AEX-19 1827:Orexin 1822:AEX-24 1817:AEX-19 1722:WHO-EM 940:  905:  897:  821:  813:  753:  743:  733:  658:, and 622:, and 604:  556:, and 514:CYP3A4 511:enzyme 492:  488:  476:  440:orexin 363:SMILES 276:D11269 137:CYP3A4 112: 1812:AEX-5 1633:5-HTP 903:S2CID 819:S2CID 383:InChI 339:JSmol 2044:EMPA 1576:Hops 1229:Kava 1003:GABA 938:PMID 895:PMID 811:PMID 751:PMID 731:ISBN 630:and 628:safe 427:and 412:and 267:KEGG 247:UNII 126:data 85:None 1645:GHB 1536:THC 930:doi 887:doi 883:291 803:doi 741:PMC 721:doi 595:'s 206:CID 2126:: 1996:, 1951:OX 1833:, 1798:OX 1735:: 1690:, 1686:, 1662:, 1658:, 1630:, 1606:, 1602:, 1568:, 1564:, 1540:, 1532:, 1508:, 1504:, 1500:, 1394:, 1390:, 1240:, 1201:, 1187:, 1183:, 1179:, 1165:, 1161:, 936:. 924:. 901:. 893:. 881:. 859:^ 831:^ 817:. 809:. 799:16 797:. 763:^ 749:. 739:. 729:. 717:45 711:. 697:^ 662:. 654:, 650:, 646:, 642:, 634:. 618:, 614:, 599:. 552:, 542:OX 516:. 453:. 443:OX 306:22 300:21 108:US 2000:) 1998:B 1994:A 1992:( 1953:2 1837:) 1835:B 1831:A 1829:( 1800:1 1779:e 1772:t 1765:v 1704:) 1694:) 1666:) 1647:) 1639:) 1626:( 1610:) 1572:) 1544:) 1538:) 1512:) 1408:) 1398:) 1302:) 1294:1 1292:H 1290:( 1269:) 1259:) 1244:) 1215:) 1205:) 1191:) 1169:) 1127:: 1123:/ 1020:: 1005:A 987:e 980:t 973:v 944:. 932:: 926:3 909:. 889:: 853:. 825:. 805:: 757:. 723:: 544:1 538:2 445:2 341:) 318:O 315:7 312:N 309:F 303:H 297:C 110::

Index


Routes of
administration

By mouth
Drug class
Orexin antagonist
ATC code
Legal status
Investigational New Drug
Pharmacokinetic
Metabolism
CYP3A4
Elimination half-life
IUPAC name
CAS Number
1293281-49-8
PubChem
67116280
ChemSpider
34989176
UNII
AIS8N3O50B
KEGG
D11269
Formula
Molar mass
JSmol
Interactive image
SMILES
InChI
orexin antagonist

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