Chemical compound
Orvepitant ATC code
(2R,4S)-4-[(8aS)-6-oxo-1,3,4,7,8,8a-hexahydropyrrolo[1,2-a]pyrazin-2-yl]-N-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethyl]-2-(4-fluoro-2-methylphenyl)-N-methylpiperidine-1-carboxamide
CAS Number 579475-18-6 Y PubChem CID ChemSpider UNII CompTox Dashboard (EPA ) DTXSID40973522 Formula C 31 H 35 F 7 N 4 O 2 Molar mass 628.636 g·mol−1 3D model (JSmol)
CC1=C(C=CC(=C1)F)[C@H]2C[C@H](CCN2C(=O)N(C)[C@H](C)C3=CC(=CC(=C3)C(F)(F)F)C(F)(F)F)N4CCN5[C@H](C4)CCC5=O
InChI=1S/C31H35F7N4O2/c1-18-12-23(32)4-6-26(18)27-16-24(40-10-11-41-25(17-40)5-7-28(41)43)8-9-42(27)29(44)39(3)19(2)20-13-21(30(33,34)35)15-22(14-20)31(36,37)38/h4,6,12-15,19,24-25,27H,5,7-11,16-17H2,1-3H3/t19-,24+,25+,27-/m1/s1
Key:XWNBGDJPEXZSQM-VZOBGQTKSA-N
Orvepitant (GW823296 ) is a drug developed by GlaxoSmithKline which acts as a selective antagonist for the NK1 receptor.[1] It was under development as a potential antidepressant drug, and early stage human clinical trials showed it to have some antidepressant effects, though not with sufficient efficacy to justify further development for this application. It was however considered a successful proof of concept for NK1 antagonists as potential antidepressants, and efforts are continuing to find more potent compounds which might be more effective.[2]
^ Di Fabio R, Alvaro G, Braggio S, Carletti R, Gerrard PA, Griffante C, et al. (November 2013). "Identification, biological characterization and pharmacophoric analysis of a new potent and selective NK1 receptor antagonist clinical candidate". Bioorganic & Medicinal Chemistry . 21 (21): 6264–73. doi:10.1016/j.bmc.2013.09.001. PMID 24075145.
^ Ratti E, Bettica P, Alexander R, Archer G, Carpenter D, Evoniuk G, et al. (May 2013). "Full central neurokinin-1 receptor blockade is required for efficacy in depression: evidence from orvepitant clinical studies". Journal of Psychopharmacology . 27 (5): 424–34. doi:10.1177/0269881113480990. PMID 23539641. S2CID 6523822.
Last Update: 2022-04-23T10:11:01Z
Orvepitant (GW823296) is a drug developed by GlaxoSmithKline which acts as a selective antagonist for the NK1 receptor. It was under development as a potential...
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Last Update: 2024-03-23T23:38:37Z
Subsequently, other trials with NK1 receptor antagonists, casopitant and orvepitant , have shown promising results. Beyond suggestions that PET receptor occupancy...
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Last Update: 2024-01-04T19:10:30Z
Lanepitant LY-306740 Maropitant Netupitant NKP-608 Nolpitantium besilate Orvepitant Rolapitant RP-67580 SDZ NKT 343 Serlopitant T-2328 Telmapitant Tradipitant...
Word Count : 223
Last Update: 2023-10-06T03:37:05Z
Lanepitant LY-306740 Maropitant Netupitant NKP-608 Nolpitantium besilate Orvepitant Rolapitant RP-67580 SDZ NKT 343 Serlopitant T-2328 Telmapitant Tradipitant...
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Last Update: 2024-05-18T05:34:14Z
receptor blockade is required for efficacy in depression: evidence from orvepitant clinical studies". Journal of Psychopharmacology. 27 (5): 424–434. doi:10...
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Last Update: 2024-03-30T06:32:48Z
Lanepitant LY-306740 Maropitant Netupitant NKP-608 Nolpitantium besilate Orvepitant Rolapitant RP-67580 SDZ NKT 343 Serlopitant T-2328 Telmapitant Tradipitant...
Word Count : 1260
Last Update: 2024-03-17T19:07:38Z
Lanepitant LY-306740 Maropitant Netupitant NKP-608 Nolpitantium besilate Orvepitant Rolapitant RP-67580 SDZ NKT 343 Serlopitant T-2328 Telmapitant Tradipitant...
Word Count : 5337
Last Update: 2023-12-20T19:49:29Z
Lanepitant LY-306740 Maropitant Netupitant NKP-608 Nolpitantium besilate Orvepitant Rolapitant RP-67580 SDZ NKT 343 Serlopitant T-2328 Telmapitant Tradipitant...
Word Count : 248
Last Update: 2023-12-05T03:23:30Z
Lanepitant LY-306740 Maropitant Netupitant NKP-608 Nolpitantium besilate Orvepitant Rolapitant RP-67580 SDZ NKT 343 Serlopitant T-2328 Telmapitant Tradipitant...
Word Count : 3270
Last Update: 2023-12-03T15:12:09Z
Lanepitant LY-306740 Maropitant Netupitant NKP-608 Nolpitantium besilate Orvepitant Rolapitant RP-67580 SDZ NKT 343 Serlopitant T-2328 Telmapitant Tradipitant...
Word Count : 491
Last Update: 2024-04-29T04:15:33Z
Lanepitant LY-306740 Maropitant Netupitant NKP-608 Nolpitantium besilate Orvepitant Rolapitant RP-67580 SDZ NKT 343 Serlopitant T-2328 Telmapitant Tradipitant...
Word Count : 2396
Last Update: 2024-03-14T07:12:16Z
Lanepitant LY-306740 Maropitant Netupitant NKP-608 Nolpitantium besilate Orvepitant Rolapitant RP-67580 SDZ NKT 343 Serlopitant T-2328 Telmapitant Tradipitant...
Word Count : 868
Last Update: 2024-01-30T01:45:55Z
Lanepitant LY-306740 Maropitant Netupitant NKP-608 Nolpitantium besilate Orvepitant Rolapitant RP-67580 SDZ NKT 343 Serlopitant T-2328 Telmapitant Tradipitant...
Word Count : 669
Last Update: 2023-01-29T12:55:18Z
Lanepitant LY-306740 Maropitant Netupitant NKP-608 Nolpitantium besilate Orvepitant Rolapitant RP-67580 SDZ NKT 343 Serlopitant T-2328 Telmapitant Tradipitant...
Word Count : 196
Last Update: 2023-10-01T01:29:59Z
Lanepitant LY-306740 Maropitant Netupitant NKP-608 Nolpitantium besilate Orvepitant Rolapitant RP-67580 SDZ NKT 343 Serlopitant T-2328 Telmapitant Tradipitant...
Word Count : 1716
Last Update: 2022-03-05T22:44:27Z
Lanepitant LY-306740 Maropitant Netupitant NKP-608 Nolpitantium besilate Orvepitant Rolapitant RP-67580 SDZ NKT 343 Serlopitant T-2328 Telmapitant Tradipitant...
Word Count : 145
Last Update: 2022-03-05T22:44:39Z
Lanepitant LY-306740 Maropitant Netupitant NKP-608 Nolpitantium besilate Orvepitant Rolapitant RP-67580 SDZ NKT 343 Serlopitant T-2328 Telmapitant Tradipitant...
Word Count : 177
Last Update: 2023-01-23T11:29:15Z
Lanepitant LY-306740 Maropitant Netupitant NKP-608 Nolpitantium besilate Orvepitant Rolapitant RP-67580 SDZ NKT 343 Serlopitant T-2328 Telmapitant Tradipitant...
Word Count : 273
Last Update: 2024-03-09T23:37:26Z
Lanepitant LY-306740 Maropitant Netupitant NKP-608 Nolpitantium besilate Orvepitant Rolapitant RP-67580 SDZ NKT 343 Serlopitant T-2328 Telmapitant Tradipitant...
Word Count : 955
Last Update: 2023-01-26T02:47:57Z
Lanepitant LY-306740 Maropitant Netupitant NKP-608 Nolpitantium besilate Orvepitant Rolapitant RP-67580 SDZ NKT 343 Serlopitant T-2328 Telmapitant Tradipitant...
Word Count : 983
Last Update: 2023-12-03T22:17:45Z
Lanepitant LY-306740 Maropitant Netupitant NKP-608 Nolpitantium besilate Orvepitant Rolapitant RP-67580 SDZ NKT 343 Serlopitant T-2328 Telmapitant Tradipitant...
Word Count : 116
Last Update: 2024-01-05T23:33:06Z
Lanepitant LY-306740 Maropitant Netupitant NKP-608 Nolpitantium besilate Orvepitant Rolapitant RP-67580 SDZ NKT 343 Serlopitant T-2328 Telmapitant Tradipitant...
Word Count : 236
Last Update: 2022-08-21T16:08:12Z
Lanepitant LY-306740 Maropitant Netupitant NKP-608 Nolpitantium besilate Orvepitant Rolapitant RP-67580 SDZ NKT 343 Serlopitant T-2328 Telmapitant Tradipitant...
Word Count : 240
Last Update: 2023-04-03T09:36:33Z
Lanepitant LY-306740 Maropitant Netupitant NKP-608 Nolpitantium besilate Orvepitant Rolapitant RP-67580 SDZ NKT 343 Serlopitant T-2328 Telmapitant Tradipitant...
Word Count : 186
Last Update: 2024-01-07T22:18:04Z
Lanepitant LY-306740 Maropitant Netupitant NKP-608 Nolpitantium besilate Orvepitant Rolapitant RP-67580 SDZ NKT 343 Serlopitant T-2328 Telmapitant Tradipitant...
Word Count : 294
Last Update: 2022-08-27T08:42:55Z
Lanepitant LY-306740 Maropitant Netupitant NKP-608 Nolpitantium besilate Orvepitant Rolapitant RP-67580 SDZ NKT 343 Serlopitant T-2328 Telmapitant Tradipitant...
Word Count : 148