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579475-24-4

579475-24-4 structure
579475-24-4 structure
  • Name: Orvepitant maleate
  • Chemical Name: (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,(Z)-but-2-enedioic acid
  • CAS Number: 579475-24-4
  • Molecular Formula: C35H39F7N4O6
  • Molecular Weight: 744.69600
  • Catalog: Signaling Pathways GPCR/G Protein Neurokinin Receptor
  • Create Date: 2017-07-02 20:52:21
  • Modify Date: 2024-01-10 08:47:16
  • Orvepitant maleate (GW823296 maleate) is potent, selective, orally active and well-tolerated neurokinin-1 receptor (NK-1) antagonist with a pKi of 10.2 for human neurokinin-1 receptor. Orvepitant maleate can across the blood-brain barrier. Orvepitant maleate has the potential for depressive disorder and chronic refractory cough (CRC) treatment[1][2].
Name (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,(Z)-but-2-enedioic acid
Synonyms (2R,4S)-N-{(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethyl}-2-(4-fluoro-2-methylphenyl)-N-methyl-4-[(8aS)-6-oxohexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl]-1-piperidinecarboxamide maleate
Orvepitant maleate (USAN)
ORVEPITANT MALEATE
UNII-HAX0H28B6W
Description Orvepitant maleate (GW823296 maleate) is potent, selective, orally active and well-tolerated neurokinin-1 receptor (NK-1) antagonist with a pKi of 10.2 for human neurokinin-1 receptor. Orvepitant maleate can across the blood-brain barrier. Orvepitant maleate has the potential for depressive disorder and chronic refractory cough (CRC) treatment[1][2].
Related Catalog
Target

NK1:10.2 (pKi)

In Vitro Orvepitant (Compound 3a) is further characterized in terms of the ability to functionally inhibit substance P (SP)-induced release of cytosolic Ca2+ in human neurokinin-1 receptor (hNK1)-CHO cells. Orvepitant (0.3-10 nM), pre-incubated for 1 h at 37℃ before adding the agonist SP, produces a non-surmountable antagonism of agonist concentration-response curve. For Orvepitant apparents pKB value of 10.30[1].
In Vivo Orvepitant (Compound 3a; 0.3-10 mg/kg; Oral administration; marmoset) treatment shows a dose dependant reduction of the number of postures was observed at 1 mg/kg (34.9% reduction), 3 mg/kg (36.6% reduction) and 10 mg/kg (46.4% reduction), suggesting a potential anxiolytic-like effect of the compound[1]. Orvepitant (compound 3a) shows an oral bioavailability (F) of 17% in rat and 55% in dog, plasma clearance (Clp) of 29 mL/min/kg in rat and 6 mL/min/kg in dog and a half-life of 2.3 h in rat and 6.1 h in dog. As far as the brain penetration in rats is concerned, a B/P ratio of 1.2 is observed 5 min after the i.v. administration of a 1 mg/kg dose of Orvepitant[1]. Animal Model: Human threat test in the marmoset (HTT)[1] Dosage: 0.3 mg/kg, 1 mg/kg, 3 mg/kg and 10 mg/kg Administration: Oral administration Result: A dose dependant reduction of the number of postures was observed at 1 mg/kg (34.9% reduction), 3 mg/kg (36.6% reduction) and 10 mg/kg (46.4% reduction).
References

[1]. Di Fabio R, et al. Identification, biological characterization and pharmacophoric analysis of a new potent and selective NK1 receptor antagonist clinical candidate. Bioorg Med Chem. 2013 Nov 1;21(21):6264-73.

[2]. Smith J, et al. The Neurokinin-1 Receptor Antagonist Orvepitant Is a Novel Antitussive Therapy for Chronic Refractory Cough: Results From a Phase 2 Pilot Study (VOLCANO-1). Chest. 2020 Jan;157(1):111-118.
Molecular Formula C35H39F7N4O6
Molecular Weight 744.69600
Exact Mass 744.27600
PSA 121.70000
LogP 6.32230
579475-21-1 structure

579475-21-1

110-16-7 structure

110-16-7

~%

579475-24-4 structure

579475-24-4

Literature: GLAXO GROUP LIMITED Patent: WO2009/124996 A1, 2009 ; Location in patent: Page/Page column 18 ;
579475-18-6 structure

579475-18-6

110-16-7 structure

110-16-7

~%

579475-24-4 structure

579475-24-4

Literature: GLAXO GROUP LIMITED Patent: WO2009/124996 A1, 2009 ; Location in patent: Page/Page column 15-17 ;
579475-18-6 structure

579475-18-6

110-16-7 structure

110-16-7

~%

1190692-55-7 structure

1190692-55-7

579475-24-4 structure

579475-24-4

Literature: GLAXO GROUP LIMITED Patent: WO2009/124996 A1, 2009 ; Location in patent: Page/Page column 19-21 ;

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title: CAS No. 579475-24-4 | Chemsrc address: https://m.chemsrc.com/en/baike/1046823.html

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