| Identification | Back Directory | [Name]
Orvepitant maleate | [CAS]
579475-24-4 | [Synonyms]
GW823296 maleate
Orvepitant maleate | [Molecular Formula]
C35H39F7N4O6 | [MDL Number]
MFCD20926416 | [MOL File]
579475-24-4.mol | [Molecular Weight]
744.696 |
| Chemical Properties | Back Directory | [solubility ]
Acetonitrile: Slightly Soluble: 0.1-1 mg/ml
Chloroform: Slightly Soluble: 0.1-1 mg/ml | [form ]
Solid | [color ]
Off-white to light yellow |
| Hazard Information | Back Directory | [Uses]
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]. | [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).
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| [IC 50]
NK1: 10.2 (pKi) | [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. DOI:10.1016/j.bmc.2013.09.001
[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. DOI:10.1016/j.chest.2019.08.001 |
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