1. GPCR/G Protein
    Neuronal Signaling
  2. Neurokinin Receptor
  3. Orvepitant maleate

Orvepitant maleate (Synonyms: GW823296 maleate)

Cat. No.: HY-122347A
Handling Instructions

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.

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Orvepitant maleate Chemical Structure

Orvepitant maleate Chemical Structure

CAS No. : 579475-24-4

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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].

IC50 & Target[1]

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).
Clinical Trial
Molecular Weight

744.70

Formula

C₃₅H₃₉F₇N₄O₆

CAS No.

579475-24-4

SMILES

O=C(N1[[email protected]@H](C2=CC=C(F)C=C2C)C[[email protected]@H](N3C[[email protected]@](CCC4=O)([H])N4CC3)CC1)N([[email protected]@H](C5=CC(C(F)(F)F)=CC(C(F)(F)F)=C5)C)C.O=C(O)/C=C\C(O)=O

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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

OrvepitantGW823296GW 823296GW-823296Neurokinin ReceptorNK receptorCRCsafewell-toleratedsubstance-Plong-lastingantidepressantCNSpharmacokineticsdepressivedisorderInhibitorinhibitorinhibit

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