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Neurokinin‐1 receptor antagonist orvepitant is an effective inhibitor of itch‐associated response in a M ongolian gerbil model of scratching behaviour
Author(s) -
Trower Michael K.,
Fisher Amy,
Upton Neil,
Ratti Emiliangelo
Publication year - 2014
Publication title -
experimental dermatology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.108
H-Index - 96
eISSN - 1600-0625
pISSN - 0906-6705
DOI - 10.1111/exd.12528
Subject(s) - scratching , gerbil , antagonist , agonist , pharmacology , antipruritic , receptor antagonist , nk1 receptor antagonist , receptor , medicine , chemistry , substance p , neuropeptide , physics , ischemia , acoustics
Data suggest that substance P could play an important role in pruritus, and therefore, blockade of the neurokinin ( NK )‐1 receptor might be antipruritic. Thus, we explored in the Mongolian gerbil the effect on scratching behaviour, induced by intra‐dermal injection of the NK ‐1 receptor‐specific agonist GR 73632, of oral administration of the NK ‐1 receptor antagonist orvepitant. Orvepitant at all doses tested (0.1–10 mg/kg p.o.) produced a profound inhibition of GR 73632 (30 nmol i.d.) induced hindlimb scratching; the minimum effective dose of orvepitant in this model was identified as ≤0.1 mg/kg. The data generated supported the proposition that the antipruritic potential of orvepitant should be evaluated in clinical trials.