Literature DB >> 25078633

Neurokinin-1 receptor antagonist orvepitant is an effective inhibitor of itch-associated response in a Mongolian gerbil model of scratching behaviour.

Michael K Trower1, Amy Fisher, Neil Upton, Emiliangelo Ratti.   

Abstract

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 GR73632, 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 GR73632 (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.
© 2014 John Wiley & Sons A/S. Published by John Wiley & Sons Ltd.

Entities:  

Keywords:  GR73632; gerbil; itch; neurokinin-1; orvepitant; pruritogen; pruritus; scratch; substance P; tachykinin

Mesh:

Substances:

Year:  2014        PMID: 25078633     DOI: 10.1111/exd.12528

Source DB:  PubMed          Journal:  Exp Dermatol        ISSN: 0906-6705            Impact factor:   3.960


  3 in total

1.  Neurokinin 1 Receptor Antagonists for Pruritus.

Authors:  Majid Alam; Joerg Buddenkotte; Fareed Ahmad; Martin Steinhoff
Journal:  Drugs       Date:  2021-03-06       Impact factor: 9.546

Review 2.  NK-1 Receptor Antagonists and Pruritus: Review of Current Literature.

Authors:  Marcelina Pojawa-Gołąb; Kamila Jaworecka; Adam Reich
Journal:  Dermatol Ther (Heidelb)       Date:  2019-06-12

3.  Neurokinin-1 antagonist orvepitant for EGFRI-induced pruritus in patients with cancer: a randomised, placebo-controlled phase II trial.

Authors:  Bruno Vincenzi; Mike Trower; Ajay Duggal; Pamela Guglielmini; Peter Harris; David Jackson; Mario E Lacouture; Emiliangelo Ratti; Giuseppe Tonini; Andrew Wood; Sonja Ständer
Journal:  BMJ Open       Date:  2020-02-06       Impact factor: 2.692

  3 in total

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