Referenced in: none

Automatically associated channels: TRP , TRPV , TRPV1

Title: Development of PAC-14028, a novel transient receptor potential vanilloid type 1 (TRPV1) channel antagonist as a new drug for refractory skin diseases.

Authors: Kyung-Min Lim, Young-Ho Park

Journal, date & volume: Arch. Pharm. Res., 2012 Mar , 35, 393-6

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/22477184

Abstract
The transient receptor potential vanilloid 1 (TRPV1) is a member of nonselective cation channels and has been implicated in the progression of neurogenic inflammation and nociception. Through the synthesis of over 2,000 new compounds, a novel non-vanilloid TRPV1 antagonist PAC-14028 was discovered. As well as ideal physicochemical and pharmacokinetic properties, PAC-14028 showed meaningful efficacies against diverse disease models that include visceral pain, inflammatory bowel disease, and inflammatory pain. Of note, PAC-14028 effectively attenuates atopic dermatitis and pruritus without significant adverse effects, which is a substantial benefit over conventional pharmacotherapy. This report introduces the potential of a novel TRPV1 antagonist PAC-14028 as a new drug for atopic dermatitis and pruritus.