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

Kyung Min Lim, Young Ho Park

Research output: Contribution to journalArticlepeer-review

32 Scopus citations

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.

Original languageEnglish
Pages (from-to)393-396
Number of pages4
JournalArchives of Pharmacal Research
Volume35
Issue number3
DOIs
StatePublished - Mar 2012

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