An LPAR ₅ -antagonist that reduces nociception and increases pruriception.

ABSTRACT:

Introduction

The G-protein coupled receptor LPAR₅ plays a prominent role in LPA-mediated pain and itch signaling. In this study we focus on the LPAR₅-antagonist compound 3 (cpd3) and its ability to affect pain and itch signaling, both in vitro and in vivo.

Methods

Nociceptive behavior in wild type mice was induced by formalin, carrageenan or prostaglandin E2 (PGE₂) injection in the hind paw, and the effect of oral cpd3 administration was measured. Scratch activity was measured after oral administration of cpd3, in mice overexpressing phospholipase A2 ( sPLA2tg ), in wild type mice (WT) and in TRPA1-deficient mice (Trpa1 KO). In vitro effects of cpd3 were assessed by measuring intracellular calcium release in HMC-1

SUBMITTER: Langedijk J 

PROVIDER: S-EPMC9360597 | biostudies-literature | 2022

REPOSITORIES: biostudies-literature