Discovery and Optimization of a Novel Series of Pyrazolyltetrahydropyran N-type Calcium Channel (Ca 2.2) Blockers for the Treatment of Pain

Overview

Journal Bioorg Med Chem Lett

Specialty Biochemistry

Date 2018 Oct 20

PMID 30337231

Citations 4

Authors

Mark J Wall

Nalin L Subasinghe

Michael P Winters

Mary Lou Lubin

Michael F A Finley

Ning Qin

Michael R Brandt

Michael P Neeper

Craig R Schneider

Raymond W Colburn

Christopher M Flores

Zhihua Sui

Affiliations

Soon will be listed here.

Abstract

A novel series of pyrazolyltetrahydropyran N-type calcium channel blockers are described. Structural modifications of the series led to potent compounds in both a cell-based fluorescent calcium influx assay and a patch clamp electrophysiology assay. Representative compounds from the series were bioavailable and showed efficacy in the rat CFA and CCI models of inflammatory and neuropathic pain.

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