Discovery of a novel superpotent and selective melanocortin-4 receptor antagonist (HS024): evaluation in vitro and in vivo.

Kask, A; Mutulis, F; Muceniece, R; Pähkla, R; Mutule, I; E Wikberg, J; Rägo, L; B Schiöth, H

doi:10.1210/endo.139.12.6352

Public

Discovery of a novel superpotent and selective melanocortin-4 receptor antagonist (HS024): evaluation in vitro and in vivo.

Shared by NobleBlocks on Dec 1, 1998 • 12:00 AM UTC

Authors:

A Kask

F Mutulis

R Muceniece

Abstract

Several novel cyclic MSH analogs were synthesized, and their binding properties were tested on cells transiently expressing the human melanocortin-1 (MC1), MC3, MC4, and MC5 receptors. We discovered a novel substance (HS024) that showed about 20-fold selectivity and very high affinity (Ki = 0.29 nM)...

Discussions