Quinine analogs as non-peptide calcitonin gene-related peptide (CGRP) receptor antagonists
摘要:
A high-throughput screen identified quinine analog 1 as an antagonist of the human calcitonin gene-related peptide (hCGRP) receptor. Thus, compound 1 displaces [I-125]-CGRP from the hCGRP receptor and inhibits CGRP-mediated cAMP production with IC50 values of 5.9 +/- 1.2 mu M and 26 +/- 5 mu M, respectively. A limited structure-activity study of 1 is described. (C) 1997 Elsevier Science Ltd.