Author/Authors :
Robert A. Daines، نويسنده , , Kelvin K. C. Sham، نويسنده , , Jack J. Taggart، نويسنده , , William D. Kingsbury، نويسنده , , James Chan، نويسنده , , Ann Breen، نويسنده , , Jyoti Disa، نويسنده , , Nambi Aiyar، نويسنده ,
Abstract :
A high-throughput screen identified quinine analog 1 as an antagonist of the human calcitonin generelated peptide (hCGRP) receptor. Thus, compound 1 displaces [125I]-CGRP from the hCGRP receptor and inhibits CGRP-mediated cAMP production with IC50 values of 5.9 ± 1.2 μM and 26 ± 5 μM, respectively. A limited structure-activity study of 1 is described.
