Structural determinants for binding to CGRP receptors expressed by human SK-N-MC and Col 29 cells: studies with chimeric and other peptides

摘要

Structure-activity relationships for the binding of human α-calcitonin gene-related peptide 8-37 (hαCGRP_8-37) have been investigated at the CGRP receptors expressed by human Sk-N-MC (neuroblastoma) and Col29 (colonic epithelia) cells by radioligand binding assays and functional assays (hαCGRP stimulation of adenylate cyclase). On SK-N-MC cells the potency order was hαCGRP_8-37 > hαCGRP_19-37=AC187>rat amylin_8-37> hα[Tyr~0]- CGRP_28-37 (apparent pKBs of 7.49±0.25, 5.89±0.20, 6.18±0.20, 6.18±0.19, 5.85±0.19 and 5.25±0.07). The SK-N-MC receptor appeared CGRP_1-like.