Journal article

Pharmacological discrimination of calcitonin receptor: receptor activity-modifying protein complexes

DL Hay, G Christopoulos, A Christopoulos, DR Poyner, PM Sexton

Molecular Pharmacology | AMER SOC PHARMACOLOGY EXPERIMENTAL THERAPEUTICS | Published : 2005

Abstract

Calcitonin (CT) receptors dimerize with receptor activity-modifying proteins (RAMPs) to create high-affinity amylin (AMY) receptors, but there is no reliable means of pharmacologically distinguishing these receptors. We used agonists and antagonists to define their pharmacology, expressing the CT(a) receptor alone or with RAMPs in COS-7 cells and measuring cAMP accumulation. Intermedin short, otherwise known as adrenomedullin 2, mirrored the action of alpha CGRP, being a weak agonist at CT(a), AMY(2a), and AMY(3a) receptors but considerably more potent at AMY(1a) receptors. Likewise, the linear calcitonin gene-related peptide (CGRP) analogs (Cys(ACM)(2,7))h alpha CGRP and (Cys(Et)(2,7))h alp..

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