Kapas S, Clark A J
Department of Chemical Endocrinology, Medical College of St Bartholomew's Hospital, London, U.K.
Biochem Biophys Res Commun. 1995 Dec 26;217(3):832-8. doi: 10.1006/bbrc.1995.2847.
Calcitonin gene-related peptide (CGRP) is a 37 residue neuropeptide that is distantly related to adrenomedullin. We have recently reported the cloning and expression of an adrenomedullin receptor which is approximately 30% homologous to the canine orphan receptor RDC-1. Therefore we tested the hypothesis that RDC-1 was a CGRP receptor. The RDC-1 gene was expressed in COS-7 cells and showed a dose dependant increase of cAMP in response to CGRP and adrenomedullin (EC50 values of 3 x 10(-9) M and 1 x 10(-7) M respectively) which was inhibited by the CGRP antagonist CGRP[8-37]. There was no cAMP response to amylin or [Cys(acm)2,7]a-hCGRP. Ligand binding studies confirmed high affinity of this receptor for CGRP and CGRP[8-37] with KD values of 9.2 x 10(-9) M and 13.4 x 10(-9) M respectively.
降钙素基因相关肽（CGRP）是一种由37个氨基酸残基组成的神经肽，与肾上腺髓质素的关系较远。我们最近报道了一种肾上腺髓质素受体的克隆和表达，该受体与犬类孤儿受体RDC-1约有30%的同源性。因此，我们检验了RDC-1是CGRP受体的假说。RDC-1基因在COS-7细胞中表达，并且对CGRP和肾上腺髓质素表现出剂量依赖性的cAMP增加（EC50值分别为3×10⁻⁹ M和1×10⁻⁷ M），这被CGRP拮抗剂CGRP[8-37]所抑制。对胰淀素或[Cys(acm)2,7]α-hCGRP没有cAMP反应。配体结合研究证实该受体对CGRP和CGRP[8-37]具有高亲和力，KD值分别为9.2×10⁻⁹ M和13.4×10⁻⁹ M。
