Ishizaka Y, Ishizaka Y, Tanaka M, Kitamura K, Kangawa K, Minamino N, Matsuo H, Eto T
First Department of Internal Medicine, Miyazaki Medical College.
Biochem Biophys Res Commun. 1994 Apr 15;200(1):642-6. doi: 10.1006/bbrc.1994.1496.
A newly identified human peptide, adrenomedullin (AM) increased cAMP levels with dose and time dependencies in a manner similar to that of human calcitonin gene-related peptide (CGRP) in rat vascular smooth muscle cells (VSMC). The EC50 value of human AM is 2 x 10(-8) M which is slightly higher than that of CGRP (8.5 x 10(-9) M). In a receptor binding assay for AM in rat VSMC, the binding of [125I] AM was competitively inhibited by human AM, but not by human CGRP. Thus, AM is thought to increase intracellular cAMP in rat VSMC via its specific receptor to evoke vasodilation.
一种新发现的人类肽,肾上腺髓质素(AM)在大鼠血管平滑肌细胞(VSMC)中,以与人类降钙素基因相关肽(CGRP)相似的方式,呈剂量和时间依赖性地增加环磷酸腺苷(cAMP)水平。人AM的半数有效浓度(EC50)值为2×10⁻⁸ M,略高于CGRP的(8.5×10⁻⁹ M)。在大鼠VSMC中进行的AM受体结合试验中,[¹²⁵I]AM的结合被人AM竞争性抑制,但不被人CGRP抑制。因此,AM被认为通过其特异性受体增加大鼠VSMC中的细胞内cAMP,从而引起血管舒张。