125I SCH 23982（一种选择性多巴胺（D1）受体配体）与人肾皮质来源的质膜的特异性结合。

Specific binding of 125I SCH 23982, a selective dopamine (D1) receptor ligand to plasma membranes derived from human kidney cortex.

作者信息

Hughes A, Sever P

机构信息

Department of Clinical Pharmacology, St Mary's Hospital Medical School, London, U.K.

出版信息

Biochem Pharmacol. 1989 Mar 1;38(5):781-5. doi: 10.1016/0006-2952(89)90231-1.

DOI:10.1016/0006-2952(89)90231-1

PMID:2522780

Abstract

Binding of the selective D-1 dopamine receptor ligand 125I SCH 23982 was studied using crude plasma membranes derived from human renal cortex. 125I SCH 23982 bound saturably to a single high affinity site (Kd = 650 pM, Bmax = 19 fmol/mg protein). Binding at 37 degrees was rapid and reversible with forward and reverse rate constants of 5.79 x 10(8) min-1 m-1 and 0.156 min-1 respectively. Antagonist and agonist competition for 125I SCH 23982 binding was also consistent with the existence of a single site possessing pharmacological characteristics similar to a D-1 dopamine receptor. It is suggested that this site may represent a D-1 (or DA1) dopamine receptor present in human renal cortex.

摘要

利用源自人肾皮质的粗制质膜研究了选择性D-1多巴胺受体配体125I SCH 23982的结合情况。125I SCH 23982可饱和地结合至单一高亲和力位点（解离常数Kd = 650皮摩尔，最大结合容量Bmax = 19飞摩尔/毫克蛋白质）。37摄氏度时的结合迅速且可逆，正向和逆向速率常数分别为5.79×10(8) 分钟-1 米-1 和0.156分钟-1。拮抗剂和激动剂对125I SCH 23982结合的竞争也与存在一个具有类似于D-1多巴胺受体药理学特征的单一位点相一致。提示该位点可能代表存在于人肾皮质中的D-1（或DA1）多巴胺受体。