特定的3H-氟哌啶醇与紫贻贝前足丝收缩肌中多巴胺受体的结合。

Specific 3H-haloperidol binding to dopamine receptors in the anterior byssus retractor muscle of Mytilus edulis.

作者信息

Ishii Y, Takayanagi I

出版信息

Jpn J Pharmacol. 1982 Dec;32(6):1151-5. doi: 10.1254/jjp.32.1151.

DOI:10.1254/jjp.32.1151

PMID:7161965

Abstract

The anterior byssus retractor muscle (ABRM) of Mytilus edulis has specific dopamine receptors. We carried out a radioligand binding assay for dopamine receptors in ABRM using (3H)-haloperidol as the radioligand. High affinity binding of (3H)-haloperidol has been shown. Scatchard analysis showed a single component of binding with an apparent equilibrium constant (KD) of 1.6 nM and a maximal number of binding sites (Bmax) of 219 fmoles/mg protein. Some dopamine antagonists displaced 3 nM (3H)-haloperidol binding, and the IC50 and Ki-value of these drugs were calculated. Considering these results, this muscle is thought to be suitable for a study of the dopamine receptors.

摘要

紫贻贝的前足丝牵缩肌（ABRM）具有特定的多巴胺受体。我们以（3H）-氟哌啶醇作为放射性配体，对ABRM中的多巴胺受体进行了放射性配体结合测定。结果显示（3H）-氟哌啶醇具有高亲和力结合。Scatchard分析表明存在单一结合成分，其表观平衡常数（KD）为1.6 nM，最大结合位点数（Bmax）为219 fmol/mg蛋白质。一些多巴胺拮抗剂能取代3 nM（3H）-氟哌啶醇的结合，并计算出这些药物的半数抑制浓度（IC50）和抑制常数（Ki值）。综合这些结果，认为该肌肉适合用于多巴胺受体的研究。