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原生动物克氏锥虫中β-肾上腺素能受体的放射性配体结合特性研究

Radioligand binding characterization of beta-adrenergic receptors in the protozoa Trypanosoma cruzi.

作者信息

de Castro S L, Oliveira M M

出版信息

Comp Biochem Physiol C Comp Pharmacol Toxicol. 1987;87(1):5-8. doi: 10.1016/0742-8413(87)90170-8.

Abstract

A direct radioligand binding technique utilizing the beta-adrenergic antagonist [3H]dihydroalprenolol was employed in the identification and characterization of Trypanosoma cruzi beta-adrenergic receptors. [3H]DHA binding was saturable (Bmax = 1.5 pmol/10(6) cells) with an apparent equilibrium dissociation constant (Kd) of 127 nM. Binding of [3H]DHA was displaced by propranolol in a concentration-dependent manner. The relative potency order of adrenergic ligands in displacing [3H]DHA binding was: propranolol greater than or equal to alprenolol greater than epinephrine. 5-Hydroxytryptamine, phentolamine and catechol had no effect. The experimental results support the suggestion that beta-adrenergic receptors are present in the pathogenic protozoa Trypanosoma cruzi.

摘要

利用β-肾上腺素能拮抗剂[3H]二氢阿普洛尔的直接放射性配体结合技术,用于鉴定和表征克氏锥虫的β-肾上腺素能受体。[3H]DHA结合具有饱和性(Bmax = 1.5 pmol/10(6) 细胞),表观平衡解离常数(Kd)为127 nM。普萘洛尔以浓度依赖性方式取代[3H]DHA的结合。肾上腺素能配体取代[3H]DHA结合的相对效价顺序为:普萘洛尔≥阿普洛尔>肾上腺素。5-羟色胺、酚妥拉明和儿茶酚无作用。实验结果支持致病性原生动物克氏锥虫中存在β-肾上腺素能受体这一观点。

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