THE METHODOLOGICAL STUDY ON RADIOLIGAND BINDING ASSAY OF ?-ADRENERGIC RECEPTORS WITH RAT BRAIN SECTIONS
- VernacularTitle:用大鼠脑切片进行?—受体放射配体结合实验的方法学研究
- Author:
Xuenong BO
- Publication Type:Journal Article
- From:
Chinese Pharmacological Bulletin
1986;0(04):-
- CountryChina
- Language:Chinese
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Abstract:
It is generally considered that the experiment of radioligand binding assay ( RBA) of receptors with frozen tissue sections is difficult. In this study the conditions involved in the RBA of ?-adre-nergic receptors with rat brain sections on the superior colliculus level was investigated. 3H-Dihydroalprenolol (3H-DHA), a ?-adrener-gic receptor antagonist, was used as the labeled ligand. The data obtained from this experment are as follows: Bmax=17.3?4.5fmol/mg of dry tissue, Kd=5.8?0.6nM, association rate constant=0.112?0.025 nM-1 ? min-1,dissociation rate constant=0.69?0.07min-1, the IC50 of propranolol=1.00?0.15?10-8M, IC50 of practolol=1.67?0.22?10-5M, IC50 of isopreterenol=1.32?0.31 ? 10-6M.These results are in agreement with those obtained from RBA with homogenate, which indicates that the frozen tissue sections are useful preparations in the RBA of ?-adrenergic receptors.
