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一般认为α_1肾上腺素受体在大鼠心脏中分为α_(1A)和α_(1B)两种受体亚型,其中α_(1A)对WB_(4101)和5-Methyl-Ura-pidil亲和性较高,对CEC(氯乙基可乐宁)不敏感,而α_(1B)亚型则对上述两种药物低亲和,并可被CEC不可逆阻断。本文用放射配体结合实验方法观察大鼠心肌组织粗制膜在CEC处理前后α_1受体亚型比例的改变。结果表明心肌组织粗制膜用10μmol/L CEC处理后与~(125)IBE的结合容量Bmax由120.8±9.4fmol/mg下降至44.6±6.8fmol/mg(约35%)。在CEC处理前,WB_(4101)和5-Methyl-Urapidil的竞争抑制曲线的计算机两位点拟合均显示有
It is generally accepted that the α 1 adrenergic receptors are classified into α 1A and α 1A receptor subtypes in rat hearts. Among them, α 1A 1A 2 binds to both WB 4101 and 5-Methyl-Ura-pidil The sex is high, insensitive to CEC (chloroethyl clonidine), while α 1B subtype is low-affinity to both drugs and irreversibly blocked by CEC. In this paper, radioligand binding assay was used to observe the change of α 1 receptor subtypes in rat cardiac myocytes before and after CEC treatment. The results showed that the Bmax of binding capacity to 125EBE decreased from 120.8 ± 9.4fmol / mg to about 44.6 ± 6.8fmol / mg (about 35%) after treatment with 10μmol / L CEC. Prior to CEC treatment, the computer two-point fit of the competitive inhibition curve for WB 4101 and 5-Methyl Urapidil showed