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机构地区:[1]北京医科大学第三医院血管医学研究所,宁夏医学院生理教研室
出 处:《北京医科大学学报》1995年第6期411-413,共3页Journal of Peking University(Health Sciences)
基 金:国家自然科学基金
摘 要:利用放射配基结合实验及离体大鼠乳头肌灌流实验方法分析β2肾上腺素受体(β2~AR)在心室中的分布及其介导的正性变力效应。β2选择性拮抗剂ICI118,551与受体结合包含高、低亲和性两个位点,K1值分别与β2-和β1-AR的亲和性相符,各占43%与57%。ICI118,551与CGP20712A均可使异丙基肾上腺素(ISO)的浓度-效应曲线显著右移,pKB值分别为7.36与8.54,均介于它们与β1-和β2-AR的亲和性之间。以上结果表明:大鼠心室中共存β1-与β2-AR两种亚型,约各占一半;β1与β2-AR均介导ISO引起的正性变力效应。he distribution and inotropic effect of β2-AR in rat ventricules were studied by method of radioligand binding assays and contractile response measurement in isolated papillary muscles.The results showed that ICI 118,551 competitively inhibited 125I-Pindolol binding with 43%high(pkr=8.O±O.16)and 57% low (pkI=5.7 ±0.15)affinity sites.The K1values of both sites were coincident with KD value for β2-and β1-AR,respectively.Concentra- tion-response curves for ispro terenol were significently shifted to the right by ICI 118,551 and CGP 20712A.Their pKB values were between the KD values for β2-and β2-AR.The data suggest that β2-and β-AR coexist in rat ventricle and β2-AR also mediated positive inotropic response.
分 类 号:R331.31[医药卫生—人体生理学] Q463[医药卫生—基础医学]
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