β-肾上腺素能激动剂在无细胞系统中对β-肾上腺素能受体的脱敏作用：5'-（β，γ-亚氨基）三磷酸鸟苷和其他嘌呤核苷酸的再敏化作用
Desensitization of beta-adrenergic receptors by beta-adrenergic agonists in a cell-free system: resensitization by guanosine 5'-(beta, gamma-imino)triphosphate and other purine nucleotides.
作者信息
Mukherjee C, Lefkowitz R J
出版信息
Proc Natl Acad Sci U S A. 1976 May;73(5):1494-8. doi: 10.1073/pnas.73.5.1494.
Abstract
Incubation of purified frog erythrocyte membranes with beta-adrenergic agonists at 25 degrees produces relatively rapid (half-time about 10 min) desensitization (inactivation) of about 60% of the beta-adrenergic receptor binding sites. The desensitized receptors no longer bind the specific beta-adrenergic ligand (-)[3H]dihydroalprenolol. The decrease in the number of functional beta-adrenergic receptors is also manifest as a decreased ability of isoproterenol to stimulate the membrane-bound adenylate cyclase.
摘要
在25摄氏度下，将纯化的青蛙红细胞膜与β-肾上腺素能激动剂一起温育，会使约60%的β-肾上腺素能受体结合位点相对快速地（半衰期约10分钟）脱敏（失活）。脱敏后的受体不再结合特异性β-肾上腺素能配体（-）[3H]二氢烯丙洛尔。功能性β-肾上腺素能受体数量的减少也表现为异丙肾上腺素刺激膜结合腺苷酸环化酶的能力下降。
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