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腺苷酸对心肌收缩有明显影响,但心肌腺苷酸受体的含量很少,只达脑组织的1/25左右。因此,~3H-环己基腺苷酸、~3H-2-氯腺苷酸及~(125)I-羟苯异丙基腺苷酸(~(125)I-HPIA)等放射性配基虽广泛应用于研究脑组织的腺苷酸受体,但这些放射性配基与心肌膜制备结合时的非特异与特异结合比太高,因而很难应用于心肌腺苷酸受体研究。最近,美国Oklahoma医学研究基金会的Linden等自腺苷酸经N~6-4-硝基苯腺苷酸(N~6-4-Nitroben-zyladenosine)合成N~6-4-氨苯腺苷酸(N~6-4-aminobenzyladenosine,ABA),再以~(125)I标记,得到一种新型的腺苷酸受体放射性配基~(125)I-氨苯腺苷酸(~(125)I-ABA),并在大鼠心、脑等膜制备与~(125)I-HPIA进行了
Adenylate has a significant effect on myocardial contractility, but the content of myocardial adenylate receptors is very small, only about 1/25 of brain tissue. Therefore, ~ 3H-Cyclohexyladenosine, ~ 3H-2-chloroadenosine and ~ (125) I-hydroxyphenylisopropyl adenine (~ 125 I- HPIA) Is used to study adenylate receptors in brain tissue. However, these radioligands are too nonspecific and specific to bind to myocardial membrane preparations and are therefore very difficult to apply in cardiac adenylate receptor studies. Recently, Linden et al. From the Oklahoma Medical Research Foundation of the United States synthesized N ~ 6-4-nitrobenzosinosine from N ~ 6-4-Nitrobenzyldenosine (125) I-adenine adenine (~ (125) I) was obtained by the labeling of ~ (125) I with N ~ 6-4-aminobenzyladenosine ) I-ABA) and were prepared in rat heart, brain and other membranes with ~ (125) I-HPIA