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[H-3]FORSKOLIN BINDING TO CARDIAC ADENYLATE CYCLASE IN GUINEA PIGS CHRONICALLY INFUSED WITH ISOPROTERENOL

机译:[H-3]福斯高林与慢性感染异丙肾上腺素的豚鼠的心脏腺苷酸环化酶结合

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Guinea pigs were infused with the beta-adrenoceptor agonist isoproterenol (400 mu g/kg/hr, 7 days) and cardiac adenylate cyclase was detected using [H-3]forskolin. Two populations of [H-3]forskolin binding sites were present in heart, the affinities (K-D 2 nM and 280 nM) and densities (Bmax 9 and 900 fmol/mg protein) of which were unchanged by isoproterenol infusion compared with vehicle (1 mM HCl). The autoradiographic localisation of [H-3]forskolin binding was also unchanged. The G protein activators NaF 10 mM and 5'-guanylylimidodiphosphate (Gpp(NH)p) 10 mu M increased [H-3]forskolin binding in heart from vehicle-treated animals by 100% and 80% respectively. NaF-stimulated binding was unchanged in isoproterenol-treated animals, however, Gpp(NH)p-stimulated binding was reduced by 35% which may indicate an increased influence of Gi. [References: 46]
机译:向豚鼠注射β-肾上腺素受体激动剂异丙肾上腺素(400μg / kg / hr,7天),并使用[H-3] forskolin检测到心脏腺苷酸环化酶。心脏中存在两个[H-3]佛司可林结合位点,与载体相比,异丙肾上腺素输注的亲和力(KD 2 nM和280 nM)和密度(Bmax 9和900 fmol / mg蛋白)没有变化。 mM HCl)。 [H-3]福司柯林结合的放射自显影定位也未改变。 G蛋白激活剂NaF 10 mM和5'-鸟苷二磷酸二磷酸酯(Gpp(NH)p)10μM使媒介物治疗的动物心脏中的[H-3]毛喉素结合增加100%和80%。在异丙肾上腺素治疗的动物中,NaF刺激的结合未改变,但是,Gpp(NH)p刺激的结合降低了35%,这可能表明Gi的影响增加。 [参考:46]

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