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在大鼠心脏上同时激动α1肾上腺素受体(α1-AR)与β-肾上腺素受体的(β-AR),较单独激动β-AR时产生的cAMP明显减少,α1A-AR亚型抑制,而α1B-AR亚型增强β-AR刺激cAMP生成的作用。但α1-AR及其亚型激动不影响forskolin引起的cAMP生成,亦不影响β-AR与[125I]吲哚洛尔的最大结合容量和解离常数。苯福林激动α1-AR对三磷酸鸟苷使异丙肾上腺素与[125I]吲哚洛尔的竞争抑制曲线右移程度无显著影响。提示α1-AR及其亚型影响β-AR心肌正性变力效应的作用发生在腺苷酸环化酶激动之前的环节,但并不影响β-AR本身及其与G蛋白的偶联。
The α1-AR and β-adrenergic receptor (β-AR) were significantly increased in the rat heart compared with those in the β-AR alone, and the α1A-AR subtype was inhibited , While α1B-AR subtype enhances the effect of β-AR on cAMP production. However, the activation of α1-AR and its subtypes did not affect the production of cAMP induced by forskolin, nor did it affect the maximal binding capacity and dissociation constant of β-AR to [125I] pindolol. Phenylephrine agonized α1-AR had no significant effect on the extent of right-shift of competitive inhibition of isoproterenol with [125I] pindolol by guanosine triphosphate. These results suggest that the effect of α1-AR and its subtypes on the positive force effect of β-AR myocardium occurs before the activation of adenylate cyclase but does not affect the β-AR itself and its coupling with G protein.