Endoh M, Satoh K, Taira N
Naunyn Schmiedebergs Arch Pharmacol. 1982 Mar;318(4):370-3. doi: 10.1007/BF00501181.
The property of adrenoceptors mediating the positive inotropic effect (PIE) in the ventricular muscle of the Japanese monkey (Macaca fuscata) was investigated by the use of phenylephrine (PE) and adrenoceptor antagonists. The intrinsic activity (0.6) and the pD2-value (5.41) for PE were comparable to those in other mammalian species. The beta-adrenoceptor antagonist, pindolol (3 x 10(-8) mol/l) shifted only the upper part of the concentration-response curve (CRC) for PE to the right; the pD2-value for PE was not significantly affected by pindolol. On the other hand, phentolamine (10(-6) mol/l) shifted the lower part of the CRC for PE more than the upper part. In the presence of both pindolol and phentolamine the curve was shifted to the right in a parallel manner. The time required for twitch relaxation was negatively correlated to the degree of PIE of PE in the presence of phentolamine but not pindolol. These results indicate that both beta- and alpha-adrenoceptors mediate the positive inotropic action in the ventricular muscle of the Japanese monkey and that in contrast to the action via beta-adrenoceptors the action via alpha-adrenoceptors is not accompanied by the "relaxant effect".
利用去氧肾上腺素(PE)和肾上腺素能受体拮抗剂,研究了日本猕猴(食蟹猴)心室肌中介导正性肌力作用(PIE)的肾上腺素能受体特性。PE的内在活性(0.6)和pD2值(5.41)与其他哺乳动物物种相当。β肾上腺素能受体拮抗剂吲哚洛尔(3×10⁻⁸ mol/l)仅使PE的浓度-反应曲线(CRC)的上部右移;吲哚洛尔对PE的pD2值无显著影响。另一方面,酚妥拉明(10⁻⁶ mol/l)使PE的CRC下部比上部右移更多。在吲哚洛尔和酚妥拉明同时存在的情况下,曲线以平行方式右移。在酚妥拉明而非吲哚洛尔存在的情况下,抽搐松弛所需时间与PE的PIE程度呈负相关。这些结果表明,β和α肾上腺素能受体均介导日本猕猴心室肌的正性肌力作用,并且与通过β肾上腺素能受体的作用相反,通过α肾上腺素能受体的作用不伴有“松弛效应”。