Koike K, Horinouchi T, Takayanagi I
Department of Chemical Pharmacology, Toho University School of Pharmaceutical Sciences, Chiba, Japan.
Eur J Pharmacol. 1995 Jun 12;279(2-3):159-63. doi: 10.1016/0014-2999(95)00147-d.
The mechanisms of the beta-adrenoceptor-mediated relaxation induced by noradrenaline in guinea pig taenia caecum were investigated. Noradrenaline caused graded relaxation of this preparation. However, the concentration-response curves for noradrenaline were unaffected by propranolol (approximately 10(-5) M) or phentolamine (approximately 10(-5) M). The responses to noradrenaline were antagonized in a concentration-dependent manner by bupranolol, and Schild plots of the data revealed a pA2 value of 5.53. Also, bupranolol antagonized responses to isoprenaline, and Schild plots of the data revealed the pA2 value to be 8.53. Noradrenaline significantly increased the cyclic AMP level in this preparation. Bupranolol (10(-4) M) significantly decreased the cyclic AMP response elicited by noradrenaline, whereas propranolol (10(-5) M) produced no effect. These results suggest that the relaxant response to noradrenaline in guinea pig taenia caecum is mainly mediated by beta 3-adrenoceptors (or atypical beta-adrenoceptors) and that in guinea pig taenia caecum noradrenaline behaves as a beta 3-selective adrenoceptor agonist.
研究了去甲肾上腺素在豚鼠盲肠带中诱导的β-肾上腺素能受体介导的舒张机制。去甲肾上腺素使该标本产生分级舒张。然而,去甲肾上腺素的浓度-反应曲线不受普萘洛尔(约10⁻⁵ M)或酚妥拉明(约10⁻⁵ M)的影响。布普萘洛尔以浓度依赖性方式拮抗对去甲肾上腺素的反应,数据的Schild图显示pA2值为5.53。此外,布普萘洛尔拮抗对异丙肾上腺素的反应,数据的Schild图显示pA2值为8.53。去甲肾上腺素显著提高了该标本中的环磷酸腺苷水平。布普萘洛尔(10⁻⁴ M)显著降低了去甲肾上腺素引起的环磷酸腺苷反应,而普萘洛尔(10⁻⁵ M)则无作用。这些结果表明,豚鼠盲肠带对去甲肾上腺素的舒张反应主要由β3-肾上腺素能受体(或非典型β-肾上腺素能受体)介导,并且在豚鼠盲肠带中去甲肾上腺素表现为β3选择性肾上腺素能受体激动剂。