Mutafova-Yambolieva V, Staneva-Stoytcheva D
Acta Physiol Pharmacol Bulg. 1985;11(1):18-25.
Experiments were made to test the effects of originally synthesized piperazine derivative of 2-aminotetralin (P11) on the alpha-adrenergic receptors of isolated vessels. Inhibition of the contracting effects of exogenously introduced noradrenaline into isolated rabbit ear artery was found at concentrations of P11 and phentolamine 1 X 10(-8) to 1 X 10(-4) M. IC50 for P11 is 0.68 microM, for phentolamine -- 0,40 microM. There is a certain shift to the right of the concentration effect curves for noradrenaline in isolated strip of rabbit aorta when P11 and phentolamine are applied in concentrations of 1 X 10(-7) to 1 X 10(-5) M. pA2 for P11 is 7.31, for phentolamine -- 8.04. Potentiation of the maximum effect of noradrenaline is observed after P11 1 X 10(-5) M, which decreases upon preliminary administration of cocaine 1 X 10(-5) M and propranolol 1 X 10(-6) M. The tested compound manifests alpha-adrenergic blocking action in the organs studied.
进行实验以测试最初合成的2-氨基四氢萘哌嗪衍生物(P11)对离体血管α-肾上腺素能受体的影响。在P11和酚妥拉明浓度为1×10⁻⁸至1×10⁻⁴M时,发现其对向离体兔耳动脉中外源性引入的去甲肾上腺素的收缩作用有抑制作用。P11的IC50为0.68微摩尔,酚妥拉明为0.40微摩尔。当以1×10⁻⁷至1×10⁻⁵M的浓度应用P11和酚妥拉明时,离体兔主动脉条中去甲肾上腺素的浓度效应曲线有一定程度的右移。P11的pA2为7.31,酚妥拉明为8.04。在1×10⁻⁵M的P11作用后,观察到去甲肾上腺素最大效应增强,而在预先给予1×10⁻⁵M可卡因和1×10⁻⁶M普萘洛尔后这种增强作用减弱。所测试的化合物在所研究的器官中表现出α-肾上腺素能阻断作用。