Chiba S
Arzneimittelforschung. 1979;29(6):895-7.
Direct effects of 5-(3-tert.-butylamino-2-hydroxy) propoxy-3,4-dihydrocarbostyril hydrochloride (carteolol) on chronotropic and inotropic activity were investigated in seventeen isolated atrium preparations which were suspended in a bath and perfused with arterial blood from the heparinized donor dog. Carteolol has little adrenergic beta-receptor stimulating effect in doses which block prominent positive chronotropic and inotropic effects of norepinephrine. At relatively larger doses, however, carteolol produced a long-lasting positive chronotrophic and inotropic effect. At extremely larger doses, carteolol produced a negative inotropic effect with little or slight negative chronotropic effect. In propranolol-treated preparations, carteolol induced less positive effects. Propranolol-induced negative chronotropic and inotropic effects were significantly reduced by treatment with carteolol. From these results, carteolol has not only potent beta-adrenoceptor blocking property but also sympathomimetic activity, and different beta 1-type cardiac adrenergic receptors may probably be suggested.
在17个离体心房标本中研究了5-(3-叔丁氨基-2-羟基)丙氧基-3,4-二氢卡巴唑盐酸盐(卡替洛尔)对变时性和变力性活性的直接作用。这些标本悬浮于浴槽中,并用来自肝素化供体犬的动脉血进行灌注。卡替洛尔在能阻断去甲肾上腺素显著的正性变时性和变力性作用的剂量下,几乎没有肾上腺素能β受体刺激作用。然而,在相对较大剂量时,卡替洛尔产生持久的正性变时性和变力性作用。在极大剂量时,卡替洛尔产生负性变力性作用,而负性变时性作用很小或轻微。在普萘洛尔处理的标本中,卡替洛尔产生的正性作用较小。用卡替洛尔处理可显著减轻普萘洛尔诱导的负性变时性和变力性作用。从这些结果来看,卡替洛尔不仅具有强大的β肾上腺素受体阻断特性,还具有拟交感活性,并且可能提示存在不同的β1型心脏肾上腺素能受体。