Comparison of two substances with a possible alpha-adrenoceptor blocking and calcium channel blocking activity in rabbits in vivo under the paced and non-paced heart conditions. I. The effects on cardiac contractility (left ventricular dP/dtmax.).

V Gersl
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Abstract

The effects of substances--which in the isolated preparations possess calcium channel and alpha-adrenoceptor blocking activity--on cardiac contractility (dP/dtmax. of the blood pressure in the left ventricle) were evaluated. Substances VUFB 17951 (0.046 and 0.46 mg/kg) and VUFB 17959 (0.045 and 0.45 mg/kg) were administered intravenously in rabbits in vivo in pentobarbital anaesthesia under the conditions of the paced and non-paced heart rate. VUFB 17951 induced dose-dependent, immediately after the administration onsetting, progressive and significant decrease in dP/dtmax. (max. 50.5% in the paced and 51.4% in the non-paced heart). The effects of substance VUFB 17959 were less marked. On the basis of the results obtained in the present study it is possible to consider the participation of more mechanisms of the action (inc. calcium-channel antagonistic ones) related to negative inotropic effects of the substances. The absence of significant differences in the reaction of dP/dtmax. between the paced and non-paced heart conditions may then indicate a presence of a direct cardiodepressant action of substances VUFB 17951 and 17959.

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两种可能阻断肾上腺素受体和钙通道的物质在家兔体内节律性和非节律性心脏状态下的比较。1 .对心脏收缩力的影响(左心室dP/dtmax)。
在分离制剂中具有钙通道和α -肾上腺素受体阻断活性的物质对心脏收缩力的影响(dP/dtmax)。测量左心室血压的变化。将VUFB 17951(0.046和0.46 mg/kg)和VUFB 17959(0.045和0.45 mg/kg)在戊巴比妥麻醉家兔体内,在心律有节奏和无节奏的情况下静脉注射。VUFB 17951在给药后立即诱导dP/dtmax进行性显著降低,呈剂量依赖性。(max。有搏动心脏50.5%,无搏动心脏51.4%)。VUFB 17959物质的作用不太明显。在本研究结果的基础上,有可能考虑更多的作用机制(包括钙通道拮抗剂)的参与,这些作用机制与物质的负性肌力作用有关。dP/dtmax反应无显著性差异。节律性和非节律性心脏病之间的差异可能表明存在VUFB 17951和17959物质的直接心脏抑制作用。
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