Hof R P
Br J Pharmacol. 1985 May;85(1):75-87. doi: 10.1111/j.1476-5381.1985.tb08833.x.
Investigations into the site of vasodilator and antivasoconstrictor activity of calcium antagonists previously performed in cats were extended to a second species, barbiturate-anaesthetized rabbits, and a second vasoconstrictor agent, vasopressin. The dihydropyridine derivative darodipine (code name PY 108-068; 10, 30 and 100 micrograms kg-1 i.v.) showed systemic haemodynamic effects comparable to those seen in cats at half these doses. Darodipine effected regional vasodilatation (measured with tracer microspheres) in the heart, brain and skeletal muscles as in cats. Only the vessels of the adrenals (dilated in rabbits but not in cats), and the kidneys and skin (constricted in rabbits but not in cats) responded differently to darodipine. Angiotensin II (A II; 0.15 and 1.5 micrograms kg-1 min-1) constricted the same vascular beds in rabbits as in cats, namely the heart, kidneys, small intestine, pancreas, spleen, skin and arterio-venous shunts (inferred from microspheres reaching the lungs), the only exceptions being the vessels of the stomach and liver (constriction only in cats) and the adrenals (constriction only in rabbits). Darodipine (30 and 100 micrograms kg-1) attenuated the A II-induced vasoconstriction in the same vascular beds in rabbits as in cats including the kidneys, which were constricted after administration of the antagonist alone. These results indicate surprisingly small species differences for the vasodilator effects of darodipine as well as the attenuation of the vasoconstrictor effects of A II. Lysine-vasopressin (2 and 50 mu kg-1 min-1) did not increase blood pressure in anaesthetized rabbits but dose-dependently lowered heart rate, cardiac output, total peripheral conductance and myocardial contractile force (measured with a strain gauge). Vasopressin constricted all peripheral vascular beds dose-dependently, except for those of the kidney and liver. The effects of vasopressin persisted in the animals infused with placebo solution. Darodipine (30 and 100 micrograms kg-1), but not verapamil (300 and 1000 micrograms kg-1) reversed the vasopressin-induced cardiac depression and decrease in cardiac output. This probably also explains most of the apparent differences between the effects of the two calcium antagonists on the peripheral circulation. Both calcium antagonists diminished the vasopressin constriction in most vascular beds except those of the spleen, skin and arterio-venous shunts. Most of the effects were dose-related but not strictly competitive, as far as this can be judged based on two doses of agonist and antagonist. 9 As with A II the effects of vasopressin were diminished in vascular beds not normally dilated by calcium antagonists. 10 Calcium antagonists display two typical patterns of activity. The vasodilator pattern consists of dilatation of the vesels of the heart, brain and, to a degree varying with the agents, skeletal muscle. The antivasoconstrictor effects occur in some but not all of the vessels constricted by the constrictor agent, vasoconstriction of the spleen, skin and arterio-venous shunts being resistant to the action of calcium antagonists. The pattern of antivasoconstrictor activity appears to depend on the constrictor compound used, inasmuch as such agents constrict different vascular beds.
先前在猫身上进行的关于钙拮抗剂血管舒张和抗血管收缩活性部位的研究扩展到了第二个物种,即巴比妥麻醉的兔子,以及第二种血管收缩剂,即血管加压素。二氢吡啶衍生物达罗地平(代号PY 108 - 068;静脉注射10、30和100微克/千克)显示出的全身血流动力学效应与在猫身上使用这些剂量一半时所见的效应相当。与在猫身上一样,达罗地平使心脏、大脑和骨骼肌出现局部血管舒张(用示踪微球测量)。只有肾上腺血管(在兔子中扩张但在猫中不扩张)以及肾脏和皮肤血管(在兔子中收缩但在猫中不收缩)对达罗地平的反应不同。血管紧张素II(A II;0.15和1.5微克/千克·分钟)在兔子中使与在猫中相同的血管床收缩,即心脏、肾脏、小肠、胰腺、脾脏、皮肤和动静脉分流(从到达肺部的微球推断),唯一的例外是胃和肝脏血管(仅在猫中收缩)以及肾上腺血管(仅在兔子中收缩)。达罗地平(30和100微克/千克)减弱了A II在兔子中与在猫中相同血管床诱导的血管收缩,包括在单独给予拮抗剂后收缩的肾脏血管。这些结果表明,达罗地平的血管舒张作用以及A II血管收缩作用的减弱,物种差异惊人地小。赖氨酸血管加压素(2和50微克/千克·分钟)在麻醉的兔子中不会升高血压,但会剂量依赖性地降低心率、心输出量、总外周传导率和心肌收缩力(用应变仪测量)。血管加压素剂量依赖性地收缩所有外周血管床,肾脏和肝脏血管除外。血管加压素的作用在输注安慰剂溶液的动物中持续存在。达罗地平(30和100微克/千克),但维拉帕米(300和1000微克/千克)不能逆转血管加压素诱导的心脏抑制和心输出量降低。这可能也解释了两种钙拮抗剂对外周循环作用的大部分明显差异。两种钙拮抗剂在除脾脏、皮肤和动静脉分流血管床之外的大多数血管床中都减弱了血管加压素的收缩作用。就根据两种激动剂和拮抗剂剂量所能判断的情况而言,大多数作用与剂量相关但并非严格竞争性的。9与A II一样,血管加压素在通常不会被钙拮抗剂扩张的血管床中的作用减弱。10钙拮抗剂表现出两种典型的活性模式。血管舒张模式包括心脏、大脑血管以及在一定程度上随药物而异的骨骼肌血管的扩张。抗血管收缩作用发生在一些但并非所有被收缩剂收缩的血管中,脾脏、皮肤和动静脉分流的血管收缩对钙拮抗剂的作用具有抗性。抗血管收缩活性模式似乎取决于所使用的收缩剂化合物,因为这些药物收缩不同的血管床。