Giannella E, Masini E, Palmerani B, Pistelli A, Mannaioni P F
Department of Preclinical and Clinical Pharmacology M. Aiazzi Mancini, Florence University, Italy.
Agents Actions. 1988 Apr;23(3-4):185-7. doi: 10.1007/BF02142535.
Calcium antagonists have been reported to exert protective effects in hypersensitivity reactions in man and animals. However, their effect on anaphylactic histamine release is highly variable and controversial. In the present paper we evaluate the effect of calcium entry blockers and BAY K 8644 on the response to specific antigen in isolated hearts taken from actively sensitized guinea-pigs and from isolated rat and guinea-pig mast cells, actively or passively sensitized. Verapamil, diltiazem, nifedipine and prenylamine dose-dependently decreased anaphylactic histamine release in isolated actively sensitized guinea-pig mast cells. BAY K 8644 was found to be ineffective. In isolated, passively sensitized rat mast cells, verapamil showed a highly significant inhibitory effect, while prenylamine (10(-4) M) was able to evoke a histamine releasing effect. In cardiac anaphylaxis verapamil, diltiazem, prenylamine, but not nifedipine, were active in reducing the release of histamine without modifying the antigen-induced arrhythmias and positive chronotropic and inotropic effects.
据报道,钙拮抗剂对人和动物的过敏反应具有保护作用。然而,它们对过敏性组胺释放的影响差异很大且存在争议。在本文中,我们评估了钙通道阻滞剂和BAY K 8644对从主动致敏豚鼠分离的离体心脏以及从主动或被动致敏的离体大鼠和豚鼠肥大细胞对特异性抗原反应的影响。维拉帕米、地尔硫䓬、硝苯地平和普尼拉明剂量依赖性地降低了离体主动致敏豚鼠肥大细胞中过敏性组胺的释放。发现BAY K 8644无效。在离体被动致敏大鼠肥大细胞中,维拉帕米显示出高度显著的抑制作用,而普尼拉明(10⁻⁴ M)能够引发组胺释放效应。在心脏过敏反应中,维拉帕米、地尔硫䓬、普尼拉明(而非硝苯地平)在减少组胺释放方面具有活性,同时不改变抗原诱导的心律失常以及正性变时和变力作用。