Itoh T, Kajiwara M, Kitamura K, Kuriyama H
Br J Pharmacol. 1981 Oct;74(2):455-68. doi: 10.1111/j.1476-5381.1981.tb09991.x.
1 Effects of the vasodilator agents, papaverine, diltiazem, and sodium nitroprusside (SNP) on the electrical and mechanical activities of the smooth muscles of the coronary artery of the pig were compared.2 At a concentration of 10(-5) M, papaverine hyperpolarized and increased the ionic conductance of the membrane, SNP slightly hyperpolarized but diltiazem had no effect on the membrane potential and membrane ionic conductance.3 At a concentration of 10(-5) M, diltiazem abolished the spike evoked by outward current pulses in the presence of tetraethylammonium (TEA) 10 mM, while papaverine and SNP slightly reduced spike amplitude.4 The K-induced contraction produced by any given concentration of K over 20.2 mM was suppressed by diltiazem and SNP dose-dependently in concentrations greater than 10(-6) M; higher concentrations of papaverine were required to suppress contraction.5 The acetylcholine (ACh)-induced contraction was suppressed by diltiazem and SNP at concentrations greater than 10(-6) M and by papaverine in concentrations over 10(-5) M.6 In saponin-treated skinned muscles, papaverine, diltiazem and SNP had no effect on the pCa-tension relationship, i.e. these agents had no effect on the Ca receptor of contractile proteins. Furthermore, the caffeine-induced contraction in skinned muscles (after Ca loading) was not affected by these agents, i.e. the mechanism of Ca release by caffeine in skinned muscles was not affected.7 Chlorpromazine, an agent interacting with calmodulin, antagonized the contractile effect of calcium on skinned muscle fibres.8 The results obtained are discussed in relation to spike and contraction generating mechanisms, i.e. the effects of these agents on Ca influx and Ca release from stored sites. The results indicated that at equimolar concentrations diltiazem suppressed the mechanical response in the coronary artery of the pig more than SNP or papaverine.
比较了血管扩张剂罂粟碱、地尔硫䓬和硝普钠(SNP)对猪冠状动脉平滑肌电活动和机械活动的影响。
在10⁻⁵ M的浓度下,罂粟碱使膜超极化并增加膜的离子电导,SNP轻微使膜超极化,但地尔硫䓬对膜电位和膜离子电导无影响。
在10⁻⁵ M的浓度下,地尔硫䓬在存在10 mM四乙铵(TEA)的情况下消除了外向电流脉冲诱发的峰电位,而罂粟碱和SNP轻微降低峰电位幅度。
浓度超过20.2 mM的任何给定浓度的[K]ₒ诱导的K⁺收缩被地尔硫䓬和SNP以大于10⁻⁶ M的浓度剂量依赖性抑制;需要更高浓度的罂粟碱来抑制收缩。
乙酰胆碱(ACh)诱导的收缩在浓度大于10⁻⁶ M时被地尔硫䓬和SNP抑制,在浓度超过10⁻⁵ M时被罂粟碱抑制。
在皂角苷处理的去皮肌肉中,罂粟碱、地尔硫䓬和SNP对pCa-张力关系无影响,即这些药物对收缩蛋白的Ca²⁺受体无影响。此外,咖啡因诱导的去皮肌肉收缩(在Ca²⁺加载后)不受这些药物影响,即咖啡因在去皮肌肉中释放Ca²⁺的机制不受影响。
氯丙嗪,一种与钙调蛋白相互作用的药物,拮抗钙对去皮肌纤维的收缩作用。
结合峰电位和收缩产生机制,即这些药物对Ca²⁺内流和从储存部位释放Ca²⁺的影响,对所得结果进行了讨论。结果表明,在等摩尔浓度下,地尔硫䓬比SNP或罂粟碱更能抑制猪冠状动脉的机械反应。