Schalekamp M A, Woittiez A J, Wenting G J, van den Meiracker A H, Man in 't Veld A J
J Hypertens Suppl. 1986 Apr;4(1):S7-12.
The haemodynamic effects of ketanserin, a compound with S2-serotonergic receptor and alpha 1-adrenoceptor blocking properties, are reviewed in patients with essential hypertension. The drug has a definite antihypertensive action, both acutely and chronically, and its haemodynamic profile is similar to that of a vasodilator acting on both arterioles and veins but with its main action on arterioles. Its vasodilator action is associated with little reflex cardiostimulation. Pressor responses to i.v. phenylephrine are not altered by therapeutic i.v. doses of ketanserin but pressor responses to methoxamine, a compound that is more specific for vascular alpha 1-receptors than phenylephrine, have been reported to be reduced after chronic oral treatment with ketanserin. However, chronic ketanserin, unlike the alpha 1-adrenoceptor antagonist, prazosin in therapeutic doses, caused no parallel shift of the dose-pressor response curve of methoxamine and the shift was very small compared with prazosin. Studies in patients with autonomic failure and virtually no endogenous alpha 1-adrenergic tone have substantiated that ketanserin is capable of lowering blood pressure independently of alpha 1-adrenoceptor blockade.
对原发性高血压患者中具有5-羟色胺2型（S2）-血清素能受体和α1-肾上腺素能受体阻断特性的化合物酮色林的血流动力学效应进行了综述。该药物在急性和慢性情况下均具有明确的降压作用，其血流动力学特征类似于一种同时作用于小动脉和静脉的血管扩张剂，但主要作用于小动脉。其血管扩张作用几乎没有反射性心脏刺激。静脉注射去氧肾上腺素的升压反应不受治疗剂量静脉注射酮色林的影响，但据报道，在用酮色林进行慢性口服治疗后，对甲氧明（一种比去氧肾上腺素对血管α1-受体更具特异性的化合物）的升压反应有所降低。然而，与治疗剂量的α1-肾上腺素能拮抗剂哌唑嗪不同，慢性使用酮色林并未使甲氧明的剂量-升压反应曲线平行移动，且与哌唑嗪相比，这种移动非常小。对自主神经功能衰竭且几乎没有内源性α1-肾上腺素能张力的患者进行的研究证实，酮色林能够独立于α1-肾上腺素能受体阻断作用来降低血压。
