Setnikar I, Cereda R, Pacini M A, Revel L, Makovec F
Rotta Research Laboratorium S.p.A., Monza.
Arzneimittelforschung. 1989 Sep;39(9):1114-9.
(+/-) Tiropramide hydrochloride, its D and L optical isomers and some of its metabolites were characterized in a number of in vitro pharmacological tests. Tiropramide showed broad spectrum antispasmodic activities on the isolated stomach of guinea pig electrically stimulated; on the longitudinal muscles of the ileum of guinea pig stimulated by electrical impulses, BaCl2, acetylcholine, histamine, serotonin, substance P and cholecystokinin octapeptide (CCK-8); on the spontaneous contractions and on the electrical inhibition of the jejunum of rabbit; on the spontaneous contractions and on the contractions provoked by BaCl2 and acetylcholine of the ascending colon of the rat; on the contractions provoked by BaCl2, acetylcholine, histamine and cerulein of the circular muscles of the gall bladder of the guinea pig; on the spontaneous contractions of the pyel-ureter preparation of the guinea pig; on the contractions of the uterus of the rat provoked by oxitocin, serotonin, acetylcholine, PGF2; on the spontaneous contraction of the portal vein of the rat; on the constriction of the tail artery of the rat provoked by electrical stimulation, epinephrine and ergotamine; on the contractions of the aortic strip of the rabbit stimulated by norepinephrine; on the contractions of the strip of bovine coronary artery depolarized by HCl. In general tiropramide had antispasmodic effect at 5-60 mumol/l concentration. It was more potent than papaverine on contractions provoked by electrical or chemical stimuli, and was less potent or ineffective on spontaneous and "physiological" contractions of the different smooth muscle preparations. Tiropramide had small effects on vascular smooth muscles and showed very small calcium channel blocking activity.
（±）盐酸替罗哌胺及其D型和L型光学异构体以及一些代谢产物在多项体外药理学试验中得到了表征。替罗哌胺在多种实验中表现出广泛的抗痉挛活性：对电刺激的豚鼠离体胃；对电脉冲、氯化钡、乙酰胆碱、组胺、5-羟色胺、P物质和八肽胆囊收缩素（CCK-8）刺激的豚鼠回肠纵肌；对兔空肠的自发收缩和电抑制；对大鼠升结肠的自发收缩以及由氯化钡和乙酰胆碱引起的收缩；对豚鼠胆囊环行肌由氯化钡、乙酰胆碱、组胺和蛙皮素引起的收缩；对豚鼠肾盂-输尿管标本的自发收缩；对大鼠子宫由催产素、5-羟色胺、乙酰胆碱、前列腺素F2引起的收缩；对大鼠门静脉的自发收缩；对大鼠尾动脉由电刺激、肾上腺素和麦角胺引起的收缩；对去甲肾上腺素刺激的兔主动脉条收缩；对盐酸去极化的牛冠状动脉条收缩。一般来说，替罗哌胺在5 - 60μmol/L浓度时具有抗痉挛作用。在电刺激或化学刺激引起的收缩方面，它比罂粟碱更有效，而对不同平滑肌标本的自发和“生理性”收缩作用较弱或无效。替罗哌胺对血管平滑肌作用较小，且显示出非常小的钙通道阻滞活性。
