Goldenberg M M
Arzneimittelforschung. 1976;26(3):341-6.
Diclonium bromide (EU-2972; 2-(3,4-dichloroanilino)quinolizinium bromide) was demonstrated to possess an effective, prolonged inhibitory action on contractions in response to stimuli or propulsive movements in the lower bowel of the dog. The compound's antagonism to contractile activity was greater in the distal colon than in the duodenum or upper bowel. Diclonium bromide was a nonselective antispasmodic but, unlike papaverine, caused profound antagonism against smooth muscle contractile responses to intrinsic motor neural excitation. The drug had weak specific anticholinergic action, but its lack of antagonistic effect on other cholinergic responses in this study indicates that the anticholinergic action contributes very little, if at all, to its overall antispasmodic effect. The compound has potential application in the treatment of spastic-colon disease.
溴化二氯尼铵(EU - 2972;2 - (3,4 - 二氯苯胺基)喹嗪鎓溴化物)已被证明对狗下肠道因刺激引起的收缩或推进运动具有有效且持久的抑制作用。该化合物对收缩活动的拮抗作用在远端结肠比在十二指肠或上肠道更强。溴化二氯尼铵是一种非选择性抗痉挛药,但与罂粟碱不同,它对平滑肌对内在运动神经兴奋的收缩反应有显著拮抗作用。该药具有较弱的特异性抗胆碱能作用,但在本研究中其对其他胆碱能反应缺乏拮抗作用表明,抗胆碱能作用即便有贡献,对其总体抗痉挛作用的贡献也非常小。该化合物在治疗痉挛性结肠疾病方面具有潜在应用价值。