Bemis K, Bendele A, Clemens J, Deldar A, Gidda J, Hamelink J, Holland D, Lamishaw B, McGrath J, Shannon H
Lilly Research Laboratories, Indianapolis, IN.
Arzneimittelforschung. 1989 Feb;39(2):240-50.
Nizatidine (N-[2-[[[2-[(dimethylamino)methyl-4-thiazolyl]- methyl]thio]ethyl]-N'-methyl-2-nitro-1,1-ethenediamine, LY139037, Axid) is a novel, potent, and selective H2-antagonist. The potential secondary pharmacologic effects of this agent on the cardiovascular, respiratory, gastrointestinal, renal, hepatic, autonomic, and central nervous systems as well as effects on circulating blood glucose and the acute inflammatory response were examined. Nizatidine was generally inactive in the tests conducted in mice, rats, guinea pigs, rabbits, and dogs. Nizatidine and the reference H2-antagonist, cimetidine, both produced effects upon the cardiovascular and respiratory systems by intravenous administration in anesthetized dogs at doses in excess of the intended clinical exposure. In summary, these studies confirm the selective pharmacologic activity of nizatidine and indicate a low potential for secondary pharmacologic side effects to be encountered clinically.
尼扎替丁(N-[2-[[[2-[(二甲氨基)甲基]-4-噻唑基]甲基]硫代]乙基]-N'-甲基-2-硝基-1,1-乙烯二胺,LY139037,爱希)是一种新型、强效且具选择性的H2拮抗剂。研究了该药物对心血管、呼吸、胃肠、肾脏、肝脏、自主神经和中枢神经系统的潜在次要药理作用,以及对循环血糖和急性炎症反应的影响。在小鼠、大鼠、豚鼠、兔子和狗身上进行的试验中,尼扎替丁通常无活性。尼扎替丁和参比H2拮抗剂西咪替丁,在麻醉犬身上静脉给药,剂量超过预期临床暴露量时,均对心血管和呼吸系统产生影响。总之,这些研究证实了尼扎替丁的选择性药理活性,并表明临床上出现次要药理副作用的可能性较低。