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异可替丁,一种组胺H1和H2受体的拮抗剂。

Icotidine, an antagonist of histamine at both H1 and H2 receptors.

作者信息

Ganellin C R, Blakemore R C, Brown T H, Cooper D G, Durant G J, Harvey C A, Ife R J, Owen D A, Parsons M E, Rasmussen A C

出版信息

N Engl Reg Allergy Proc. 1986 Mar-Apr;7(2):126-33. doi: 10.2500/108854186779047762.

DOI:10.2500/108854186779047762
PMID:2886901
Abstract

SK&F 93319 (icotidine), 2-[4-(3-methoxypyrid-2-yl)butylamino]-5-[(6-methylpyrid-3-yl )-methyl]- pyrimidin-4-one trihydrochloride, has been identified as a novel agent which combines into one molecule the ability to antagonize the actions of histamine at H1 and H2 receptors across a similar concentration or dose range. The degree of antagonism of vascular responses to histamine exceeds that possible with either an H1- or H2-receptor histamine antagonist alone. SK&F 93319 may have therapeutic utility in conditions requiring simultaneous antagonism of histamine at H1 and H2 receptors.

摘要

SK&F 93319(异可替丁),即2-[4-(3-甲氧基吡啶-2-基)丁基氨基]-5-[(6-甲基吡啶-3-基)甲基]-嘧啶-4-酮三盐酸盐,已被鉴定为一种新型药物,它在相似的浓度或剂量范围内,将组胺H1和H2受体的拮抗作用结合于一个分子中。对组胺血管反应的拮抗程度超过单独使用H1或H2受体组胺拮抗剂所能达到的程度。SK&F 93319在需要同时拮抗组胺H1和H2受体的病症中可能具有治疗作用。

相似文献

1
Icotidine, an antagonist of histamine at both H1 and H2 receptors.异可替丁,一种组胺H1和H2受体的拮抗剂。
N Engl Reg Allergy Proc. 1986 Mar-Apr;7(2):126-33. doi: 10.2500/108854186779047762.
2
Cardiovascular studies with SK&F 93319, an antagonist of histamine at both H1- and H2-receptors.使用SK&F 93319进行的心血管研究,SK&F 93319是一种对H1和H2受体均有拮抗作用的组胺拮抗剂。
Br J Pharmacol. 1984 Oct;83(2):427-32. doi: 10.1111/j.1476-5381.1984.tb16503.x.
3
Evidence for histamine H1 and H2 receptors in guinea-pig oxyntic cells.豚鼠壁细胞中组胺H1和H2受体的证据。
J Pharmacol Exp Ther. 1983 Oct;227(1):115-21.
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Bioisosteric design of conformationally restricted pyridyltriazole histamine H2-receptor antagonists.构象受限的吡啶基三唑组胺H2受体拮抗剂的生物电子等排体设计
J Med Chem. 1983 Jan;26(1):1-6. doi: 10.1021/jm00355a001.
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Electrophysiological actions of histamine and H1-, H2-receptor antagonists in cardiac tissue.组胺及H1、H2受体拮抗剂在心脏组织中的电生理作用。
Agents Actions. 1986 Apr;18(1-2):186-90. doi: 10.1007/BF01988017.
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Synthesis and pharmacology of combined histamine H1-/H2-receptor antagonists containing diphenhydramine and cyproheptadine derivatives.
Arch Pharm (Weinheim). 1996 Feb;329(2):87-94. doi: 10.1002/ardp.19963290206.
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Cardiac and gastric effects of histamine H2 receptor antagonists: no evidence for a correlation between lipophilicity and receptor affinity.组胺H2受体拮抗剂对心脏和胃部的作用:没有证据表明亲脂性与受体亲和力之间存在相关性。
Br J Pharmacol. 1996 Aug;118(7):1813-21. doi: 10.1111/j.1476-5381.1996.tb15608.x.
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Characterization of the histamine receptors in the guinea-pig lung: evidence for relaxant histamine H3 receptors in the trachea.豚鼠肺中组胺受体的特性:气管中存在组胺H3舒张受体的证据。
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Evaluation of the role of Histamine H1- and H2-receptors in cutaneous inflammation in the guinea-pig produced by histamine and mast cell degranulation.组胺H1和H2受体在组胺和肥大细胞脱颗粒引起的豚鼠皮肤炎症中的作用评估。
Br J Pharmacol. 1980 Aug;69(4):615-23. doi: 10.1111/j.1476-5381.1980.tb07912.x.

引用本文的文献

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Correlation between log POCT/H2O and pKB estimates for a series of muscarinic and histamine H2-receptor antagonists.一系列毒蕈碱和组胺H2受体拮抗剂的即时检测(POCT)/水的对数与pKB估计值之间的相关性
Br J Pharmacol. 1988 May;94(1):264-74. doi: 10.1111/j.1476-5381.1988.tb11523.x.