一些带有11-乙酰基-5,11-二氢-6H-吡啶并[2,3-b][1,4]-苯并二氮杂卓-6-酮部分作为抗毒蕈碱剂的甲氧卡明相关四胺的合成及生物活性：第二代高选择性M2毒蕈碱受体拮抗剂 - Suppr

Suppr

超能文献

Synthesis and biological activity of some methoctramine-related tetraamines bearing a 11-acetyl-5,11-dihydro-6H-pyrido[2,3-b][1,4]-benzodiazepin-6-one moiety as antimuscarinics: a second generation of highly selective M2 muscarinic receptor antagonists.

作者信息

Melchiorre C, Bolognesi M L, Chiarini A, Minarini A, Spampinato S

机构信息

Department of Pharmaceutical Sciences, University of Bologna, Italy.

出版信息

J Med Chem. 1993 Nov 12;36(23):3734-7. doi: 10.1021/jm00075a032.

DOI:10.1021/jm00075a032

PMID:8246244

Abstract

摘要

相似文献

Synthesis and biological activity of some methoctramine-related tetraamines bearing a 11-acetyl-5,11-dihydro-6H-pyrido[2,3-b][1,4]-benzodiazepin-6-one moiety as antimuscarinics: a second generation of highly selective M2 muscarinic receptor antagonists.一些带有11-乙酰基-5,11-二氢-6H-吡啶并[2,3-b][1,4]-苯并二氮杂卓-6-酮部分作为抗毒蕈碱剂的甲氧卡明相关四胺的合成及生物活性：第二代高选择性M2毒蕈碱受体拮抗剂

J Med Chem. 1993 Nov 12;36(23):3734-7. doi: 10.1021/jm00075a032.

Design, synthesis, and biological activity of methoctramine-related tetraamines bearing an 11-acetyl-5,11-dihydro-6H-pyrido[2,3-b][1,4] benzodiazepin-6-one moiety: structural requirements for optimum occupancy of muscarinic receptor subtypes as revealed by symmetrical and unsymmetrical polyamines.带有11-乙酰基-5,11-二氢-6H-吡啶并[2,3-b][1,4]苯并二氮杂䓬-6-酮部分的甲氧卡明相关四胺的设计、合成及生物活性：对称和不对称多胺揭示的毒蕈碱受体亚型最佳占据的结构要求

J Med Chem. 1994 Sep 30;37(20):3363-72. doi: 10.1021/jm00046a021.

The design of novel methoctramine-related tetraamines as muscarinic receptor subtype selective antagonists.新型甲氧胺相关四胺类作为毒蕈碱受体亚型选择性拮抗剂的设计。

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Synthesis of novel succinamide derivatives having the 5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one skeleton as potent and selective M2 muscarinic receptor antagonists. I.具有5,11-二氢-6H-吡啶并[2,3-b][1,4]苯并二氮杂卓-6-酮骨架的新型琥珀酰胺衍生物作为强效和选择性M2毒蕈碱受体拮抗剂的合成。I.

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Selective blockade of muscarinic M2 receptors in vivo by the new antagonist tripitramine.新型拮抗剂曲匹拉明对体内毒蕈碱M2受体的选择性阻断作用。

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Methoctramine-related polymethylene tetraamines. 4. Chirality effect on M2 muscarinic receptor blocking activity.与甲辛胺相关的聚亚甲基四胺。4. 手性对M2毒蕈碱受体阻断活性的影响。

Farmaco. 1991 Jul-Aug;46(7-8):861-72.

Further investigation on methoctramine-related tetraamines: effects of terminal N-substitution and of chain length separating the four nitrogens on M2 muscarinic receptor blocking activity.关于美索曲明相关四胺的进一步研究：末端N-取代以及分隔四个氮原子的链长对M2毒蕈碱受体阻断活性的影响。

Farmaco. 1991 Oct;46(10):1167-78.

Structure-activity relationships among methoctramine-related polymethylene tetraamines. 3. Effect of the four nitrogens on M2 muscarinic blocking activity as revealed by symmetrical and unsymmetrical polyamines.甲辛胺相关的聚亚甲基四胺的构效关系。3. 对称和不对称多胺揭示的四个氮原子对M2毒蕈碱阻断活性的影响。

Farmaco. 1991 Mar;46(3):417-34.

Universal template approach to drug design: polyamines as selective muscarinic receptor antagonists.药物设计的通用模板方法：多胺作为选择性毒蕈碱受体拮抗剂

J Med Chem. 1998 Oct 8;41(21):4150-60. doi: 10.1021/jm981038d.

Prejunctional muscarinic receptors on cholinergic nerves in guinea pig airways are of the M2 subtype.

Eur J Pharmacol. 1991 Jan 25;193(1):117-9. doi: 10.1016/0014-2999(91)90209-9.

引用本文的文献

Evidence for cross-talk between M2 and M3 muscarinic acetylcholine receptors in the regulation of second messenger and extracellular signal-regulated kinase signalling pathways in Chinese hamster ovary cells.中国仓鼠卵巢细胞中M2和M3毒蕈碱型乙酰胆碱受体在调节第二信使和细胞外信号调节激酶信号通路中的相互作用证据。

Br J Pharmacol. 2003 Apr;138(7):1340-50. doi: 10.1038/sj.bjp.0705178.

Analysis of the muscarinic receptor subtype mediating inhibition of the neurogenic contractions in rabbit isolated vas deferens by a series of polymethylene tetra-amines.一系列聚亚甲基四胺对兔离体输精管神经源性收缩抑制作用的毒蕈碱受体亚型分析

Br J Pharmacol. 2001 Mar;132(5):1009-16. doi: 10.1038/sj.bjp.0703891.

Selective blockade of muscarinic M2 receptors in vivo by the new antagonist tripitramine.新型拮抗剂曲匹拉明对体内毒蕈碱M2受体的选择性阻断作用。

Naunyn Schmiedebergs Arch Pharmacol. 1995 Sep;352(3):304-7. doi: 10.1007/BF00168561.

Characterization of the interaction between muscarinic M2 receptors and beta-adrenoceptor subtypes in guinea-pig isolated ileum.豚鼠离体回肠中M2毒蕈碱受体与β-肾上腺素能受体亚型之间相互作用的表征

Br J Pharmacol. 1995 Jan;114(1):49-56. doi: 10.1111/j.1476-5381.1995.tb14904.x.

In vitro characterization of tripitramine, a polymethylene tetraamine displaying high selectivity and affinity for muscarinic M2 receptors.曲匹拉明的体外特性研究，曲匹拉明是一种对毒蕈碱M2受体具有高选择性和亲和力的聚亚甲基四胺。

Br J Pharmacol. 1995 Apr;114(7):1507-17. doi: 10.1111/j.1476-5381.1995.tb13378.x.

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