一种新型强效选择性组胺H3受体激动剂，4-（1H-咪唑-4-基甲基）哌啶。 - Suppr

A new potent and selective histamine H3 receptor agonist, 4-(1H-imidazol-4-ylmethyl)piperidine.

作者信息

Vollinga R C, de Koning J P, Jansen F P, Leurs R, Menge W M, Timmerman H

机构信息

Leiden/Amsterdam Center for Drug Research, Department of Pharmacochemistry, Vrije Universiteit Amsterdam, The Netherlands.

出版信息

J Med Chem. 1994 Feb 4;37(3):332-3. doi: 10.1021/jm00029a002.

DOI:10.1021/jm00029a002

PMID:8308858

Abstract

摘要

相似文献

A new potent and selective histamine H3 receptor agonist, 4-(1H-imidazol-4-ylmethyl)piperidine.一种新型强效选择性组胺H3受体激动剂，4-（1H-咪唑-4-基甲基）哌啶。

J Med Chem. 1994 Feb 4;37(3):332-3. doi: 10.1021/jm00029a002.

Identification of 4-(1H-imidazol-4(5)-ylmethyl)pyridine (immethridine) as a novel, potent, and highly selective histamine H(3) receptor agonist.鉴定4-（1H-咪唑-4（5）-基甲基）吡啶（伊美替啶）为一种新型、强效且高度选择性的组胺H(3)受体激动剂。

J Med Chem. 2004 May 6;47(10):2414-7. doi: 10.1021/jm049932u.

N-substituted piperidinyl alkyl imidazoles: discovery of methimepip as a potent and selective histamine H3 receptor agonist.N-取代哌啶基烷基咪唑类：作为一种强效且选择性组胺H3受体激动剂的美替美吡的发现。

J Med Chem. 2005 Mar 24;48(6):2100-7. doi: 10.1021/jm049475h.

Investigation of the histamine H3 receptor binding site. Design and synthesis of hybrid agonists with a lipophilic side chain.组胺 H3 受体结合部位的研究。具有亲脂侧链的混合激动剂的设计与合成。

J Med Chem. 2010 Sep 9;53(17):6445-56. doi: 10.1021/jm100643t.

Synthesis and in vitro pharmacology of a series of new chiral histamine H3-receptor ligands: 2-(R and S)-Amino-3-(1H-imidazol-4(5)-yl)propyl ether derivatives.一系列新型手性组胺H3受体配体的合成及体外药理学研究：2-(R和S)-氨基-3-(1H-咪唑-4(5)-基)丙基醚衍生物

J Med Chem. 1999 Apr 8;42(7):1193-202. doi: 10.1021/jm980408v.

Synthesis and structure-activity relationships of conformationally constrained histamine H(3) receptor agonists.构象受限组胺H(3)受体激动剂的合成及构效关系

J Med Chem. 2003 Dec 4;46(25):5445-57. doi: 10.1021/jm030905y.

Reduction of CYP450 inhibition in the 4-[(1H-imidazol-4-yl)methyl]piperidine series of histamine H3 receptor antagonists.组胺H3受体拮抗剂的4-[(1H-咪唑-4-基)甲基]哌啶系列中CYP450抑制作用的降低

Bioorg Med Chem Lett. 2006 Feb 15;16(4):989-94. doi: 10.1016/j.bmcl.2005.10.087. Epub 2005 Nov 15.

Cyclopropane-based conformational restriction of histamine. (1S,2S)-2-(2-aminoethyl)-1-(1H-imidazol-4-yl)cyclopropane, a highly selective agonist for the histamine H3 receptor, having a cis-cyclopropane structure.基于环丙烷的组胺构象限制。（1S，2S）-2-（2-氨基乙基）-1-（1H-咪唑-4-基）环丙烷，一种组胺H3受体的高选择性激动剂，具有顺式环丙烷结构。

J Med Chem. 2003 May 8;46(10):1980-8. doi: 10.1021/jm020415q.

Novel histamine H3 receptor antagonists based on the 4-[(1H-imidazol-4-yl)methyl]piperidine scaffold.基于4-[(1H-咪唑-4-基)甲基]哌啶骨架的新型组胺H3受体拮抗剂。

Bioorg Med Chem Lett. 2006 Jan 15;16(2):395-9. doi: 10.1016/j.bmcl.2005.09.076. Epub 2005 Oct 21.

Synthesis and structure-activity relationships of N-aryl-piperidine derivatives as potent (partial) agonists for human histamine H3 receptor.合成及 N-芳基哌啶衍生物的构效关系作为人组氨酸 H3 受体的有效（部分）激动剂。

Bioorg Med Chem. 2010 Jul 15;18(14):5441-8. doi: 10.1016/j.bmc.2010.04.052. Epub 2010 Apr 21.

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Synthesis and Pharmacological Characterization of New Photocaged Agonists for Histamine H and H Receptors.组胺H1和H2受体新型光笼激动剂的合成与药理学特性研究

Pharmaceuticals (Basel). 2024 Apr 21;17(4):536. doi: 10.3390/ph17040536.

Influence of the Novel Histamine H3 Receptor Antagonist/Inverse Agonist M39 on Gastroprotection and PGE2 Production Induced by ()-Alpha-Methylhistamine in C57BL/6 Mice.新型组胺H3受体拮抗剂/反向激动剂M39对（）-α-甲基组胺诱导的C57BL/6小鼠胃保护作用及前列腺素E2生成的影响

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Bioluminescence Resonance Energy Transfer Based G Protein-Activation Assay to Probe Duration of Antagonism at the Histamine H Receptor.基于生物发光共振能量转移的 G 蛋白激活测定法探究组胺 H 受体拮抗剂的作用持续时间。

Int J Mol Sci. 2019 Jul 30;20(15):3724. doi: 10.3390/ijms20153724.

International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors.国际基础与临床药理学联合会。XCVIII.组胺受体。

Pharmacol Rev. 2015 Jul;67(3):601-55. doi: 10.1124/pr.114.010249.

Interaction Between Brain Histamine and Serotonin, Norepinephrine, and Dopamine Systems: In Vivo Microdialysis and Electrophysiology Study.脑组胺与血清素、去甲肾上腺素和多巴胺系统之间的相互作用：体内微透析和电生理学研究

J Mol Neurosci. 2015 Jun;56(2):320-8. doi: 10.1007/s12031-015-0536-3. Epub 2015 Mar 29.

Identification and characterization of ZEL-H16 as a novel agonist of the histamine H3 receptor.鉴定并表征 ZEL-H16 为组胺 H3 受体的新型激动剂。

PLoS One. 2012;7(8):e42185. doi: 10.1371/journal.pone.0042185. Epub 2012 Aug 1.

H3 receptors and pain modulation: peripheral, spinal, and brain interactions.H3 受体与疼痛调制：外周、脊髓和脑内相互作用。

J Pharmacol Exp Ther. 2011 Jan;336(1):30-7. doi: 10.1124/jpet.110.171264. Epub 2010 Sep 23.

Activation of peripheral and spinal histamine H3 receptors inhibits formalin-induced inflammation and nociception, respectively.外周和脊髓组胺H3受体的激活分别抑制福尔马林诱导的炎症和伤害感受。

Pharmacol Biochem Behav. 2007 Nov;88(1):122-9. doi: 10.1016/j.pbb.2007.07.014. Epub 2007 Jul 25.

Inhibition of cortical acetylcholine release and cognitive performance by histamine H3 receptor activation in rats.组胺H3受体激活对大鼠皮质乙酰胆碱释放及认知能力的抑制作用。

Br J Pharmacol. 1996 Dec;119(8):1656-64. doi: 10.1111/j.1476-5381.1996.tb16086.x.

Evaluation of the receptor selectivity of the H3 receptor antagonists, iodophenpropit and thioperamide: an interaction with the 5-HT3 receptor revealed.H3受体拮抗剂碘苯丙胺和硫代哌酰胺的受体选择性评估：揭示了与5-HT3受体的相互作用。

Br J Pharmacol. 1995 Oct;116(4):2315-21. doi: 10.1111/j.1476-5381.1995.tb15071.x.

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A new potent and selective histamine H3 receptor agonist, 4-(1H-imidazol-4-ylmethyl)piperidine.

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