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中枢神经系统中的组胺受体。

Histamine receptors in the central nervous system.

作者信息

Timmerman H

机构信息

Department of Pharmacochemistry, Faculty of Chemistry, Free University, Amsterdam, The Netherlands.

出版信息

Pharm Weekbl Sci. 1989 Oct 20;11(5):146-50. doi: 10.1007/BF01959461.

DOI:10.1007/BF01959461
PMID:2687795
Abstract

The role of histamine in brain function is discussed. A brief review is presented on the three types of histamine receptors with regard to their biochemistry and functions, as well as on specific ligands, both agonists and antagonists. It is concluded that several aspects of the pharmacology of histamine in the central nervous system are still a matter of empirism and speculations. The recent publications on the brain-penetrating H2 antagonist zolantidine and the selective H3 agonists and antagonists are expected to contribute to the knowledge of the histaminergic pathways in the brain. Therapeutical areas within the central nervous system are related to behaviour (including wake-sleep), neuroendocrinal processes, the control of muscle activity and cerebral circulation.

摘要

本文讨论了组胺在脑功能中的作用。简要回顾了三种组胺受体的生物化学和功能,以及特定的配体,包括激动剂和拮抗剂。得出的结论是,组胺在中枢神经系统中的药理学的几个方面仍然是经验主义和推测的问题。关于脑穿透性H2拮抗剂佐兰替丁以及选择性H3激动剂和拮抗剂的最新出版物有望增进对脑中组胺能途径的了解。中枢神经系统内的治疗领域与行为(包括觉醒-睡眠)、神经内分泌过程、肌肉活动控制和脑循环有关。

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1
Histamine receptors in the central nervous system.中枢神经系统中的组胺受体。
Pharm Weekbl Sci. 1989 Oct 20;11(5):146-50. doi: 10.1007/BF01959461.
2
Autoradiographic localization of binding sites for [3H]histamine and H1- and H2-antagonists on cultured neurones and glial cells.[3H]组胺以及H1和H2拮抗剂在培养的神经元和神经胶质细胞上结合位点的放射自显影定位。
Neuroscience. 1984 Nov;13(3):863-70. doi: 10.1016/0306-4522(84)90101-5.
3
Characterization and distribution of histamine H1- and H2-receptors in precapillary vessels.组胺H1和H2受体在毛细血管前血管中的特征与分布
J Cardiovasc Pharmacol. 1984;6 Suppl 4:S587-97. doi: 10.1097/00005344-198406004-00005.
4
Histamine receptors in the brain.
N Engl Reg Allergy Proc. 1985 Spring;6(2):195-200. doi: 10.2500/108854185779045233.
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Current Knowledge and Perspectives on Histamine H1 and H2 Receptor Pharmacology: Functional Selectivity, Receptor Crosstalk, and Repositioning of Classic Histaminergic Ligands.组胺H1和H2受体药理学的当前知识与展望:功能选择性、受体相互作用以及经典组胺能配体的重新定位
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Histamine receptors in the human ureter.人类输尿管中的组胺受体。
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Molecular pharmacological aspects of histamine receptors.组胺受体的分子药理学方面
Pharmacol Ther. 1995 Jun;66(3):413-63. doi: 10.1016/0163-7258(95)00006-3.
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Histamine H1- and H2-receptors are differentially and spatially distributed in cerebral vessels.组胺H1和H2受体在脑血管中呈差异分布且具有空间特异性。
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Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist.人组胺H4受体上组胺H1、H2和H3受体配体的评估:4-甲基组胺作为首个强效且选择性H4受体激动剂的鉴定。
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Central H1- and H2-histaminergic stimulation of pituitary-adrenocortical response under stress in rats.大鼠应激状态下垂体 - 肾上腺皮质反应的中枢H1和H2组胺能刺激
Neuroendocrinology. 1983 Jun;36(6):424-30. doi: 10.1159/000123493.

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Nanodelivery of Histamine H3/H4 Receptor Modulators BF-2649 and Clobenpropit with Antibodies to Amyloid Beta Peptide in Combination with Alpha Synuclein Reduces Brain Pathology in Parkinson's Disease.纳米递药:组胺 H3/H4 受体调节剂 BF-2649 和 Clobenpropit 与针对淀粉样 β 肽的抗体以及 α 突触核蛋白联合应用可减轻帕金森病的脑病理学改变。
Adv Neurobiol. 2023;32:55-96. doi: 10.1007/978-3-031-32997-5_2.
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Striatal cholinergic interneuron regulation and circuit effects.纹状体胆碱能中间神经元调节与回路效应。
Front Synaptic Neurosci. 2014 Oct 21;6:22. doi: 10.3389/fnsyn.2014.00022. eCollection 2014.
3
Histamine in the regulation of wakefulness.

本文引用的文献

1
Distribution of the histaminergic neuron system in the central nervous system of rats; a fluorescent immunohistochemical analysis with histidine decarboxylase as a marker.大鼠中枢神经系统中组胺能神经元系统的分布;以组氨酸脱羧酶为标记物的荧光免疫组织化学分析
Brain Res. 1984 Mar 12;295(1):13-25. doi: 10.1016/0006-8993(84)90811-4.
2
A theoretical investigation of histamine tautomerism.
J Med Chem. 1984 Nov;27(11):1531-4. doi: 10.1021/jm00377a023.
3
Auto-inhibition of brain histamine release mediated by a novel class (H3) of histamine receptor.由一类新型组胺受体(H3)介导的脑组胺释放的自身抑制作用。
组胺在觉醒调节中的作用。
Sleep Med Rev. 2011 Feb;15(1):65-74. doi: 10.1016/j.smrv.2010.06.004. Epub 2010 Sep 20.
Nature. 1983 Apr 28;302(5911):832-7. doi: 10.1038/302832a0.
4
Effects of antidepressant drugs on histamine-H1 receptors in the brain.抗抑郁药物对大脑中组胺-H1受体的影响。
Life Sci. 1984 Feb 6;34(6):597-605. doi: 10.1016/0024-3205(84)90494-6.
5
Histamine H2-binding on guinea pig cerebral cortex.
Agents Actions. 1986 Apr;18(1-2):231-4. doi: 10.1007/BF01988028.
6
The histaminergic system in the guinea pig central nervous system: an immunocytochemical mapping study using an antiserum against histamine.豚鼠中枢神经系统中的组胺能系统:一项使用抗组胺血清的免疫细胞化学定位研究。
J Comp Neurol. 1988 Jul 8;273(2):163-86. doi: 10.1002/cne.902730204.
7
Polyclonal and monoclonal antibodies directed against SK & F 94461, a specific H1 histamine receptor ligand.
Mol Pharmacol. 1988 Aug;34(2):136-44.
8
Characterization of histamine H1-receptor binding peptides in guinea pig brain using [125I]iodoazidophenpyramine, an irreversible specific photoaffinity probe.
Proc Natl Acad Sci U S A. 1988 Apr;85(8):2743-7. doi: 10.1073/pnas.85.8.2743.
9
Centrally applied histamine increases gastric acid secretion in rats.中枢给予组胺可增加大鼠胃酸分泌。
Naunyn Schmiedebergs Arch Pharmacol. 1988 Jul;338(1):96-8. doi: 10.1007/BF00168818.
10
A detailed mapping of histamine H1-receptors in guinea-pig central nervous system established by autoradiography with [125I]iodobolpyramine.通过使用[125I]碘博来胺放射自显影法建立的豚鼠中枢神经系统中组胺H1受体的详细图谱。
Neuroscience. 1988 Aug;26(2):553-600. doi: 10.1016/0306-4522(88)90167-4.