用[3H]美吡拉敏在哺乳动物脑膜中鉴定出组胺H1受体。
Histamine H1 receptors identified in mammalian brain membranes with [3H]mepyramine.
作者信息
Tran V T, Chang R S, Snyder S H
出版信息
Proc Natl Acad Sci U S A. 1978 Dec;75(12):6290-4. doi: 10.1073/pnas.75.12.6290.
Abstract
The antihistamine [3H]mepyramine binds to H1 histamine receptors in mammalian brain membranes. Potencies of H1 antihistamines at the binding sites correlate with their pharmacological antihistamine effects in the guinea pig ileum. Specific [3H]mepyramine binding is saturable with a dissociation constant of about 4 nM in both equilibrium and kinetic experiments and a density of 10 pmol per gram of whole kinetic experiments and a density of 10 pmol per gram of whole brain. Some tricyclic antidepressants are potent inhibitors of specific [3H]mepyramine binding. Regional variations of [3H]mepyramine binding do not correlate with variations in endogeneous histamine and histidine decarboxylase activity.
摘要
抗组胺药[3H]美吡拉敏可与哺乳动物脑膜中的H1组胺受体结合。H1抗组胺药在结合位点的效力与其在豚鼠回肠中的药理抗组胺作用相关。在平衡实验和动力学实验中，特异性[3H]美吡拉敏结合均具有饱和性，解离常数约为4 nM，每克全脑的密度为10 pmol。一些三环类抗抑郁药是特异性[3H]美吡拉敏结合的强效抑制剂。[3H]美吡拉敏结合的区域差异与内源性组胺和组胺脱羧酶活性的差异无关。
相似文献
1
Histamine H1 receptors identified in mammalian brain membranes with [3H]mepyramine.用[3H]美吡拉敏在哺乳动物脑膜中鉴定出组胺H1受体。
Proc Natl Acad Sci U S A. 1978 Dec;75(12):6290-4. doi: 10.1073/pnas.75.12.6290.
2
[3H]mepyramine binding to histamine H1 receptors in bovine retina.[3H]美吡拉敏与牛视网膜中组胺H1受体的结合
Biochem Biophys Res Commun. 1986 Mar 13;135(2):445-50. doi: 10.1016/0006-291x(86)90014-8.
3
Affinities of histamine H1-antagonists in guinea pig brain: similarity of values determined from [3H]mepyramine binding and from inhibition of a functional response.组胺H1拮抗剂在豚鼠脑中的亲和力：由[3H]美吡拉敏结合及功能反应抑制所测定值的相似性
J Neurochem. 1981 Nov;37(5):1357-60. doi: 10.1111/j.1471-4159.1981.tb04692.x.
4
Histamine H1-receptor in the retina: species differences.
Biochem Biophys Res Commun. 1988 Jan 15;150(1):316-22. doi: 10.1016/0006-291x(88)90522-0.
5
Histamine H1-receptors labeled in vivo: antidepressant and antihistamine interactions.体内标记的组胺H1受体：抗抑郁药与抗组胺药的相互作用
Eur J Pharmacol. 1980 Jun 13;64(2-3):177-81. doi: 10.1016/0014-2999(80)90043-6.
6
Histamine H1-receptors in the guinea-pig urinary bladder.豚鼠膀胱中的组胺H1受体
Eur J Pharmacol. 1985 Aug 7;114(1):89-92. doi: 10.1016/0014-2999(85)90526-6.
7
Specific binding of [3H]mepyramine to histamine H1-receptors in vascular smooth muscle membranes.[3H] 美吡拉敏与血管平滑肌膜中组胺H1受体的特异性结合。
Agents Actions. 1983 Apr;13(2-3):162-6. doi: 10.1007/BF01967322.
8
Characteristics of histamine H1-receptors in peripheral tissues labeled with [3H]mepyramine.
J Pharmacol Exp Ther. 1979 Jun;209(3):437-42.
9
The binding of doxepin to histamine H1-receptors in guinea-pig and rat brain.多塞平与豚鼠和大鼠脑中组胺H1受体的结合。
Br J Pharmacol. 1985 Feb;84(2):417-24. doi: 10.1111/j.1476-5381.1985.tb12925.x.
10
Histamine H1-receptors in the brain of the guinea-pig and the rat: differences in ligand binding properties and regional distribution.豚鼠和大鼠脑中的组胺H1受体：配体结合特性和区域分布的差异。
Br J Pharmacol. 1980 Apr;68(4):687-96. doi: 10.1111/j.1476-5381.1980.tb10861.x.
引用本文的文献
1
Acupuncture and Neural Mechanism in the Management of Low Back Pain-An Update.针灸与下腰痛管理中的神经机制——最新进展
Medicines (Basel). 2018 Jun 25;5(3):63. doi: 10.3390/medicines5030063.
2
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.
3
Monoamine reuptake inhibitors in Parkinson's disease.单胺再摄取抑制剂在帕金森病中的应用。
Parkinsons Dis. 2015;2015:609428. doi: 10.1155/2015/609428. Epub 2015 Feb 25.
4
Involvement of sigma-1 receptors in the antidepressant-like effects of dextromethorphan.σ-1受体参与右美沙芬的抗抑郁样作用。
PLoS One. 2014 Feb 28;9(2):e89985. doi: 10.1371/journal.pone.0089985. eCollection 2014.
5
Polymorphism of human cytochrome P450 2D6 and its clinical significance: part II.人细胞色素 P450 2D6 的多态性及其临床意义：第二部分。
Clin Pharmacokinet. 2009;48(12):761-804. doi: 10.2165/11318070-000000000-00000.
6
Differential effects of acute and repeat dosing with the H3 antagonist GSK189254 on the sleep-wake cycle and narcoleptic episodes in Ox-/- mice.H3拮抗剂GSK189254急性给药和重复给药对Ox-/-小鼠睡眠-觉醒周期及发作性睡病发作的不同影响。
Br J Pharmacol. 2009 May;157(1):104-17. doi: 10.1111/j.1476-5381.2009.00205.x.
7
Relationship between sedation and pupillary function: comparison of diazepam and diphenhydramine.镇静与瞳孔功能之间的关系：地西泮与苯海拉明的比较
Br J Clin Pharmacol. 2006 Jun;61(6):752-60. doi: 10.1111/j.1365-2125.2006.02632.x.
8
Comparative structure-activity relationships of benztropine analogues at the dopamine transporter and histamine H(1) receptors.苯海索类似物在多巴胺转运体和组胺H(1)受体上的比较构效关系。
Bioorg Med Chem. 2006 Jun 1;14(11):3625-34. doi: 10.1016/j.bmc.2006.01.017. Epub 2006 Feb 3.
9
The roles of CYP2D6 and stereoselectivity in the clinical pharmacokinetics of chlorpheniramine.CYP2D6的作用及立体选择性在氯苯那敏临床药代动力学中的表现
Br J Clin Pharmacol. 2002 May;53(5):519-25. doi: 10.1046/j.1365-2125.2002.01578.x.
10
Effects of the putative P-type calcium channel blocker, R,R-(-)-daurisoline on neurotransmitter release.假定的P型钙通道阻滞剂R，R-（-）-蝙蝠葛碱对神经递质释放的影响。
Naunyn Schmiedebergs Arch Pharmacol. 1995 Dec;352(6):670-8. doi: 10.1007/BF00171327.
本文引用的文献
1
Antihistamine activity of the optical isomers of pheniramine and its chlor- and brom-substituted derivatives.
Chemotherapia (Basel). 1961;3:120-7. doi: 10.1159/000219537.
2
Some chemical and physical properties associated with histamine antagonism.一些与组胺拮抗作用相关的化学和物理性质。
Br J Pharmacol Chemother. 1955 Sep;10(3):270-8. doi: 10.1111/j.1476-5381.1955.tb00870.x.
3
Inhibition of the uptake of tritiated catecholamines by antidepressant and related agents.抗抑郁药及相关药物对氚标记儿茶酚胺摄取的抑制作用。
Eur J Pharmacol. 1967 Dec;2(3):181-6. doi: 10.1016/0014-2999(67)90084-2.
4
5
The pharmacology of iprindole, a new antidepressant.新型抗抑郁药伊普吲哚的药理学
Psychopharmacologia. 1969;15(3):169-85. doi: 10.1007/BF00411167.
6
The binding of conformationally restricted antihistamines to histamine receptors.
J Pharm Pharmacol. 1973 Nov;25(11):887-94. doi: 10.1111/j.2042-7158.1973.tb09968.x.
7
Histamine H1-receptors in brain labeled with 3H-mepyramine.
Eur J Pharmacol. 1978 Apr 15;48(4):463-4. doi: 10.1016/0014-2999(78)90177-2.
8
Brain histamine receptors as targets for antidepressant drugs.
Nature. 1978 Mar 23;272(5651):329-33. doi: 10.1038/272329a0.
9
Specific binding of 3H-mepyramine to histamine H1 receptors in intestinal smooth muscle.
Nature. 1977 Nov 24;270(5635):361-3. doi: 10.1038/270361a0.
10
Histaminergic mechanisms in brain.大脑中的组胺能机制。
Annu Rev Pharmacol Toxicol. 1977;17:325-39. doi: 10.1146/annurev.pa.17.040177.001545.
Zotero 插件