多塞平与豚鼠和大鼠脑中组胺H1受体的结合。
The binding of doxepin to histamine H1-receptors in guinea-pig and rat brain.
作者信息
Aceves J, Mariscal S, Morrison K E, Young J M
出版信息
Br J Pharmacol. 1985 Feb;84(2):417-24. doi: 10.1111/j.1476-5381.1985.tb12925.x.
Abstract
The affinity constant for doxepin obtained from inhibition of histamine-induced contraction of guinea-pig intestinal smooth muscle at 30 degrees C was 2.6 +/- 0.18 X 10(10)M-1. The slope of a Schild plot was not significantly different from unity. The affinity constant of doxepin did not vary markedly with temperature. At 37 degrees C it was 3.75 +/- 0.02 X 10(10)M-1 and at 25 degrees C 2.1 X 10(10)M-1. Doxepin was a competitive inhibitor of [3H]-mepyramine binding to guinea-pig cerebellar homogenates. The affinity constant derived for doxepin at 30 degrees C was 1.12 +/- 0.45 X 10(10)M-1. Hill coefficients for curves of doxepin or mepyramine inhibition of [3H]-mepyramine binding in guinea-pig cerebellum, cerebral cortex and hippocampus did not differ significantly from unity. The mean affinity of mepyramine for histamine H1-receptors in rat brain homogenates at 30 degrees C was 3.5 X 10(8)M-1. Hill coefficients for curves of doxepin or mepyramine inhibition of [3H]-mepyramine binding to homogenates of rat cerebral cortex or rat whole brain were near unity. These studies provide no evidence that doxepin binds preferentially to a sub-class of histamine H1-receptors in rat brain.
摘要
在30℃下，通过抑制组胺诱导的豚鼠肠道平滑肌收缩得到的多塞平亲和常数为2.6±0.18×10¹⁰M⁻¹。Schild图的斜率与1无显著差异。多塞平的亲和常数随温度变化不明显。在37℃时为3.75±0.02×10¹⁰M⁻¹，在25℃时为2.1×10¹⁰M⁻¹。多塞平是[³H] - 美吡拉敏与豚鼠小脑匀浆结合的竞争性抑制剂。在30℃下得到的多塞平亲和常数为1.12±0.45×10¹⁰M⁻¹。多塞平或美吡拉敏抑制豚鼠小脑、大脑皮层和海马中[³H] - 美吡拉敏结合的曲线的希尔系数与1无显著差异。在30℃时，美吡拉敏对大鼠脑匀浆中组胺H1受体的平均亲和力为3.5×10⁸M⁻¹。多塞平或美吡拉敏抑制[³H] - 美吡拉敏与大鼠大脑皮层或大鼠全脑匀浆结合的曲线的希尔系数接近1。这些研究没有提供证据表明多塞平在大鼠脑中优先结合组胺H1受体的一个亚类。
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本文引用的文献
1
Protein measurement with the Folin phenol reagent.使用福林酚试剂进行蛋白质测定。
J Biol Chem. 1951 Nov;193(1):265-75.
2
STIMULANT ACTIONS OF VOLATILE ANAESTHETICS ON SMOOTH MUSCLE.挥发性麻醉药对平滑肌的兴奋作用
Br J Pharmacol Chemother. 1964 Apr;22(2):356-65. doi: 10.1111/j.1476-5381.1964.tb02040.x.
3
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Br J Pharmacol. 1980 Apr;68(4):687-96. doi: 10.1111/j.1476-5381.1980.tb10861.x.
4
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Eur J Pharmacol. 1981 Apr 9;70(4):501-9. doi: 10.1016/0014-2999(81)90361-7.
5
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Eur J Pharmacol. 1982 Jul 9;81(2):301-7. doi: 10.1016/0014-2999(82)90448-4.
6
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Eur J Pharmacol. 1982 Mar 12;78(3):279-85. doi: 10.1016/0014-2999(82)90029-2.
7
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Eur J Pharmacol. 1984 Jan 27;97(3-4):265-9. doi: 10.1016/0014-2999(84)90458-8.
8
The nature of the binding of [3H]mepyramine to homogenates of guinea-pig cerebral cortex at different [3H]ligand concentrations.在不同[³H]配体浓度下，[³H]美吡拉敏与豚鼠大脑皮层匀浆的结合性质。
Biochem Pharmacol. 1983 Aug 15;32(16):2449-51. doi: 10.1016/0006-2952(83)90690-1.
9
Inositol phospholipid hydrolysis in rat cerebral cortical slices: I. Receptor characterisation.大鼠大脑皮质切片中的肌醇磷脂水解：I. 受体特性
J Neurochem. 1984 May;42(5):1379-87. doi: 10.1111/j.1471-4159.1984.tb02798.x.
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Br J Pharmacol. 1982 Oct;77(2):347-57. doi: 10.1111/j.1476-5381.1982.tb09304.x.
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