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多塞平,一种三环类抗抑郁药,可与培养物中的正常、完整星形胶质细胞结合,并抑制异丙肾上腺素诱导的环磷酸腺苷生成增加。

Doxepin, a tricyclic antidepressant, binds to normal, intact astroglial cells in cultures and inhibits the isoproterenol-induced increase in cyclic AMP production.

作者信息

Hertz L, Richardson J S, Mukerji S

出版信息

Can J Physiol Pharmacol. 1980 Dec;58(12):1515-9. doi: 10.1139/y80-230.

DOI:10.1139/y80-230
PMID:6263430
Abstract

Doxepin binds to intact astrocytes in primary cultures. The binding is competitively displaceable by excess cold doxepin and it is pronounced (Bmax = 27 nmol/mg protein) but the affinity is rather low (KD = 30 microM). The binding is inhibited by other antidepressants (amitriptyline, desipramine, tranylcypromine, iprindole) and propranolol but not by isoproterenol. Nevertheless, doxepin counteracts effectively the increase in the production of cyclic AMP evoked by isoproterenol.

摘要

多塞平与原代培养中的完整星形胶质细胞结合。这种结合可被过量的冷多塞平竞争性取代,且结合明显(Bmax = 27 nmol/mg蛋白质),但亲和力相当低(KD = 30 μM)。其他抗抑郁药(阿米替林、地昔帕明、反苯环丙胺、茚满二氮卓)和普萘洛尔可抑制这种结合,但异丙肾上腺素无此作用。然而,多塞平可有效对抗异丙肾上腺素引起的环磷酸腺苷生成增加。

相似文献

1
Doxepin, a tricyclic antidepressant, binds to normal, intact astroglial cells in cultures and inhibits the isoproterenol-induced increase in cyclic AMP production.多塞平,一种三环类抗抑郁药,可与培养物中的正常、完整星形胶质细胞结合,并抑制异丙肾上腺素诱导的环磷酸腺苷生成增加。
Can J Physiol Pharmacol. 1980 Dec;58(12):1515-9. doi: 10.1139/y80-230.
2
The effects of antidepressant drugs on adenylyl cyclase linked beta adrenergic binding sites on mouse astrocytes in primary cultures.抗抑郁药物对原代培养小鼠星形胶质细胞中与腺苷酸环化酶相连的β-肾上腺素能结合位点的影响。
Prog Neuropsychopharmacol Biol Psychiatry. 1983;7(4-6):675-80. doi: 10.1016/0278-5846(83)90044-1.
3
The effects of the tricyclic antidepressants desipramine, doxepin and iprindole on the isolated perfused rabbit heart.三环类抗抑郁药地昔帕明、多塞平和茚满二氮䓬对离体灌注兔心脏的作用。
Naunyn Schmiedebergs Arch Pharmacol. 1974;284(3):215-32. doi: 10.1007/BF00500343.
4
Chronic antidepressant exposure enhances 5-hydroxytryptamine7 receptor-mediated cyclic adenosine monophosphate accumulation in rat frontocortical astrocytes.长期暴露于抗抑郁药可增强5-羟色胺7受体介导的大鼠前额叶皮质星形胶质细胞中环磷酸腺苷的积累。
J Pharmacol Exp Ther. 1996 Dec;279(3):1551-8.
5
Acute and chronic effects of antidepressant drugs on beta-adrenergic function in astrocytes in primary cultures: an indication of glial involvement in affective disorders?抗抑郁药物对原代培养星形胶质细胞β-肾上腺素能功能的急性和慢性影响:胶质细胞参与情感障碍的一个迹象?
J Neurosci Res. 1983;9(2):173-82. doi: 10.1002/jnr.490090209.
6
High-affinity binding of [3H]doxepin to histamine H1-receptors in rat brain: possible identification of a subclass of histamine H1-receptors.[3H]多塞平与大鼠脑内组胺H1受体的高亲和力结合:组胺H1受体一个亚类的可能鉴定
Eur J Pharmacol. 1982 Mar 12;78(3):279-85. doi: 10.1016/0014-2999(82)90029-2.
7
Cyclic AMP regulation of messenger RNA level of the stimulatory GTP-binding protein Gs alpha. Isoproterenol, forskolin and 8-bromoadenosine 3':5'-cyclic monophosphate increase the level of Gs alpha mRNA in cultured astroglial cells.环磷酸腺苷对刺激性鸟苷结合蛋白Gsα信使核糖核酸水平的调节。异丙肾上腺素、福斯高林和8-溴腺苷3':5'-环一磷酸可提高培养的星形胶质细胞中Gsα信使核糖核酸的水平。
Eur J Biochem. 1994 Jan 15;219(1-2):529-37. doi: 10.1111/j.1432-1033.1994.tb19968.x.
8
Alpha- and beta-adrenoceptor regulation of cyclic AMP accumulation in cultured rat astrocytes. A comparison of primary protoplasmic and mixed fibrous/protoplasmic astroglial cultures.培养的大鼠星形胶质细胞中环磷酸腺苷积累的α和β肾上腺素能受体调节。原代原生质星形胶质细胞培养物与混合纤维/原生质星形胶质细胞培养物的比较。
Biochem Pharmacol. 1991 Jun 21;42(1):59-69. doi: 10.1016/0006-2952(91)90681-t.
9
Melatonin inhibits beta-adrenoceptor-stimulated cyclic AMP accumulation in rat astroglial cell cultures.
Neuroendocrinology. 1984 Mar;38(3):176-81. doi: 10.1159/000123887.
10
Effects of chronic doxepin and amitriptyline administration in naïve mice and in neuropathic pain mice model.慢性给予多塞平和阿米替林对未处理小鼠及神经性疼痛小鼠模型的影响。
Neuroscience. 2015 May 21;294:38-50. doi: 10.1016/j.neuroscience.2015.03.003. Epub 2015 Mar 10.

引用本文的文献

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Inhibition of Microglial Activation by Amitriptyline and Doxepin in Interferon-β Pre-Treated Astrocyte-Microglia Co-Culture Model of Inflammation.在干扰素-β预处理的星形胶质细胞-小胶质细胞共培养炎症模型中,阿米替林和多塞平对小胶质细胞活化的抑制作用
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Memory in astrocytes: a hypothesis.星形胶质细胞中的记忆:一种假说。
Theor Biol Med Model. 2006 Jan 18;3:2. doi: 10.1186/1742-4682-3-2.