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皮摩尔浓度的左旋多巴对突触前β-肾上腺素能受体的活性具有立体选择性增强作用,以促进大鼠下丘脑切片中内源性去甲肾上腺素的释放。

Picomolar concentrations of L-dopa stereoselectively potentiate activities of presynaptic beta-adrenoceptors to facilitate the release of endogenous noradrenaline from rat hypothalamic slices.

作者信息

Goshima Y, Nakamura S, Ohno K, Misu Y

机构信息

Department of Pharmacology, Yokohama City University School of Medicine, Japan.

出版信息

Neurosci Lett. 1991 Aug 19;129(2):214-6. doi: 10.1016/0304-3940(91)90464-5.

DOI:10.1016/0304-3940(91)90464-5
PMID:1660577
Abstract

Interactions between (-)-isoproterenol and DOPA on the release of endogenous noradrenaline (NA) evoked by electrical field stimulation (2 Hz, alternative polarity) were studied in rat superfused hypothalamic slices in the presence of 3-hydroxybenzylhydrazine, an inhibitor of L-aromatic amino acid decarboxylase, and cocaine. Isoproterenol (0.3-3 nM) facilitated the NA release in a concentration-dependent manner, while 10 pM L-DOPA alone produced no effect. This facilitation at 0.3-3 nM was potentiated by 20-70% by simultaneously applied 10 pM L-DOPA but that at 3 nM was not modified by 10 pM D-DOPA. This potentiation of the isoproterenol (3 nM)-induced facilitation of the NA release was concentration-dependent at 1-10 pM of L-DOPA. L-DOPA methyl ester (1 nM) antagonized the L-DOPA (10 pM)-induced potentiation of the facilitation of the NA release by 3 nM isoproterenol to a level of the facilitation by isoproterenol alone, whereas 10 nM (-) propranolol antagonized both the facilitation by isoproterenol alone and its potentiation by L-DOPA to a control level. Picomolar concentrations of L-DOPA stereoselectively act on a recognition site for itself, and then potentiate activities of presynaptic beta-adrenoceptors to facilitate the NA release from rat hypothalamic slices.

摘要

在存在L-芳香族氨基酸脱羧酶抑制剂3-羟基苄基肼和可卡因的情况下,在大鼠下丘脑灌流切片中研究了(-)-异丙肾上腺素与多巴对电场刺激(2Hz,交替极性)诱发的内源性去甲肾上腺素(NA)释放的相互作用。异丙肾上腺素(0.3-3nM)以浓度依赖性方式促进NA释放,而单独使用10pM左旋多巴则无作用。同时应用10pM左旋多巴可使0.3-3nM时的这种促进作用增强20-70%,但3nM时的促进作用不受10pM右旋多巴的影响。左旋多巴(1-10pM)对异丙肾上腺素(3nM)诱导的NA释放促进作用的这种增强呈浓度依赖性。左旋多巴甲酯(1nM)将左旋多巴(10pM)诱导的3nM异丙肾上腺素对NA释放促进作用的增强拮抗至单独异丙肾上腺素促进作用的水平,而10nM(-)普萘洛尔将单独异丙肾上腺素的促进作用及其被左旋多巴的增强作用均拮抗至对照水平。皮摩尔浓度的左旋多巴对其自身的识别位点具有立体选择性作用,然后增强突触前β-肾上腺素能受体的活性,以促进大鼠下丘脑切片中NA的释放。

相似文献

1
Picomolar concentrations of L-dopa stereoselectively potentiate activities of presynaptic beta-adrenoceptors to facilitate the release of endogenous noradrenaline from rat hypothalamic slices.皮摩尔浓度的左旋多巴对突触前β-肾上腺素能受体的活性具有立体选择性增强作用,以促进大鼠下丘脑切片中内源性去甲肾上腺素的释放。
Neurosci Lett. 1991 Aug 19;129(2):214-6. doi: 10.1016/0304-3940(91)90464-5.
2
L-dopa facilitates the release of endogenous norepinephrine and dopamine via presynaptic beta 1- and beta 2-adrenoceptors under essentially complete inhibition of L-aromatic amino acid decarboxylase in rat hypothalamic slices.在大鼠下丘脑切片中,左旋多巴在L-芳香族氨基酸脱羧酶基本完全被抑制的情况下,通过突触前β1和β2肾上腺素能受体促进内源性去甲肾上腺素和多巴胺的释放。
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3
L-dopa methyl ester antagonizes competitively L-dopa-induced facilitation of noradrenaline release from rat hypothalamic slices.左旋多巴甲酯竞争性拮抗左旋多巴诱导的大鼠下丘脑切片去甲肾上腺素释放的促进作用。
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L-dihydroxyphenylalanine methyl ester is a potent competitive antagonist of the L-dihydroxyphenylalanine-induced facilitation of the evoked release of endogenous norepinephrine from rat hypothalamic slices.L-二羟基苯丙氨酸甲酯是L-二羟基苯丙氨酸诱导大鼠下丘脑切片内源性去甲肾上腺素诱发释放增强作用的强效竞争性拮抗剂。
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5
L-dopa potentiates presynaptic inhibitory alpha 2-adrenoceptor- but not facilitatory angiotensin II receptor-mediated modulation of noradrenaline release from rat hypothalamic slices.左旋多巴增强大鼠下丘脑切片中去甲肾上腺素释放的突触前抑制性α2 -肾上腺素能受体介导的调节,但不增强促肾上腺皮质激素释放激素受体介导的调节。
Jpn J Pharmacol. 1993 May;62(1):119-22. doi: 10.1254/jjp.62.119.
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Biphasic actions of L-DOPA on the release of endogenous noradrenaline and dopamine from rat hypothalamic slices.左旋多巴对大鼠下丘脑切片内源性去甲肾上腺素和多巴胺释放的双相作用。
Br J Pharmacol. 1986 Sep;89(1):229-34. doi: 10.1111/j.1476-5381.1986.tb11139.x.
7
L-dopa-like regulatory actions of L-threo-3,4-dihydroxyphenylserine on the release of endogenous noradrenaline via presynaptic receptors in rat hypothalamic slices.L-苏式-3,4-二羟基苯丝氨酸对大鼠下丘脑切片中内源性去甲肾上腺素经突触前受体释放的左旋多巴样调节作用。
J Pharm Pharmacol. 1992 Dec;44(12):990-5. doi: 10.1111/j.2042-7158.1992.tb07080.x.
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Nanomolar L-dopa facilitates release of dopamine via presynaptic beta-adrenoceptors: comparative studies on the actions in striatal slices from control and 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-treated C57 black mice, an animal model for Parkinson's disease.纳摩尔浓度的左旋多巴通过突触前β-肾上腺素能受体促进多巴胺释放:对正常和1-甲基-4-苯基-1,2,3,6-四氢吡啶(MPTP)处理的C57黑小鼠(帕金森病动物模型)纹状体切片中作用的比较研究。
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[Transmitter-like release and pharmacological activities of levodopa].[左旋多巴的递质样释放及药理活性]
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