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5-羟色胺和多巴胺作为贻贝中的神经递质:一种有机汞对5-羟色胺受体的阻断作用

Serotonin and dopamine as neurotransmitters in mytilus: block of serotonin receptors by an organic mercurial.

作者信息

Twarog B M, Muneoka Y, Ledgere M

出版信息

J Pharmacol Exp Ther. 1977 May;201(2):350-6.

PMID:16121
Abstract

The effects of mersalyl, bromo-LSD (BOL) and methysergide (UML) on the relaxation of catch by certain indole and catechol derivatives were studied in the anterior byssus retractor muscle of Mytilus. Mersalyl antagonized relaxation in response to serotonin whereas BOL and UML were less effective. Two other indole derivatives, ergotamine and gramine, were also blocked by mersalyl; BOL and UML antagonized relaxation in response to dopamine more effectively than did mersalyl. Two other catechols, epinephrine and norepinephrine, were also blocked more effectively by BOL and UML than by mersaly. Relaxation in response to neural stimulation was blocked more effectively by mersalyl than by BOL. The blocking action of mersalyl on neural relaxation reversed very poorly after washing the drug, but complete reversal was induced by brief exposure to dithiothreitol. It is concluded that the evidence supports an hypothesis that the transmitter released by relaxing nerves is serotonin. It is suggested that mersalyl blocks serotonin by combining with a sulfhydryl group at or near the site on the receptor to which the indole nitrogen attaches.

摘要

在贻贝前足丝牵缩肌中,研究了汞撒利、溴化麦角酸二乙酰胺(BOL)和甲基麦角新碱(UML)对某些吲哚和儿茶酚衍生物引起的捕捉松弛的影响。汞撒利拮抗5-羟色胺引起的松弛,而BOL和UML的作用较弱。另外两种吲哚衍生物,麦角胺和禾胺,也被汞撒利阻断;BOL和UML拮抗多巴胺引起的松弛比汞撒利更有效。另外两种儿茶酚,肾上腺素和去甲肾上腺素,也被BOL和UML比汞撒利更有效地阻断。汞撒利比BOL更有效地阻断神经刺激引起的松弛。汞撒利对神经松弛的阻断作用在冲洗药物后逆转很差,但通过短暂暴露于二硫苏糖醇可诱导完全逆转。结论是,证据支持一种假说,即松弛神经释放的递质是5-羟色胺。有人提出,汞撒利通过与受体上吲哚氮附着位点处或附近的巯基结合来阻断5-羟色胺。

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