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从人血小板中释放儿茶酚胺和5-羟色胺。

Liberation of catecholamines and 5-hydroxytryptamine from human blood-platelets.

作者信息

Peyer M, Pletscher A

出版信息

Naunyn Schmiedebergs Arch Pharmacol. 1981 Feb;316(1):81-6. doi: 10.1007/BF00507232.

Abstract

Spontaneous and drug-induced liberation of 14C-5-hydroxytryptamine (14C-5HT), 3H-dopamine (3H-DA) and 3H-noradrenaline (3H-NA) from normal and reserpinized human blood-platelets has been determined from measurements of the amine contents before and after incubation in tris-buffer. In normal platelets the spontaneous liberation of 3H-catecholamines was more marked than that of 14C-5HT, but was less in percent for all these labelled amines than in reserpinized platelets. Thrombin lowered amine contents more in normal than in reserpinized platelets. The initial thrombin-induced decrease of 14C-5HT, in contrast to that of 3H-catecholamines, showed a partial recovery after 30 min which was abolished by imipramine. The benzoquinolizine Ro 4-1284 diminished all the amines in normal, but not in reserpinized platelets. In normal platelets tryamine affected 14C-5HT and 3H-DA about equally, whereas 3H-NA much less. Octopamine showed a similar pattern as tryamine, but was less potent. P-chlormethamphetamine (PCMA) and amphetamine decreased 3H-DA less markedly than 14C-5HT and 3H-NA not at all. In reserpinized platelets these arylalkylamines induced a decrease of 14C-5HT but not of 3H-catecholamines. It is concluded that (a) 3H-catecholamines like 14C-5HT are mainly localized in the granular pool of normal human platelets, (b) the pattern of action of a drug on intra- and extragranular amines depends not only on the nature of the drug and the amine to be liberated, but in comparison with previous results also on the species, (c) platelets are not completely satisfactory models for monoaminergic neurons, especially catecholaminergic ones regarding drug-induced amine liberation.

摘要

通过测定在三羟甲基氨基甲烷缓冲液中孵育前后的胺含量,已确定了正常和利血平化人血小板中14C - 5 - 羟色胺(14C - 5HT)、3H - 多巴胺(3H - DA)和3H - 去甲肾上腺素(3H - NA)的自发释放及药物诱导释放。在正常血小板中,3H - 儿茶酚胺的自发释放比14C - 5HT更明显,但对于所有这些标记胺而言,其释放百分比比利血平化血小板中的少。凝血酶使正常血小板中的胺含量降低的程度比利血平化血小板中的更大。与3H - 儿茶酚胺不同,凝血酶最初诱导的14C - 5HT含量降低在30分钟后出现部分恢复,而这一恢复被丙咪嗪消除。苯并喹啉嗪Ro 4 - 1284使正常血小板中的所有胺含量降低,但对利血平化血小板中的胺含量无影响。在正常血小板中,酪胺对14C - 5HT和3H - DA的影响大致相同,而对3H - NA的影响则小得多。章鱼胺表现出与酪胺相似的模式,但效力较弱。对氯甲基苯丙胺(PCMA)和苯丙胺使3H - DA降低的程度不如14C - 5HT明显,对3H - NA则完全无影响。在利血平化血小板中,这些芳基烷基胺可诱导14C - 5HT含量降低,但对3H - 儿茶酚胺无影响。得出以下结论:(a)与14C - 5HT一样,3H - 儿茶酚胺主要定位于正常人血小板的颗粒池中;(b)药物对颗粒内和颗粒外胺的作用模式不仅取决于药物的性质和要释放的胺,而且与先前的结果相比还取决于物种;(c)血小板对于单胺能神经元,尤其是关于药物诱导的胺释放的儿茶酚胺能神经元而言,并不是完全令人满意的模型。

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