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在人类腮腺唾液腺副交感神经支配已消除的情况下,阿托品是否为毛果芸香碱的拮抗剂?

Is atropine a pilocarpine antagonist in cases of eliminated parasympathetic innervation of the human parotid salivary gland?

作者信息

Levin S L

机构信息

Clinic for Nervous Diseases, Leningrad Paediatric College, USSR.

出版信息

J Auton Pharmacol. 1987 Sep;7(3):215-31. doi: 10.1111/j.1474-8673.1987.tb00151.x.

Abstract

1 Following denervation of the human parotid salivary gland, pilocarpine caused an intensified stimulant response on salivation and a stimulant effect of atropine on salivary secretion was revealed. However, despite its stimulant effect on salivary secretion, atropine retained its action in blocking the salivatory response to pilocarpine. 2 This dualism in the action of atropine is explained by an action on different muscarinic receptor sub-types, i.e. on some sub-types atropine behaves as an antagonist and on others as an agonist. 3 Under the particular conditions in which the studies were performed, pilocarpine neither prevented nor increased the subsequent paradoxical response to atropine. Moreover, when injected at the peak of the atropine salivatory response it caused neither addition nor synergism to the atropine response. 4 Following the simultaneous injection of both pilocarpine and atropine, atropine initially suppressed the effect of pilocarpine and then itself caused a powerful paradoxical salivation. 5 Pilocarpine injected at the end of the paradoxical secretory response to atropine caused no secretion indicating that atropine retained its antisecretory effect against pilocarpine. 6 The extent of pilocarpine secretory responses is dependent upon the presence or absence of atropine, whilst the atropine effect is independent of the presence of pilocarpine. This points to the presence of differing populations of cholinoreceptors to explain the agonist effects of pilocarpine and atropine.

摘要

1 人体腮腺去神经支配后,毛果芸香碱对唾液分泌产生增强的刺激反应,且显示出阿托品对唾液分泌有刺激作用。然而,尽管阿托品对唾液分泌有刺激作用,但它在阻断毛果芸香碱引起的唾液分泌反应方面仍保持其作用。2 阿托品作用的这种二元性是由其对不同毒蕈碱受体亚型的作用来解释的,即在某些亚型上阿托品表现为拮抗剂,而在其他亚型上表现为激动剂。3 在进行研究的特定条件下,毛果芸香碱既未预防也未增强随后对阿托品的反常反应。此外,在阿托品唾液分泌反应的峰值注射时,它既未增强也未协同阿托品反应。4 同时注射毛果芸香碱和阿托品后,阿托品最初抑制毛果芸香碱的作用,然后自身引起强烈的反常唾液分泌。5 在对阿托品的反常分泌反应结束时注射毛果芸香碱未引起分泌,这表明阿托品对毛果芸香碱仍保持其抗分泌作用。6 毛果芸香碱分泌反应的程度取决于阿托品的存在与否,而阿托品的作用则与毛果芸香碱的存在无关。这表明存在不同群体的胆碱能受体来解释毛果芸香碱和阿托品的激动剂作用。

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