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豚鼠的离体提睾肌制备以及(体外)精索神经-提睾肌制备

The isolated cremaster muscle preparation and (external) spermatic nerve-cremaster muscle preparation of the guinea-pig.

作者信息

Kelkar V V, Gupta R S, Gokhale S V

出版信息

J Pharm Pharmacol. 1976 Apr;28(4):290-3. doi: 10.1111/j.2042-7158.1976.tb04155.x.

Abstract

The isolated cremaster muscle preparation and spermatic nerve-cremaster muscle preparation of the guinea-pig were studied in vitro to determine their suitability as pharmacological test models. The preparation was contracted by acetylcholine, carbachol, succinylcholine and decamethonium (pD2 values, 4-2, 5-3, 7-3 and 7-4, respectively) through an action on a curare-sensitive cholinoceptor. Lobeline and DMPP were ineffective. Nicotine contracted the muscle, but there was tachyphylaxis. Tubocurarine and hexamethonium presumably competitively antagonized acetylcholine (pA2 values, 7-3 and 5-8); lobeline was a non-competitive antagonist (pD'2 value, 6-4). Atropine and mecamylamine exerted a dualistic action against acetylcholine (final pD'2 values, 5-3 and 6-7, respectively). Tubocurarine, succinylcholine and decamethonium exhibited their typical action when tested with spermatic nerve-cremaster muscle preparation; the latter two drugs also produced muscle spasm. Hexamethonium was a weak blocker of neuromuscular transmission. Atropine, mecamylamine, lobeline and DMPP exhibited neuromuscular blocking activity; however, directly evoked muscle twitches were also notably affected. The cremaster muscle preparations seem to add usefully to the list of currently used in vitro tests, with the added advantage that a mammalian skeletal muscle model is used for simultaneous quantitative studies.

摘要

对豚鼠的离体提睾肌标本和精索神经 - 提睾肌标本进行了体外研究,以确定它们作为药理学测试模型的适用性。该标本通过作用于对箭毒敏感的胆碱受体,被乙酰胆碱、卡巴胆碱、琥珀酰胆碱和十烃季铵(pD2值分别为4 - 2、5 - 3、7 - 3和7 - 4)收缩。洛贝林和二甲基苯基哌嗪无效。尼古丁使肌肉收缩,但出现快速耐受性。筒箭毒碱和六甲铵可能竞争性拮抗乙酰胆碱(pA2值分别为7 - 3和5 - 8);洛贝林是非竞争性拮抗剂(pD'2值为6 - 4)。阿托品和美加明对乙酰胆碱发挥二元作用(最终pD'2值分别为5 - 3和6 - 7)。用精索神经 - 提睾肌标本进行测试时,筒箭毒碱、琥珀酰胆碱和十烃季铵表现出它们的典型作用;后两种药物还产生肌肉痉挛。六甲铵是神经肌肉传递的弱阻断剂。阿托品、美加明、洛贝林和二甲基苯基哌嗪表现出神经肌肉阻断活性;然而,直接诱发的肌肉抽搐也受到显著影响。提睾肌标本似乎可以有效地补充到目前使用的体外测试列表中,其额外的优点是使用了哺乳动物骨骼肌模型进行同步定量研究。

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