6-氨甲基-3-甲基-4H-1,2,4-苯并噻二嗪-1,1-二氧化物对牛磺酸选择性拮抗作用的进一步证据。

Further evidence for selective antagonism of taurine by 6-aminomethyl-3-methyl-4H-1,2,4-benzothiadiazine-1,1-dioxide.

作者信息

Martin G E, Bendesky R J, Williams M

出版信息

Brain Res. 1981 Dec 21;229(2):530-5. doi: 10.1016/0006-8993(81)91017-9.

PMID:7198001

Abstract

The putative taurine antagonist 6-aminomethyl-3-methyl-4H-1,2,4-benzothiadiazine-1,1-dioxide (TAG), was examined for activity in blocking contraversive turning evoked by the injection of taurine into the substantia nigra of the rat. Microinjected intranigrally as pretreatment to taurine, TAG caused a 71% reduction in taurine elicited turning. On the other hand, TAG pretreatment did not diminish the number of turns evoked by the intranigral injection of the GABA agonist, muscimol. These results and the lack of effect of TAG in a number of central radioligand binding assays provide further indications that TAG may be a selective taurine antagonist.

摘要

对假定的牛磺酸拮抗剂6-氨甲基-3-甲基-4H-1,2,4-苯并噻二嗪-1,1-二氧化物（TAG）进行了研究，以考察其阻断向大鼠黑质注射牛磺酸所诱发的反向旋转行为的活性。TAG经黑质内微量注射作为牛磺酸的预处理，可使牛磺酸诱发的旋转行为减少71%。另一方面，TAG预处理并未减少向黑质内注射GABA激动剂蝇蕈醇所诱发的旋转次数。这些结果以及TAG在多项中枢放射性配体结合试验中无作用，进一步表明TAG可能是一种选择性牛磺酸拮抗剂。