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大鼠纹状体和伏隔核中的多巴胺受体;使用多巴胺刚性类似物的构象研究。

Dopamine receptors in rat striatum and nucleus accumbens; conformational studies using rigid analogues of dopamine.

作者信息

Woodruff G N, Watling K J, Andrews C D, Poat J A, McDermed J D

出版信息

J Pharm Pharmacol. 1977 Jul;29(7):422-7. doi: 10.1111/j.2042-7158.1977.tb11357.x.

Abstract

A study was made of the actions of dopamine and of some 2-amino-1,2,3,4-tetrahydronaphthalenes on dopamine-sensitive adenylate cyclase in homogenates of rat striatum and nucleus accumbens. The compounds were also tested for their ability to stimulate motor activity following bilateral injection into the nucleus accumbens of conscious rats. The most active compounds on adenylate cyclase from both striatum and nucleus accumbens were dopamine and 2-amino-6,7-dihydroxy-1,2,3,4-tetrahydronaphthalene(6,7-diOHATN). The 5,6-dihydroxy analogue (5,6-diOHATN) was 50 times less active than 6,7-diOHATN in striatal homogenates and 350 times less active in homogenates of nucleus accumbens. All dihydroxy compounds tested were active in causing stimulation of motor activity, the most active compounds being 6,7-and5,6diOHATN. Both dimethoxy derivatives tested were inactive on the adenylate cyclase and as locomotor stimulants.

摘要

对多巴胺及某些2-氨基-1,2,3,4-四氢萘对大鼠纹状体和伏隔核匀浆中多巴胺敏感腺苷酸环化酶的作用进行了研究。还测试了这些化合物在向清醒大鼠伏隔核双侧注射后刺激运动活性的能力。对纹状体和伏隔核的腺苷酸环化酶最具活性的化合物是多巴胺和2-氨基-6,7-二羟基-1,2,3,4-四氢萘(6,7-二羟基四氢萘)。5,6-二羟基类似物(5,6-二羟基四氢萘)在纹状体匀浆中的活性比6,7-二羟基四氢萘低50倍,在伏隔核匀浆中的活性低350倍。所有测试的二羟基化合物在引起运动活性刺激方面均有活性,最具活性的化合物是6,7-二羟基四氢萘和5,6-二羟基四氢萘。所测试的两种二甲氧基衍生物对腺苷酸环化酶无活性,也不是运动兴奋剂。

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