Novel dopamine receptor agonists and antagonists with preferential action on autoreceptors.
Novel dopamine receptor agonists and antagonists with preferential action on autoreceptors.
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新型多巴胺受体激动剂和拮抗剂，对自身受体具有优先作用。
DOI：
10.1021/jm00146a012
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发表时间：
1985
影响因子：
7.3
通讯作者：
B. Andersson
中科院分区：
文献类型：
--
作者：
A. Johansson;L. Arvidsson;U. Hacksell;J. Nilsson;K. Svensson;S. Hjorth;D. Clark;A. Carlsson;D. Sanchez;B. Andersson
合成了顺式-5-羟基-1-甲基-2-（二正丙胺基）四氢萘及其甲醚的对映体。通过在大鼠中使用生物化学和行为测试来测试化合物的中枢多巴胺（DA）受体活性。1和2的（1 R，2S）-（-）对映体被表征为中枢作用DA-受体激动剂，而相应的（1 S，2 R）-（+）对映体被表征为中枢作用DA-受体拮抗剂。化合物（+）-1和（+）-2与经典的精神抑制剂的不同之处在于能够在宽剂量范围内增加DA合成速率而不降低运动活性，这表明对DA自身受体具有显著的选择性。此外，（-）对映体似乎优先作用于DA自身受体。
The enantiomers of cis-5-hydroxy-1-methyl-2-(di-n-propylamino)tetralin and its methyl ether have been synthesized. The compounds were tested for central dopamine (DA) receptor activity, by using biochemical and behavioral tests in rats. The (1R,2S)-(-) enantiomers of 1 and 2 are characterized as centrally acting DA-receptor agonists while the corresponding (1S,2R)-(+) enantiomers are characterized as centrally acting DA-receptor antagonists. Compounds (+)-1 and (+)-2 differ from classical neuroleptics in being able to increase DA synthesis rate in a wide dose range without reducing locomotor activity, suggesting a pronounced selectivity for DA autoreceptors. Also the (-) enantiomers seem to act preferentially on DA autoreceptors.