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左那曲朵是一种强效的大麻素类镇痛药,可拮抗氟哌啶醇诱导的纹状体多巴胺合成激活。

Levonantradol, a potent cannabinoid-related analgesic, antagonizes haloperidol-induced activation of striatal dopamine synthesis.

作者信息

Koe B K

出版信息

Eur J Pharmacol. 1981 Mar 12;70(2):231-5. doi: 10.1016/0014-2999(81)90219-3.

Abstract

Levonantradol antagonized the compensatory acceleration of striatal dopamine synthesis induced by haloperidol. This effect was stereospecific, since the pharmacologically less active enantiomer, dextronantradol was approximately 30 times less effective. delta 9-Tetrahydrocannabinol at a dose 320 times higher than levonantradol also attenuated the haloperidol effect, but cannabidiol was inactive at a dose 750 times higher. GABA-like actions of levonantradol may be responsible for this responsible for this antagonism of haloperidol, but anticholinergic effects may also contribute.

摘要

左纳曲朵拮抗了氟哌啶醇诱导的纹状体多巴胺合成的代偿性加速。这种作用具有立体特异性,因为药理活性较低的对映体右纳曲朵的效力约低30倍。剂量比左纳曲朵高320倍的Δ⁹ - 四氢大麻酚也减弱了氟哌啶醇的作用,但剂量比左纳曲朵高750倍的大麻二酚却无活性。左纳曲朵的GABA样作用可能是其拮抗氟哌啶醇作用的原因,但抗胆碱能作用也可能有贡献。

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