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ZK 91296,一种苯二氮䓬受体部分激动剂。

ZK 91296, a partial agonist at benzodiazepine receptors.

作者信息

Petersen E N, Jensen L H, Honoré T, Braestrup C, Kehr W, Stephens D N, Wachtel H, Seidelman D, Schmiechen R

出版信息

Psychopharmacology (Berl). 1984;83(3):240-8. doi: 10.1007/BF00464788.

Abstract

5-benzyloxy-4-methoxymethyl-beta-carboline-3-carboxylate) is a potent and selective ligand for benzodiazepine (BZ) receptors. Biochemical investigations indicate that ZK 91296 may be a partial agonist at BZ receptors. Such partial agonism may explain to some extent why ZK 91296 needs higher BZ receptor occupancy than diazepam for the same effect against chemical convulsants and for behavioural effects. The lack of sedative effects, and the very potent inhibition of reflex epilepsy, spontaneous epilepsy and DMCM-induced seizures suggest, furthermore, that ZK 91296 may possess pharmacological selectivity for a particular type of BZ receptor interaction, perhaps including topographic as well as receptor subtype differentiation.

摘要

5-苄氧基-4-甲氧基甲基-β-咔啉-3-羧酸酯是一种强效且选择性的苯二氮䓬(BZ)受体配体。生化研究表明,ZK 91296可能是BZ受体的部分激动剂。这种部分激动作用在一定程度上可以解释为什么ZK 91296在针对化学惊厥剂和行为效应产生相同效果时,比地西泮需要更高的BZ受体占有率。此外,缺乏镇静作用以及对反射性癫痫、自发性癫痫和DMCM诱导的癫痫发作具有非常强效的抑制作用表明,ZK 91296可能对特定类型的BZ受体相互作用具有药理学选择性,这可能包括拓扑学以及受体亚型的区分。

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