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7-Methyl-6,7,8,9,14,15-hexahydro-5H-benz[d]indolo[2,3-g]azecine: a new heterocyclic system and a new lead compound for dopamine receptor antagonists.

Abstract：

:Partially hydrogenated derivatives of the new heterocyclic ring systems benz[d]indolo[2,3-g]azecine and bisindolo[3,2-d][2, 3-g]azecine were synthesized starting from lactones and amines via the described synthetic methods. In binding assays with rat striatal receptors, 7-methyl-6,7,8,9,14,15-hexahydro-5H-benz[d]indolo[2, 3-g]azecine (LE 300) proved to be of high affinity for the D(1) binding site (K(i) = 0.08 nmol for displacement of [(3)H]SCH23390), being superior in this assay to standards such as butaclamol and SCH23390. This compound was characterized as a dopamine antagonist by conditioned avoidance response test with mice. Thus, LE 300 represents the lead of a new class of dopamine antagonists for future investigations.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Witt T,Hock FJ,Lehmann J

doi

10.1021/jm9911478

keywords:

subject

Has Abstract

pub_date

2000-05-18 00:00:00

pages

2079-81

issue

10

eissn

0022-2623

issn

1520-4804

pii

jm9911478

journal_volume

43

pub_type

杂志文章

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