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. 1975 Feb;18(2):185-8.
doi: 10.1021/jm00236a016.

Neuroleptic agents of the benzocycloheptapyridoisoquinoline series. 1. Syntheses and stereochemical and structural requirements for activity of butaclamol and related compounds

Neuroleptic agents of the benzocycloheptapyridoisoquinoline series. 1. Syntheses and stereochemical and structural requirements for activity of butaclamol and related compounds

F T Bruderlein et al. J Med Chem. 1975 Feb.

Abstract

The syntheses and the structural and stereochemical requirements for antagonism of (+)-amphetamine-induced sterotypy are described for a series of benzocycloheptapyridoisoquinoline derivatives. One of these compounds, (plus or minus)-(4a,13b-trans)[3(OH),13b(H)-trans[-3-tert-butyl-2,3,4,4a,8,9,13b,14-octahydro-1H-benzo[6,7]cyclohepta[1,2,3-de]pyrido[2,1-a]isoquinolin-3ol hydrochloride (butaclamol hydrochloride, USAN), is currently being studied in man. The relationship between structure and antiamphetamine activity in this class of compounds is discussed.

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