Pivaloyl esters of N,N-dialkylated dopamine congeners. Central dopamine-receptor stimulating activity

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Abstract
A sensitive biochemical screening method was designed to test for dopamine-receptor stimulating activity. For behavioral studies and for determination of the duration of action on the compounds, motor activity measurements were taken using reserpinized rats. O,O''-Dipivaloyl-N,N-dipropyldopamine was the only derivative of a series of dipivaloyl-N,N-dialkyldopamines studied that showed any significant activity. The monopivaloyl ester 2-(3-pivaloyloxyphenyl)-N,N-dipropylethylamine seemed to be more potent. The same relationship was found for the corresponding phenols, N,N-dipropyldopamine and 2-(3-hydroxyphenyl)-N,N-dipropylethylamine, although both were more active than their pivaloyl esters.