SYNTHESIS AND EVALUATION OF 2-(5-METHOXYTHIOPHEN-3-YL)ETHYLAMINES AS POTENTIAL DOPAMINE AGONISTS

The synthesis of 2-(5-methoxythiophen-3-yl)ethylamine and some derivat ives bearing propyl and 2-phenylethyl substituents on the amino group has been described. The affinities for dopamine D-1 and D-2 receptors were evaluated by binding assays on rat striatum. None of the compound s show affinity for the D-1 receptor. In the D-2 binding assays the N- propyl-N-(2- phenylethyl) derivatives show affinity similar to that of the reference compound N-n-propyl-N-(2-phenylethyl)-2-(3-hydroxy- phe nyl)ethylamine (1, RU 24213). In preliminary behavioral tests (5-metho xythiophen-3-yl)ethyl]phenethylpropylamine behaves as a selective D-2 agonist.