Synthesis and evaluation of 2-(5-methoxythiophen-3-yl)ethylamines as potential dopamine agonists

Add time:08/03/2019    Source:sciencedirect.com

The synthesis of 2-(5-methoxythiophen-3-yl)ethylamine and some derivatives bearing propyl and 2-phenylethyl substituents on the amino group has been described. The affinities for dopamine D1 and D2 receptors were evaluated by binding assays on rat striatum. None of the compounds show affinity for the D1 receptor. In the D2 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-hydroxyphenyl)ethylamine (1, RU 24213). In preliminary behavioral tests [2-(5-methoxythiophen-3-yl)ethyl]phenethylpropylamine behaves as a selective D2 agonist.

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