Synthesis and dopamine receptors binding affinity of 2-(3-fluoro-4-hydroxyphenyl)ethylamine and its N-alkyl derivatives.

Il Farmaco; edizione scientifica Pub Date : 1988-01-01
M Cardellini, G M Cingolani, F Claudi, V Perlini, W Balduini, F Cattabeni
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Abstract

The 2-(3-fluoro-4-hydroxyphenyl)ethylamine and its N,N-dialkyl derivatives were synthesized. The affinity of new compounds for dopamine binding sites was measured in a test involving displacement of [3H]SCH 23390 (D-1 selective) and [3H]spiperone (D-2 selective) from homogenized rat striatal tissue. No compound proved effective in displacing [3H]SCH 23390. Two derivatives are selective displacers of [3H]spiperone.

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2-(3-氟-4-羟基苯基)乙胺及其n -烷基衍生物的合成及多巴胺受体结合亲和力。
合成了2-(3-氟-4-羟基苯基)乙胺及其N,N-二烷基衍生物。通过从匀浆大鼠纹状体组织中置换[3H]SCH 23390 (D-1选择性)和[3H]spiperone (D-2选择性)的实验,测量了新化合物对多巴胺结合位点的亲和力。未发现有效取代[3H] sch23390的化合物。两种衍生物是[3H]spiperone的选择性置换物。
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