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BIBTEX RIS

Piperazinomethyl Tetralines: Synthesis and Affinities for D1, D2 and 5-HT2A Receptors.

1995; Pharmaceutical Society of Japan; Volume: 43; Issue: 7 Linguagem: Inglês

10.1248/cpb.43.1234

ISSN

1347-5223

Autores

Enrique Raviña, José M. Cid, Jesus NEGREIRA, Elena Castro, Victor M. Moldes, Tomas G-FERREIRO, Elizabeth De La Rosa, Jose MACALLEJA, Marı́a L. de Ceballos,

Tópico(s)

Synthesis and Biological Evaluation

Resumo

Starting from the methyl ester of β-(bromomethyl)-γ-phenylbutyric acid and its m-fluoro derivative, we have prepared 2-[4[3-(p-fluorobenzoyl)-1-propyl]piperazin-1-ylmethyl]tetraline (QF0105B) and the corresponding 7-fluoro derivative (QF0106B). The affinities of these compounds for D1 and D2 dopamine and 5-HT2A receptors was evaluated in vitro. The afinities of QF0105B and QF0106B for D2 receptors are less than that of haloperidol (pKi's for inhibition of [3H]spiperone binding : 7.72, 7.06 and 8.30, respectively) but all three compounds have similar affinities for 5-HT2A receptors (pKi'S for inhibition of [3H]ketanserine binding : 7.70, 7.36 and 7.70, respectively).

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