1025918-05-1Relevant articles and documents
Piperazinomethyl tetralines: Synthesis and affinities for D1, D2 and 5- HT(2A) receptors
Ravina,Cid,Negreira,Castro,Moldes,G-Ferreiro,Rosa,MaCalleja,De Ceballos
, p. 1234 - 1237 (2007/10/03)
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-HT(2A) receptors was evaluated in vitro. The affinities of QF0105B and QF0106B for D2 receptors are less than that of haloperidol (pK(i)'s for inhibition of [3H]spiperone binding: 7.72, 7.06 and 8.30, respectively) but all three compounds have similar affinities for 5-HT(2A) receptors (pK(i)'s for inhibition of [3H]ketanserine binding: 7.70, 7.36 and 7.70, respectively).