Serotonin transporter inhibitors: Synthesis and binding potency of 2'-methyl- and 3'-methyl-6-nitroquipazine
Racemic 2'-methyl- and 3'-methyl-6-nitroquipazine ligands were selected as targets, synthesized and evaluated at the serotonin transporter employing an in vitro competitive inhibition assay with [3H]paroxetine and rat cortical membrane. The 2'-methyl-6-nitroquipazine was found to be 50 times more potent than the 3'-methyl-substituted counterpart and of comparable potency to the known high affinity agent 5-iodo-6-nitroquipazine. (C) 2000 Elsevier Science Ltd.
Gerdes, John M.,DeFina, Steven C.,Wilson, Paul A.,Taylor, Scott E.
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