Serotonin transporter inhibitors: synthesis and binding potency of 2′-methyl- and 3′-methyl-6-nitroquipazine
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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.
Gerdes, J. M., DeFina, S. C., Wilson, P. A., & Taylor, S. E. (2000). Serotonin transporter inhibitors: synthesis and binding potency of 2′-methyl- and 3′-methyl-6-nitroquipazine. Bioorganic & Medicinal Chemistry Letters, 10(23), 2643–2646. https://doi.org/10.1016/s0960-894x(00)00546-1
Bioorganic & Medicinal Chemistry Letters
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