• Journal Article

2 beta-substituted analogues of cocaine. Synthesis and inhibition of binding to the cocaine receptor

Citation

Lewin, A., Gao, Y. G., Abraham, P., Boja, J. W., Kuhar, M. J., & Carroll, F. (1992). 2 beta-substituted analogues of cocaine. Synthesis and inhibition of binding to the cocaine receptor. Journal of Medicinal Chemistry, 35(1), 135-140.

Abstract

The potencies of a series of 2 beta-substituted cocaine analogues to displace [3H]-3 beta-(p-fluorophenyl)tropane-2 beta-carboxylic acid methyl ester binding in rat striatal membranes demonstrate the requirement for a 2 beta-substituent with two hydrogen-bond acceptors. The insensitivity of the ester moiety to steric and electronic factors suggests its modification to provide site-specific irreversible ligands