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Identification of the first trans-(3R,4R)-dimethyl-4-(3- hydroxyphenyl)piperidine derivative to possess highly potent and selective opioid kappa receptor antagonist activity
Thomas, J., Atkinson, R., Rothman, RB., Fix, S., Mascarella, S., Vinson, N., Xu, H., Dersch, CM., Lu, YF., Cantrell, BE., Zimmerman, DM., & Carroll, F. (2001). Identification of the first trans-(3R,4R)-dimethyl-4-(3- hydroxyphenyl)piperidine derivative to possess highly potent and selective opioid kappa receptor antagonist activity. Journal of Medicinal Chemistry, 44(17), 2687-2690. https://doi.org/10.1021/jm015521r
A structurally novel opioid kappa receptor selective ligand has been identified. This compound, (3R)-7-hydroxy- N-((1S)-1-{[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl] methyl}-2-methylpropyl)-1,2,3,4-tetrahydro-3-isoquinolinecarboxamide (JDTic, 10) demonstrated high affinity for the kappa receptor in the binding assay (kappa Ki ) 0.3 nM) and highly potent and selective kappa antagonism in the [35S]GTP-ç-S assay using cloned opioid receptors (kappa Ki ) 0.006 nM, u/kappa ratio ) 570, ä/kappa ratio > 16600).
