TY - JOUR T1 - Identification of the first trans-(3R,4R)- dimethyl-4-(3-hydroxyphenyl)piperidine derivative to possess highly potent and selective opioid kappa receptor antagonist activity. AU - Thomas,J B, AU - Atkinson,R N, AU - Rothman,R B, AU - Fix,S E, AU - Mascarella,S W, AU - Vinson,N A, AU - Xu,H, AU - Dersch,C M, AU - Lu,Y, AU - Cantrell,B E, AU - Zimmerman,D M, AU - Carroll,F I, PY - 2001/8/10/pubmed PY - 2001/9/8/medline PY - 2001/8/10/entrez SP - 2687 EP - 90 JF - Journal of medicinal chemistry JO - J Med Chem VL - 44 IS - 17 N2 - 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 K(i) = 0.3 nM) and highly potent and selective kappa antagonism in the [(35)S]GTP-gamma-S assay using cloned opioid receptors (kappa K(i) = 0.006 nM, mu/kappa ratio = 570, delta/kappa ratio > 16600). SN - 0022-2623 UR - https://www.unboundmedicine.com/medline/citation/11495579/Identification_of_the_first_trans__3R4R___dimethyl_4__3_hydroxyphenyl_piperidine_derivative_to_possess_highly_potent_and_selective_opioid_kappa_receptor_antagonist_activity_ L2 - https://doi.org/10.1021/jm015521r DB - PRIME DP - Unbound Medicine ER -