Discovery of N-{4-[(3-Hydroxyphenyl)-3-methylpiperazin-1-yl] methyl-2-methylpropyl}-4-phenoxybenzamide Analogues as Selective Kappa Opioid Receptor …
…, JB Thomas, LE Brieaddy, SW Mascarella…
Index: Kormos, Chad M.; Jin, Chunyang; Cueva, Juan Pablo; Runyon, Scott P.; Thomas, James B.; Brieaddy, Lawrence E.; Mascarella, S. Wayne; Navarro, Hernan A.; Gilmour, Brian P.; Carroll, F. Ivy Journal of Medicinal Chemistry, 2013 , vol. 56, # 11 p. 4551 - 4567
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Citation Number: 6
Abstract
There is continuing interest in the discovery and development of new κ opioid receptor antagonists. We recently reported that N-substituted 3-methyl-4-(3-hydroxyphenyl) piperazines were a new class of opioid receptor antagonists. In this study, we report the syntheses of two piperazine JDTic-like analogues. Evaluation of the two compounds in an in vitro [35S] GTPγS binding assay showed that neither compound showed the high potency ...
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