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Probes for narcotic receptor-mediated phenomena. 25. Synthesis and evaluation of N-alkyl-substituted (alpha-piperazinylbenzyl) benzamides as novel, highly selective delta opioid receptor agonists

Katsura, Y.; Zhang, X.; Homma, K.; Rice, K.C.; Calderon, S.N.; Rothman, R.B.; Yamamura, H.I.; Davis, P.; Flippen-Anderson, J.L.; Xu, H.; Becketts, K.; Foltz, E.J.; Porreca, F.

Journal of Medicinal Chemistry 40(18): 2936-2947

1997


ISSN/ISBN: 0022-2623
PMID: 9288176
DOI: 10.1021/jm970106d
Accession: 009247319

A series of N-alkyl- and N,N-dialkyl-4-(alpha-((2S,5R)-4-allyl-2,5-dimethyl-1-piperazinyl)benzyl)benzamides were synthesized and evaluated for binding affinities at mu, delta, and kappa opioid receptor subtypes. Several compounds (2e,f,h,i,m) strongly bound to the delta receptor with IC-50 values in the nanomolar range.

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