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Bioorg Med Chem Lett. 2001 Jul 9;11(13):1741-3.

Piperazinyl benzamidines: synthesis and affinity for the delta opioid receptor.

Author information

1
Drug Discovery Division, R. W. Johnson Pharmaceutical Research Institute, Welsh and McKean Roads, 19477, Spring House, PA, USA. snortey@prius.jnj.com

Abstract

Piperazinyl benzamidines were prepared and found to bind to the rat delta (delta) opioid receptor. The most active compounds had a N,N-diethylcarboxamido group and a N-benzyl piperazine. The most potent among these was N,N-diethyl-4-[4-(phenylmethyl)-1-piperazinyl][2-(trifluoromethyl)phenyl]iminomethyl]benzamide (27) with a 1.22nM K(i) for the rat delta opioid receptor and ca. 1000 x selectivity relative to the mu opioid subtype.

PMID:
11425550
DOI:
10.1016/s0960-894x(01)00272-4
[Indexed for MEDLINE]

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