2. Academic Validation
  3. Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. 4. Opioid receptor binding properties of 8-[N-(4'-phenyl)-phenethyl)carboxamido] analogues of cyclazocine and ethylketocycalzocine

Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. 4. Opioid receptor binding properties of 8-[N-(4'-phenyl)-phenethyl)carboxamido] analogues of cyclazocine and ethylketocycalzocine

  • J Med Chem. 2006 Sep 7;49(18):5635-9. doi: 10.1021/jm060278n.
Mark P Wentland 1,  Melissa VanAlstine,  Robert Kucejko,  Rongliang Lou,  Dana J Cohen,  Amy L Parkhill,  Jean M Bidlack
Affiliations

Affiliation

  • 1 Department of Chemistry and Chemical Biology, Rensselaer Polytechnic Institute, Troy, New York 12180, USA. [email protected]
PMID: 16942039 DOI: 10.1021/jm060278n
Abstract

The synthesis and evaluation of a series of aryl-containing N-monosubstituted analogues of the lead compound 8-carboxamidocyclazocine were performed to probe a putative hydrophobic binding pocket of opioid receptors. High binding affinity to mu, kappa, and delta opioid receptors was observed for the 8-[N-(4'-phenyl)-phenethyl)carboxamido] analogue.

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