Section 11
Chapter 10,993

Mixed kappa agonists and mu agonists/antagonists as potential pharmacotherapeutics for cocaine abuse: synthesis and opioid receptor binding affinity of N-substituted derivatives of morphinan

Neumeyer, J.L.; Gu, X.H.; van Vliet, L.A.; DeNunzio, N.J.; Rusovici, D.E.; Cohen, D.J.; Negus, S.S.; Mello, N.K.; Bidlack, J.M.

Bioorganic and Medicinal Chemistry Letters 11(20): 2735-2740


ISSN/ISBN: 0960-894X
PMID: 11591513
DOI: 10.1016/s0960-894x(01)00543-1
Accession: 010992459

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A series of new N-substituted derivatives of morphinan was synthesized and their binding affinity for the three opioid receptors (mu, delta, and kappa) was determined. A paradoxical effect of N-propargyl (MCL-117) and N-(3-iodoprop-(2E)-enyl) (MCL-118) substituents on the binding affinities for the mu and kappa opioid receptors was observed. All of these novel derivatives showed a preference for the mu and kappa versus delta binding.

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