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Bioorg. Med. Chem. Lett. · Oct 2001
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.
- J L Neumeyer, X H Gu, L A van Vliet, N J DeNunzio, D E Rusovici, D J Cohen, S S Negus, N K Mello, and J M Bidlack.
- Alcohol and Drug Abuse Research Center, McLean Hospital, Harvard Medical School, 115 Mill Street, Belmont, MA 02478, USA. neumeyer@mclean.harvard.edu
- Bioorg. Med. Chem. Lett. 2001 Oct 22;11(20):2735-40.
AbstractA 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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