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.
Article Details
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Neumeyer JL, Gu XH, van Vliet LA, DeNunzio NJ, Rusovici DE, Cohen DJ, Negus SS, Mello NK, Bidlack JM
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.
Bioorg Med Chem Lett. 2001 Oct 22;11(20):2735-40.
- PubMed ID
- 11591513 [ View in PubMed]
- Abstract
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.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Levorphanol Kappa-type opioid receptor Ki (nM) 2.3 N/A N/A Details Levorphanol Mu-type opioid receptor Ki (nM) 0.21 N/A N/A Details