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.

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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

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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