Pharmacological Properties of Bivalent Ligands Containing Butorphan Linked to Nalbuphine, Naltrexone, and Naloxone at μ, δ, and κ Opioid Receptors

Our investigation of bivalent ligands at μ, δ, and κ opioid receptors is focused on the preparation of ligands containing κ agonist and μ agonist/antagonist pharmacophores at one end joined by a chain containing the μ antagonist pharmacophores (naltrexone, naloxone, or nalbuphine) at the other end....

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Veröffentlicht in:	Journal of medicinal chemistry 2007-05, Vol.50 (9), p.2254-2258
Hauptverfasser:	Peng, Xuemei, Knapp, Brian I, Bidlack, Jean M, Neumeyer, John L
Format:	Artikel
Sprache:	eng
Schlagworte:	3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer - pharmacology Animals Biological and medical sciences CHO Cells Cricetinae Cricetulus Guanosine 5'-O-(3-Thiotriphosphate) - pharmacology Humans Ligands Medical sciences Morphinans - chemical synthesis Morphinans - chemistry Morphinans - pharmacology Nalbuphine - analogs & derivatives Nalbuphine - chemical synthesis Nalbuphine - pharmacology Naloxone - analogs & derivatives Naloxone - chemical synthesis Naloxone - pharmacology Naltrexone - analogs & derivatives Naltrexone - chemical synthesis Naltrexone - pharmacology Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems Pharmacology. Drug treatments Radioligand Assay Receptors, Opioid, delta - agonists Receptors, Opioid, delta - antagonists & inhibitors Receptors, Opioid, delta - drug effects Receptors, Opioid, kappa - agonists Receptors, Opioid, kappa - antagonists & inhibitors Receptors, Opioid, kappa - drug effects Receptors, Opioid, mu - agonists Receptors, Opioid, mu - antagonists & inhibitors Receptors, Opioid, mu - drug effects Structure-Activity Relationship
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Zusammenfassung:	Our investigation of bivalent ligands at μ, δ, and κ opioid receptors is focused on the preparation of ligands containing κ agonist and μ agonist/antagonist pharmacophores at one end joined by a chain containing the μ antagonist pharmacophores (naltrexone, naloxone, or nalbuphine) at the other end. These ligands were evaluated in vitro by their binding affinity at μ, δ, and κ opioid receptors and their relative efficacy in the [35S]GTPγS assay.
ISSN:	0022-2623 1520-4804
DOI:	10.1021/jm061327z