Pharmacological properties of bivalent ligands containing butorphan linked to nalbuphine, naltrexone, and naloxone at mu, delta, and kappa opioid receptors.
Article Details
- CitationCopy to clipboard
Peng X, Knapp BI, Bidlack JM, Neumeyer JL
Pharmacological properties of bivalent ligands containing butorphan linked to nalbuphine, naltrexone, and naloxone at mu, delta, and kappa opioid receptors.
J Med Chem. 2007 May 3;50(9):2254-8. Epub 2007 Apr 4.
- PubMed ID
- 17407276 [ View in PubMed]
- Abstract
Our investigation of bivalent ligands at mu, delta, and kappa opioid receptors is focused on the preparation of ligands containing kappa agonist and mu agonist/antagonist pharmacophores at one end joined by a chain containing the mu antagonist pharmacophores (naltrexone, naloxone, or nalbuphine) at the other end. These ligands were evaluated in vitro by their binding affinity at mu, delta, and kappa opioid receptors and their relative efficacy in the [35S]GTPgammaS assay.
DrugBank Data that Cites this Article
- Drug Targets
Drug Target Kind Organism Pharmacological Action Actions Nalbuphine Kappa-type opioid receptor Protein Humans YesAgonistDetails Nalbuphine Mu-type opioid receptor Protein Humans YesAntagonistDetails - Binding Properties
Drug Target Property Measurement pH Temperature (°C) Nalbuphine Kappa-type opioid receptor EC 50 (nM) 27 N/A N/A Details Nalbuphine Kappa-type opioid receptor Ki (nM) 2.2 N/A N/A Details Nalbuphine Mu-type opioid receptor IC 50 (nM) 110 N/A N/A Details Nalbuphine Mu-type opioid receptor Ki (nM) 0.89 N/A N/A Details Nalbuphine Mu-type opioid receptor EC 50 (nM) 14 N/A N/A Details Naloxone Kappa-type opioid receptor IC 50 (nM) 320 N/A N/A Details Naloxone Kappa-type opioid receptor EC 50 (nM) 10 N/A N/A Details Naloxone Kappa-type opioid receptor Ki (nM) 1.1 N/A N/A Details Naloxone Mu-type opioid receptor IC 50 (nM) 23 N/A N/A Details Naloxone Mu-type opioid receptor Ki (nM) 0.79 N/A N/A Details