(-)-Pentazocine analgesia in mice: interactions with a sigma receptor system.
Article Details
- CitationCopy to clipboard
Chien CC, Pasternak GW
(-)-Pentazocine analgesia in mice: interactions with a sigma receptor system.
Eur J Pharmacol. 1995 Dec 27;294(1):303-8.
- PubMed ID
- 8788445 [ View in PubMed]
- Abstract
(-)-Pentazocine is active in the tailflick assay in CD-1 mice, although it shows a biphasic dose-response curve with a peak effect of only 30%. Co-administration of haloperidol shifts the dose-response curve to the left and elevates the maximal response to 70% through a blockade of sigma 1 receptors, but the curve remains biphasic. (+)-Pentazocine is inactive in all antinociceptive assays, either alone or with haloperidol. The analgesic actions of (-)-pentazocine are readily reversed by nor-binaltorphimine, but not by the mu-selective opioid receptor antagonist beta-funaltrexamine, implying a kappa 1-opioid receptor mechanism of action. This conclusion is supported by the ability of antisense oligodeoxynucleotides directed against the KOR-1 clone, which encodes the kappa 1-opioid receptor, to block (-)-pentazocine analgesia.
DrugBank Data that Cites this Article
- Drug Targets
Drug Target Kind Organism Pharmacological Action Actions Pentazocine Kappa-type opioid receptor Protein Humans YesAgonistDetails Pentazocine Sigma non-opioid intracellular receptor 1 Protein Humans YesAgonistDetails