| 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 σ1 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 μ-selective opioid receptor antagonist β-funaltrexamine, implying a κ1-opioid receptor mechanism of action. This conclusion is supported by the ability of antisense oligodeoxynucleotides directed against the KOR-1 clone, which encodes the κ1-opioid receptor, to block (-)-pentazocine analgesia. © 1995 Elsevier Science B.V. All rights reserved. |
| Keywords: |
controlled study; unclassified drug; dose response; nonhuman; mouse; animals; mice; haloperidol; animal experiment; dose-response relationship, drug; drug antagonism; base sequence; morphine; analgesics, opioid; analgesia; mu opiate receptor antagonist; receptors, opioid, mu; tail flick test; beta funaltrexamine; enkephalin[2,5 dextro penicillamine]; oligonucleotides, antisense; reaction time; opioid receptor; pentazocine; receptors, opioid, delta; receptors, sigma; 3,4 dichloro n methyl n [2 (1 pyrrolidinyl)cyclohexyl]benzeneacetamide methanesulfonate; kappa opiate receptor; radioligand; antisense oligodeoxynucleotide; antisense; dopamine antagonists; subcutaneous drug administration; norbinaltorphimine; male; priority journal; article; sigma opiate receptor; enkephalin[2 dextro alanine 5 dextro leucine]; sulpiride; n methyl n [7 (1 pyrrolidinyl) 1 oxaspiro[4.5]dec 8 yl]benzeneacetamide; σ receptor; kor-1; κ-opioid analgesia; κ{script}-opioid receptor; kappa1 opiate receptor
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