Exploring delta-receptor function using the selective opioid antagonist naltrindole.
Until recently the only pharmacological probes for delta-receptors have been peptide enkephalin analogues. These suffer from a number of limitations including high cost, partial agonist effects and a propensity for neurotoxicity. A stable non-peptide antagonist, naltrindole, has recently become available. We have explored its intrinsic actions and found that it attenuated swim stress-induced antinociception, a model for endogenous delta-receptor activation. Naltrindole may therefore be a useful alternative to presently available delta-receptor antagonists.
Jackson
H C
HC
Reckitt and Colman Psychopharmacology Unit, School of Medical Sciences, Bristol, England.
Ripley
T L
TL
Nutt
D J
DJ
D000818:Animals; D001522:Behavior, Animal / Q000187:drug effects; D007211:Indoles / Q000494:pharmacology*; D008297:Male; D009019:Morphinans / Q000494:pharmacology*; D009271:Naltrexone / Q000031:analogs & derivatives*; D009292:Narcotic Antagonists / Q000494:pharmacology*; D010146:Pain / Q000503:physiopathology; D051381:Rats; D011919:Rats, Inbred Strains; D011957:Receptors, Opioid / Q000187:drug effects* / Q000502:physiology; D017465:Receptors, Opioid, delta; D013315:Stress, Psychological / Q000503:physiopathology
D007211:Indoles; D009019:Morphinans; D009292:Narcotic Antagonists; D011957:Receptors, Opioid; D017465:Receptors, Opioid, delta; D009271:Naltrexone; C055382:naltrindole