Lack of effect of gamma-hydroxybutyrate on mu, delta and kappa opioid receptor binding.
gamma-Hydroxybutyrate (GHB) and morphine induce a number of similar effects. Moreover, the effects they elicit can be reversed by the opiate antagonist naloxone (NX), suggesting that GHB may produce at least some of its central effects by acting as an opiate agonist. The present study considered this possibility by examining the effect of GHB on mu, delta, and kappa-opioid receptor binding in concentrations of 1 nM-0.1 mM. GHB was inactive in each instance, at every dose examined. GHB is consequently not a direct opiate receptor agonist. It is also unlikely to be an indirect (enkephalin or dynorphin release-stimulating) agonist. The mechanism of action involved whereby NX can reverse the effects of GHB must therefore not involve opioid mechanisms; at least not directly.
Feigenbaum
J J
JJ
Department of Research and Development, American Institute of Biotechnology, Illinois, IL 60007-3840, USA.
Simantov
R
R
D000759:Adjuvants, Anesthesia / Q000494:pharmacology*; D000700:Analgesics / Q000494:pharmacology; D000818:Animals; D004174:Diprenorphine / Q000494:pharmacology; D020875:Enkephalin, Ala(2)-MePhe(4)-Gly(5)-; D004745:Enkephalins / Q000494:pharmacology; D005048:Etorphine / Q000494:pharmacology; D005910:Glioma; D006168:Guinea Pigs; D009270:Naloxone / Q000494:pharmacology; D009292:Narcotic Antagonists / Q000494:pharmacology; D009294:Narcotics / Q000494:pharmacology; D009447:Neuroblastoma; D011957:Receptors, Opioid / Q000819:agonists / Q000378:metabolism*; D017465:Receptors, Opioid, delta / Q000819:agonists / Q000037:antagonists & inhibitors / Q000378:metabolism; D017473:Receptors, Opioid, kappa / Q000819:agonists / Q000037:antagonists & inhibitors / Q000378:metabolism; D017450:Receptors, Opioid, mu / Q000819:agonists / Q000037:antagonists & inhibitors / Q000378:metabolism; D012978:Sodium Oxybate / Q000494:pharmacology*; D014316:Tritium; D014407:Tumor Cells, Cultured / Q000737:chemistry / Q000187:drug effects
D000759:Adjuvants, Anesthesia; D000700:Analgesics; D004745:Enkephalins; D009292:Narcotic Antagonists; D009294:Narcotics; D011957:Receptors, Opioid; D017465:Receptors, Opioid, delta; D017473:Receptors, Opioid, kappa; D017450:Receptors, Opioid, mu; D014316:Tritium; D020875:Enkephalin, Ala(2)-MePhe(4)-Gly(5)-; D004174:Diprenorphine; D009270:Naloxone; D005048:Etorphine; D012978:Sodium Oxybate