title: Intracerebroventricular administration of superFIT and its enantiomer to rats: evidence for in vivo acylation of [3H]DADL binding sites.
abstract: SuperFIT is an high affinity acylating ligand derived from fentanyl. Previous studies suggested that a selective acylation of delta receptors (J. Med. Chem. 29:1087-1093, 1986) resulted from exposure of membranes to this and structurally related compounds. We report in this preliminary study that intracerebroventricular administration of either superFIT or its enantiomer 18 to 24 hours prior to sacrifice decreased the subsequent binding of [3H]DADL to both its higher and lower affinity binding sites.
mesh_terms: D000215:Acylation; D000818:Animals; D002552:Cerebral Ventricles / Q000187:drug effects / Q000502:physiology*; D004743:Enkephalin, Leucine / Q000031:analogs & derivatives* / Q000378:metabolism; D016308:Enkephalin, Leucine-2-Alanine; D005283:Fentanyl / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000494:pharmacology; D007202:Indicators and Reagents; D007276:Injections, Intraventricular; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains; D011957:Receptors, Opioid / Q000187:drug effects / Q000378:metabolism*; D013237:Stereoisomerism
chemical_list: D007202:Indicators and Reagents; D011957:Receptors, Opioid; C046222:3-methylfentanyl isothiocyanate; D004743:Enkephalin, Leucine; D016308:Enkephalin, Leucine-2-Alanine; D005283:Fentanyl