enkephalin--ala(2)-mephe(4)-gly(5)- has been researched along with fentanyl-isothiocyanate* in 2 studies
2 other study(ies) available for enkephalin--ala(2)-mephe(4)-gly(5)- and fentanyl-isothiocyanate
| Article | Year |
|---|---|
Fentanyl isothiocyanate reveals the existence of physically associated mu- and delta-opioid receptors mediating inhibition of adenylate cyclase in rat neostriatum.
Dopamine D-1 receptor-stimulated cyclic AMP efflux from superfused rat neostriatal slices was strongly inhibited by the delta-opioid receptor agonist, [D-Pen2, D-Pen5]enkephalin (DPDPE, 1 microM), and by the mu-opioid receptor agonist, [D-Ala2,MePhe4,Gly-ol5]enkephalin (DAGO, 1 microM). Naloxone (0.1 microM) fully antagonized the inhibitory effect of DAGO, leaving that of DPDPE virtually unchanged. Preincubation of the slices with the irreversible delta receptor ligand, fentanyl isothiocyanate (FIT, 1 microM) did not affect the inhibitory effect of DAGO, but prevented that of DPDPE. Naloxone no longer antagonized the inhibitory effect of DAGO when the delta receptors were selectively and irreversibly blocked by FIT. These data indicate that FIT and naloxone, acting on delta and mu receptors, respectively, may share a common binding site, suggesting the involvement of a functional mu, delta-opioid receptor-complex. Topics: Adenylyl Cyclase Inhibitors; Animals; Caudate Nucleus; Cyclic AMP; Enkephalin, Ala(2)-MePhe(4)-Gly(5)-; Enkephalin, D-Penicillamine (2,5)-; Enkephalins; Fentanyl; In Vitro Techniques; Isothiocyanates; Male; Putamen; Rats; Rats, Inbred Strains; Receptors, Dopamine; Receptors, Opioid; Receptors, Opioid, delta; Receptors, Opioid, mu | 1988 |
Tritiated-6-beta-fluoro-6-desoxy-oxymorphone: a highly selective ligand for the opiate mu receptor whose binding is characterized by low nonspecific binding.
In this paper we examine the binding of [3H]FOXY (tritiated-6-beta-fluoro-6-desoxy-oxymorphone) to membranes of rat brain. Using the site-directed alkylating agents BIT and FIT, evidence is presented that [3H]FOXY selectively labels mu opiate binding sites in vitro. Further, BIT and FIT did not significantly affect [3H]bremazocine binding to kappa receptors. Scatchard plots of [3H]FOXY binding were somewhat curvilinear, suggesting the presence of two classes of mu binding sites. At concentrations up to 19 nM, 90 percent of the total binding was specific. The combination of high mu-selectivity and low nonspecific binding suggests the [3H]FOXY may prove to be a powerful tool for studying the opiate mu receptor. Topics: Animals; Benzomorphans; Brain; Enkephalin, Ala(2)-MePhe(4)-Gly(5)-; Enkephalin, Leucine; Enkephalin, Leucine-2-Alanine; Enkephalins; Fentanyl; Hydromorphone; Isothiocyanates; Kinetics; Oxymorphone; Rats; Receptors, Opioid; Receptors, Opioid, mu; Thiocyanates; Tomography, Emission-Computed | 1984 |