Compounds > enkephalin--ala(2)-mephe(4)-gly(5)-

enkephalin--ala(2)-mephe(4)-gly(5)- and noribogaine

enkephalin--ala(2)-mephe(4)-gly(5)- has been researched along with noribogaine* in 2 studies

Other Studies

2 other study(ies) available for enkephalin--ala(2)-mephe(4)-gly(5)- and noribogaine

Article	Year
Noribogaine stimulates naloxone-sensitive [35S]GTPgammaS binding. Neuroreport, 1998, Jan-05, Volume: 9, Issue:1 Noribogaine is formed in vivo by the O-demethylation of the indole alkaloid ibogaine. We report here that noribogaine acts as a full agonist at the mu-opioid receptor. Noribogaine-stimulated guanylyl 5'gamma-[35S]thio]triphosphate ([35S]GTPgammaS) was studied in rat thalamic membranes to measure activation of guanine nucleotide binding proteins (G-proteins) in the presence of excess GDP. Noribogaine caused a 170% increase above basal [35S]GTPgammaS binding at sub-micromolar effective concentrations (EC50) in a naloxone-sensitive manner, confirming that this effect was an opioid receptor-mediated process. The level of intrinsic activity for noribogaine in these assays was comparable to the full agonists DAMGO and morphine. In contrast, ibogaine had no significant effect on [35S]GTPgammaS binding over a similar concentration range. The efficacy of noribogaine as a full mu-opioid agonist may explain ibogaine's ability to block the acute signs of opiate withdrawal and its suppressive effects on morphine self-administration. Topics: Animals; Binding, Competitive; Enkephalin, Ala(2)-MePhe(4)-Gly(5)-; Enkephalins; Guanosine 5'-O-(3-Thiotriphosphate); Ibogaine; Logistic Models; Male; Naloxone; Radioligand Assay; Rats; Rats, Sprague-Dawley; Receptors, Opioid, mu; Stimulation, Chemical; Sulfur Radioisotopes	1998
Radioligand-binding study of noribogaine, a likely metabolite of ibogaine. Brain research, 1995, Mar-27, Volume: 675, Issue:1-2 Radioligand-binding studies were performed to ascertain the actions of noribogaine, a suspected metabolite of ibogaine, on opioid receptors. Consistent with previous results, ibogaine showed highest affinity for kappa opioid receptors (Ki = 3.77 +/- 0.81 microM), less affinity for mu receptors (Ki = 11.04 +/- 0.66 microM) and no affinity for delta receptors (Ki > 100 microM). Noribogaine showed a higher affinity than ibogaine for all of the opioid receptors: kappa Ki = 0.96 +/- 0.08 microM, mu Ki = 2.66 +/- 0.62 microM and delta Ki = 24.72 +/- 2.26 microM. These data suggest that noribogaine is active in vivo and that it may contribute to ibogaine's pharmacological effects. Topics: Analgesics; Animals; Benzeneacetamides; Cattle; Cerebral Cortex; Enkephalin, Ala(2)-MePhe(4)-Gly(5)-; Enkephalin, D-Penicillamine (2,5)-; Enkephalins; Ibogaine; In Vitro Techniques; Kinetics; Naloxone; Pyrrolidines; Radioligand Assay; Receptors, Opioid	1995

Article

Year

Noribogaine stimulates naloxone-sensitive [35S]GTPgammaS binding.

Neuroreport, 1998, Jan-05, Volume: 9, Issue:1

Noribogaine is formed in vivo by the O-demethylation of the indole alkaloid ibogaine. We report here that noribogaine acts as a full agonist at the mu-opioid receptor. Noribogaine-stimulated guanylyl 5'gamma-[35S]thio]triphosphate ([35S]GTPgammaS) was studied in rat thalamic membranes to measure activation of guanine nucleotide binding proteins (G-proteins) in the presence of excess GDP. Noribogaine caused a 170% increase above basal [35S]GTPgammaS binding at sub-micromolar effective concentrations (EC50) in a naloxone-sensitive manner, confirming that this effect was an opioid receptor-mediated process. The level of intrinsic activity for noribogaine in these assays was comparable to the full agonists DAMGO and morphine. In contrast, ibogaine had no significant effect on [35S]GTPgammaS binding over a similar concentration range. The efficacy of noribogaine as a full mu-opioid agonist may explain ibogaine's ability to block the acute signs of opiate withdrawal and its suppressive effects on morphine self-administration.

Topics: Animals; Binding, Competitive; Enkephalin, Ala(2)-MePhe(4)-Gly(5)-; Enkephalins; Guanosine 5'-O-(3-Thiotriphosphate); Ibogaine; Logistic Models; Male; Naloxone; Radioligand Assay; Rats; Rats, Sprague-Dawley; Receptors, Opioid, mu; Stimulation, Chemical; Sulfur Radioisotopes

1998

Radioligand-binding study of noribogaine, a likely metabolite of ibogaine.

Brain research, 1995, Mar-27, Volume: 675, Issue:1-2

Radioligand-binding studies were performed to ascertain the actions of noribogaine, a suspected metabolite of ibogaine, on opioid receptors. Consistent with previous results, ibogaine showed highest affinity for kappa opioid receptors (Ki = 3.77 +/- 0.81 microM), less affinity for mu receptors (Ki = 11.04 +/- 0.66 microM) and no affinity for delta receptors (Ki > 100 microM). Noribogaine showed a higher affinity than ibogaine for all of the opioid receptors: kappa Ki = 0.96 +/- 0.08 microM, mu Ki = 2.66 +/- 0.62 microM and delta Ki = 24.72 +/- 2.26 microM. These data suggest that noribogaine is active in vivo and that it may contribute to ibogaine's pharmacological effects.

Topics: Analgesics; Animals; Benzeneacetamides; Cattle; Cerebral Cortex; Enkephalin, Ala(2)-MePhe(4)-Gly(5)-; Enkephalin, D-Penicillamine (2,5)-; Enkephalins; Ibogaine; In Vitro Techniques; Kinetics; Naloxone; Pyrrolidines; Radioligand Assay; Receptors, Opioid

1995