geoscience.net logo
+ Resolve Article
+ Follow Us
Follow on FacebookFollow on Facebook
Follow on TwitterFollow on Twitter

+ Translate
+ Subscribe to Site Feed
GeoScience Most Shared ContentMost Shared Content

Irreversible opiate agonists and antagonists. III. Phenylhydrazone derivatives of naloxone and oxymorphone


, : Irreversible opiate agonists and antagonists. III. Phenylhydrazone derivatives of naloxone and oxymorphone. Journal of Pharmacology and Experimental Therapeutics 235(3): 846-850

In view of previous studies indicating that the irreversible properties of opiate azines such as naloxonazine are not due to a bivalent mechanism, we have synthesized a series of opiate hydrazones. In standard competition assays which measure both reversible and irreversible inhibition of binding, the hydrazone derivatives lowered radiolabeled opioid binding almost as well as naloxone and oxymorphone. However, the phenylhydrazone derivatives produced a profound wash-resistant inhibition of binding. The similar potencies of the methylhydrazine and phenylhydrazine derivatives in standard competition studies contrasted significantly with their effectiveness in eliciting wash-resistant inhibition of binding, suggesting the importance of the phenyl group in the production of wash-resistant inhibition. The p-nitrophenyl hydrazones were the most effective wash-irreversible inhibitors. Although oxymorphoazine does not irreversibly inhibit radiolabeled opioid binding as effectively as naloxonazine or naltrexonazine, the oxymorphone phenylhydrazones were as potent as their corresponding naloxone compounds. Incubation of [3H] naloxone-p-nitrophenylhydrazone with albumin demonstrated significant incorporation of radiolabel into the protein after sodium dodecylsulfate gel electrophoresis. This suggests that the phenylhydrazones have significant reactivities toward proteins and might produce their irreversible actions through covalent interactions.

US$29.90

PMID: 2416910


Other references

Reme, C.; Reinboth, J.; Clausen, M.; Hafezi, F., 1996: Light damage revisited: Converging evidence, diverging views. Are observations on ultraviolet (UV)- and visible light-induced ocular changes in animals relevant for human pathology? Different conclusions are drawn by different groups, depending on their perspective: while in the epidemiologist's view th...

van Niekerk, C.C.; Vooijs, P.; Casparie-van Velsen, I.J.; Poels, L.G., 1997: Differentiation margins of ovarian tumor pathology: first incidences of epithelial ovarian tumors monitored by marker antibodies. The first incidence of ovarian tumors in The Netherlands was analyzed during the PALGA data. The first incidences of benign epithelial ovarian tumors reach a plateau, at a level of 60 to 65 cases per 100,000 women beyond the age of 40 years. The b...

Blyandur, O.V. (Ed), 1978: The electrophysiology of maize. This book contains the results of many years' work on the electrical properties of maize in relation to breeding and genetics. Data are included on the relationship between the genetical characteristics of plants and their electrical properti...

Howlett, F.; Morley, M.J.an; Urquhart, A.R., 1942: The chemical analysis of fibre mixtures. The same general procedure is used for all combinations of fibers[long dash]one component is dissolved from the mixture and after suitable washing and drying the remaining insoluble component is weighed. Two stipulations are given: (1) It is assum...

Gleichmann, W.; Weise, M.; Matthes, K.J., 1976: Serum prealbumin and haptoglobin in acute hepatitis. Verhandlungen der Deutschen Gesellschaft für Innere Medizin 82 Pt 1: 422-425

Batra, P.; Mangione, C.M.; Cheng, E.; Steers, W.Neil.; Nguyen, T.A.; Bell, D.; Kuo, A.A.; Gregory, K.D., 2017: A Cluster Randomized Controlled Trial of the MyFamilyPlan Online Preconception Health Education Tool. To evaluate whether exposure to MyFamilyPlan-a web-based preconception health education module-changes the proportion of women discussing reproductive health with providers at well-woman visits. Cluster randomized controlled trial. One hundred thi...

Golden, J.; Mahaffey, R.A.; Pasour, J.A.; Young, F.C.; Kapetanakos, C.A., 1978: Intense proton beam current measurement via prompt gamma rays from nuclear reactions. The current of an intense, pulsed proton beam is experimentally determined by monitoring prompt gamma rays from nuclear reactions induced in a suitable target. Relevant data are given on the reactions employed including (7)Li(p,gamma) (8)Be, (19)F...

Broda, E.; Findenegg, G.R., 1967: Specificity of zinc uptake by Chlorella. The competition of various cations with labelled zinc in the active (metabolic) uptake of the latter by Chlorella was measured. The series obtained does not coincide with that of the passive uptake in the same system, and the specificity is higher...

Limcangco-Lopez, P.D., 1967: Selenium meta-bolism in lambs fed varying selenium intakes. Lambs were given diets with 0.01, 0.26 and 0.51 or 5.01 ppm Se. Poorer growth and efficiency of feed conversion at the extreme levels was indicative of marginal signs of deficiency and toxicity. The uptake of 75Se by red blood cells from the lambs...

Zalocar D.D.mitrovic, Y.; Casco, S.L.; Asselborn, V.M., 1998: Estudio de la biomasa y diversidad del fitoplancton de la laguna Paiva, Corrientes, Argentina. Physis Buenos Aires1998) Diciembre; 55(128-129): Section B: 1-13