+ Translate

Spectrum of the mu binding sites delta binding sites and kappa binding sites in homogenates of rat brain

, : Spectrum of the mu binding sites delta binding sites and kappa binding sites in homogenates of rat brain. British Journal of Pharmacology 77(3): 461-468

In homogenates of rat brain, the binding characteristics of tritiated opiates and opioid peptides were examined and the relative capacities of .mu.-, .delta.- and .kappa.-binding sites of the opiate receptor were determined by saturation analysis. In competition experiments, binding of the selective .mu.-ligand [3H]-[D-Ala2,MePhe4,Gly-ol5]enkephalin at the .mu.-site was displaced by [D-Ala2,D-Leu5]enkephalin with rather low affinity (KI [inhibition constant] = 12.6 nM) and more readily by the ketazocine-like compounds (-)-ethylketazocine (KI = 3.1 nM) and (-)-bremazocine (KI = 0.32 nM), which also displaced the binding of [3H]-[D-Ala2,D-Leu5]enkephalin from the .delta.-site. The binding to the .kappa.-site was easily displaced by ethylketazocine (1.0 nM) and bremazocine (0.37 nM) but not by the .mu.-ligand [D-Ala2,MePhe4,Gly-ol5]enkephalin (KI = 2000-3000 nM) or the .delta.-ligand [D-Ala2,D-Leu5]enkephalin (KI > 20,000 nM). Kd and the binding capacity (pmol/g) of the .mu.-binding site were determined with the selective .mu.-ligand [3H]-[D-Ala2,MePhe4,Gly-ol5]enkephalin. For the .delta.-site, [3H]-[D-Ala2, D-Leu5]enkephalin was used in the presence of unlabeled [D-Ala2,MePhe4,Gly-ol5]enkephalin in order to suppress cross-reactivity to the .mu.-binding site. For the estimation of .delta.-binding, [3H]-(.+-.)-ethylketazocine or [3H]-(-)-bremazocine were used in the presence of unlabeled .mu.- and .delta.-ligands for the suppression of cross-reactivities to the .mu.- and .delta.-binding sites. In rat brain the capacity of the .mu.-binding site was 7.3 pmol/g brain, that of the .kappa.-binding site 6.7 pmol/g brain and that of the .delta.-binding site 2.0 pmol/g brain. The .kappa.-binding site had the lowest value whereas in the guinea-pig brain the capacity of the .mu.-binding site was lower than that of the .delta.- or .kappa.-binding site.

(PDF 0-2 workdays service)

Order PDF Full Text


Click here to order any other PDF Full Text

Accession: 006461260

PDF Full Text: Submit

Submit PDF Full Text

No spam - Every submission is manually reviewed

Due to poor quality, we do not accept files from Researchgate

Submitted PDF Full Texts will always be free for everyone
(We only charge for PDFs that we need to acquire)

Select a PDF file:

Other references

Eisenhart, C.; Wilson, P. W., 1943: Statistical Methods and Control in Bacteriology. The following statistical methods are described with special reference to bacteriological data: -(1) tests of agreement of observed distributions of bacterial counts with theoretical distributions based on the binomial distribution or Poisson seri...

Doherty, Jennifer A.; Weiss, Noel S.; Dightman, Douglas; Houck, John; Chen, Chu, 2001: Polymorphisms in CYP1A1, CYP1A2, CYP1B1, and COMT and risk of endometrial cancer. Proceedings of the American Association for Cancer Research Annual Meeting 42: 499, March

Lutz, M; Bauer, R; Begerow, D; Oberwinkler, F., 2004: Tuberculina-Thanatophytum. Mycological research 108(3): 227-238

Agrawal N.M.; Roth S.; Graham D.Y.; White R.H.; Germain B.; Brown J.A.; Stromatt S.C., 1991: Misoprostol compared with sucralfate in the prevention of nonsteroidal anti inflammatory drug induced gastric ulcer a randomized controlled trial. Objectives: To compare the efficacy and frequency of adverse experiences of misoprostol and sucralfate in the prevention of gastric ulcers in patients receiving nonsteroidal anti-inflammatory drug (NSAID) therapy. Design: A prosepctive, randomized...

Garcia Asua, Guillermo; Cogdell, Richard J.; Hunter, C. Neil, 2002: Functional assembly of the foreign carotenoid lycopene into the photosynthetic apparatus of Rhodobacter sphaeroides, achieved by replacement of the native 3-step phytoene desaturase with its 4-step counterpart from Erwinia herbicola. Photosynthetic organisms synthesize a diverse range of carotenoids. These pigments are important for the assembly, function and stability of photosynthetic pigment-protein complexes, and they are used to quench harmful radicals. The photosynthetic...

Zanobini A.; Firenzuoli A.M., 1974: Quantitative analysis of free and bound iron in spinach. Bollettino Societa Italiana Biologia Sperimentale 50(12): 892-894

Kol'tsova, M. M., 1976: Differences in physiological characteristics of conditioned connection systems in gradual and instantaneous conditioning. Two types of system formation, with gradual and instantaneous conditioning are described. The 1st type is characterized by inertia, which is linked with high intensity of the developing conditioned tonic excitation. In the other type, the system i...

Gylling, H.; Miettinen, T. A., 1995: Soluble and insoluble fecal bile acids. Gastroenterology 108(4 SUPPL ): A1078

Louis C., 1982: Ground water and seepage problems; report on current knowledge and general report. Proceedings of the International Conference on Soil Mechanics and Foundation Engineering = Comptes Rendus du Congres International de Mecanique des Sols et des Travaux de Fondations: ol. 4; Pages 277-290. 1982.

Haertel, M.; Zaunbauer, W., 1996: Radiodiagnosis of gastrointestinal lymphoma. Radiological synopsis of primary gastrointestinal lymphoma depends on the growth direction and dynamism of the tumor, i.e. grade of malignancy and stage of the pathological process at diagnosis. Initial nodal-polypoid lesions, because of their muc...