EurekaMag.com logo
+ Site Statistics
References:
47,893,527
Abstracts:
28,296,643
+ Search Articles
+ Subscribe to Site Feeds
EurekaMag Most Shared ContentMost Shared
EurekaMag PDF Full Text ContentPDF Full Text
+ PDF Full Text
Request PDF Full TextRequest PDF Full Text
+ Follow Us
Follow on FacebookFollow on Facebook
Follow on TwitterFollow on Twitter
Follow on Google+Follow on Google+
Follow on LinkedInFollow on LinkedIn

+ 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.


Accession: 006461260

Submit PDF Full Text: Here


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:
Close
Close

Related references

Gillan, M.G.; Kosterlitz, H.W., 1982: Spectrum of the mu, delta- and kappa-binding sites in homogenates of rat brain. 1 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 determined by saturation analysis.2 In comp...

Gackenheimer, S.L.; Suter, T.M.; Pintar, J.E.; Quimby, S.J.; Wheeler, W.J.; Mitch, C.H.; Gehlert, D.R.; Statnick, M.A., 2005: Localization of opioid receptor antagonist [3H]-LY255582 binding sites in mouse brain: comparison with the distribution of mu, delta and kappa binding sites. Agonist stimulation of opioid receptors increases feeding in rodents, while opioid antagonists inhibit food intake. The pan-opioid antagonist, LY255582, produces a Sustained reduction in food intake and body weight in rodent models of obesity. How...

Robson L.E.; Paterson S.J.; Kosterlitz H.W., 1988: Modulation by salts of binding affinities and capacities at mu delta and kappa opioid binding sites in guinea pig brain. Society for Neuroscience Abstracts 14(1): 577

Kamisaki Y.; Ishikawa T.; Takao Y.; Omodani H.; Kuno N.; Itoh T., 1990: Binding of tritiated p aminoclonidine to two sites alpha 2 adrenoceptors and imidazoline binding sites distribution of imidazoline binding sites in rat brain. Binding sites labeled by [3H]p-aminoclonidine ([3H]PAC) were investigated by the competitive analysis with imidazoline and non-imidazoline derivatives. Phenylethylamine derivatives displaced only the part of specific sites for [3H]PAC, which was c...

Kamisaki, Y.; Ishikawa, T.; Takao, Y.; Omodani, H.; Kuno, N.; Itoh, T., 1990: Binding of [3H]p-aminoclonidine to two sites, alpha 2-adrenoceptors and imidazoline binding sites: distribution of imidazoline binding sites in rat brain. Binding sites labeled by [3H]p-aminoclonidine [( 3H]PAC) were investigated by the competitive analysis with imidazoline and non-imidazoline derivatives. Phenylethylamine derivatives displaced only the part of specific sites for [3H]PAC, which was...

Itzhak, Y.; Bonnet, K.A.; Groth, J.; Hiller, J.M.; Simon, E.J., 1982: Multiple opiate binding sites in human brain regions: evidence for kappa and sigma sites. Life Sciences 31(12-13): 1363-1366

Itzhak Y.; Bonnet K.A.; Groth J.; Hiller J.M.; Simon E.J., 1982: Multiple opiate binding sites in the human brain regions evidence for kappa and sigma sites. Life Sciences 31(12-13): 1363-1366

Widdowson, P.S.; Renouard, A.; Vilaine, J.P., 1993: Binding of [3H]angiotensin II and [3H]DuP 753 (Losartan) to rat liver homogenates reveals multiple sites. Relationship to AT1a- and AT1b-type angiotensin receptors and novel nonangiotensin binding sites. The binding characteristics of radiolabeled angiotensin II and the nonpeptidergic angiotensin AT1 receptor antagonist, DuP 753 (Losartan), were studied in rat liver homogenates. Competition experiments with human angiotensin I, II, and III and wit...

Van Drunen, C.M.; Mientjes, E.; Van Zuylen, C.; Van D.P.tte, P.; Goosen, N., 1994: Transposase A binding sites in the attachment sites of bacteriophage Mu that are essential for the activity of the enhancer and A binding sites that promote transposition towards Fpro-lac. In this paper we determine which of the A binding sites in the attachment sites of phage Mu are required for the stimulatory activity of the transpositional enhancer (IAS). For this purpose the transposition frequencies of mini-Mu's with diff...

van Drunen, C.M.; Mientjes, E.; van Zuylen, O.; van de Putte, P.; Goosen, N., 1994: Transposase A binding sites in the attachment sites of bacteriophage Mu that are essential for the activity of the enhancer and A binding sites that promote transposition towards Fpro-lac. In this paper we determine which of the A binding sites in the attachment sites of phage Mu are required for the stimulatory activity of the transpositional enhancer (IAS). For this purpose the transposition frequencies of mini-Mu's with diff...