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001-es BibID:BIBFORM004324
Első szerző:Birkás Erika
Cím:Synthesis and pharmacological characterization of a novel, highly potent, peptidomimetic delta-opioid radio antagonist, [H-3]Tyr-Tic-(2S, 3R)-beta-MePhe-Phe-OH / Birkas E., Kertész I., Tóth G., Bakota L., Gulya K., Szucs M.
Dátum:2008
Megjegyzések:[(3)H]Tyr-Tic-(2S,3R)-beta-MePhe-Phe-OH (where Tic: 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid) with a specific radioactivity of 53.7 Ci/mmol was synthesized and characterized in receptor binding assays at 25 degrees C in rat brain membranes. The specific binding was saturable and displayed high affinity, with a K(D) of 0.16+/-0.005 nM and B(max) of 85.9+/-6.3 fmol/mg protein. NaCl increased its affinity by about 4-fold in membranes of rat brain and Chinese Hamster Ovary Cells stably transfected with the human delta-opioid receptors (hDOR-CHO) showing that the new ligand is an antagonist. The prototypic delta-opioid ligands were much more potent than mu- or kappa-specific ligands in competition assays. The autoradiographic distribution of the binding sites of the new ligand agreed with the known locations of the delta-opioid receptors in rat brain. The unlabeled new ligand was about 7-fold more potent than the parent peptide in competing for the binding sites of [(3)H]Tyr-Tic-(2S,3R)-beta-MePhe-Phe-OH in rat brain membranes. Likewise, the threo-beta-methyl analog was 3.8-fold more potent than the parent compound in antagonizing the effect of DPDPE in the [(35)S]GTPgammaS functional assay in hDOR-CHO membranes. The new, highly potent, conformationally constrained antagonist may be a valuable pharmacological tool in understanding the structural and topographical requirements of peptide ligand binding to the delta-opioid receptors.
Tárgyszavak:Orvostudományok Klinikai orvostudományok idegen nyelvű folyóiratközlemény külföldi lapban
Megjelenés:Neuropeptides. - 42 : 1 (2008), p. 57-67. -
További szerzők:Kertész István (1966-) (vegyész) Tóth Géza Bakota Lidia Gulya Károly Szűcs Mária
Internet cím:elektronikus változat
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