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Titolo:
SLIDE-BINDING CHARACTERIZATION AND AUTORADIOGRAPHIC LOCALIZATION OF DELTA-OPIOID RECEPTORS IN RAT AND MOUSE BRAINS WITH THE TETRAPEPTIDE ANTAGONIST [H-3]TIPP
Autore:
BAKOTA L; SZIKRA J; TOTH G; GULYA K;
Indirizzi:
UNIV SZEGED,DEPT ZOOL & CELL BIOL,2 EGYETEM U,POB 659 H-6722 SZEGED HUNGARY UNIV SZEGED,DEPT ZOOL & CELL BIOL H-6722 SZEGED HUNGARY BIOL RES CTR,INST BIOCHEM H-6701 SZEGED HUNGARY
Titolo Testata:
Life sciences (1973)
fascicolo: 15, volume: 63, anno: 1998,
pagine: 1377 - 1385
SICI:
0024-3205(1998)63:15<1377:SCAALO>2.0.ZU;2-0
Fonte:
ISI
Lingua:
ENG
Soggetto:
CYCLIC ENKEPHALIN ANALOG; OPIATE RECEPTORS; NALTRINDOLE; AGONIST; POTENT; SITES; DIFFERENTIATION; SELECTIVITY; PEPTIDES; LIGANDS;
Keywords:
AUTORADIOGRAPHY; DELTA OPIOID ANTAGONIST; DELTA OPIOID RECEPTOR; SLIDE-BINDING;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
26
Recensione:
Indirizzi per estratti:
Citazione:
L. Bakota et al., "SLIDE-BINDING CHARACTERIZATION AND AUTORADIOGRAPHIC LOCALIZATION OF DELTA-OPIOID RECEPTORS IN RAT AND MOUSE BRAINS WITH THE TETRAPEPTIDE ANTAGONIST [H-3]TIPP", Life sciences (1973), 63(15), 1998, pp. 1377-1385

Abstract

Slide-binding and autoradiographic studies were performed on cryostatsections from brains of adult Sprague-Dawley rats and BALE C mice to describe the binding characteristics of the tetrapeptide [H-3]TIPP, anantagonist with high specificity and affinity for the delta opioid receptors. Steady-state binding of [H-3]TIPP to cryostat sections of brain paste was reached in 120-180 min of incubation. Specific [H-3]TIPP binding resulted in maximal numbers of binding sites (B-max) of 15.59 and 23.91 fmol/mg protein, and dissociation constants (K-d) of 0.46 and 0.85 nM for rat and mouse brain paste sections, respectively. TIPP displayed the highest affinity for delta opioid receptors in inhibitingspecific [H-3]TIPP binding, with IC50 values of 0.82 nM and 0.14 nM in rat and mouse brain sections, respectively. While DPDPE was also effective in displacing the specific binding of [H-3]TIPP (IC50 = 3.18 +/- 0.53 nM and 0.63 +/- 0.42 nM in rat and mouse brain paste sections, respectively), other subclass-selective or nonopioid ligands were muchless effective, or ineffective. Autoradiographic localization of [H-3]TIPP binding revealed the characteristic distribution of delta opioidreceptors in both species. In consequence of its antagonistic nature,and of its unnatural amino acid residue, which makes this ligand moreresistant to biodegradation, [H-3]TIPP is a superior ligand for evaluation of the binding characteristics and autoradiogaphic distribution of the delta opioid receptors.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 02/04/20 alle ore 18:43:55