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Titolo:
BIOCHEMICAL AND PHARMACOLOGICAL CHARACTERIZATION OF MU-OPIOID, DELTA-OPIOID AND KAPPA(3)-OPIOID RECEPTORS EXPRESSED IN BE(2)-C NEUROBLASTOMA-CELLS
Autore:
STANDIFER KM; CHENG J; BROOKS AI; HONRADO CP; SU W; VISCONTI LM; BIEDLER JL; PASTERNAK GW;
Indirizzi:
MEM SLOAN KETTERING CANC CTR,DEPT NEUROL,1275 YORK AVE NEW YORK NY 10021 MEM SLOAN KETTERING CANC CTR,COTZIAS LAB NEUROONCOL NEW YORK NY 10021 MEM SLOAN KETTERING CANC CTR,CELLULAR & BIOCHEM GENET LAB NEW YORK NY10021 CORNELL UNIV,COLL MED,DEPT NEUROL NEW YORK NY 00000 CORNELL UNIV,COLL MED,DEPT NEUROSCI & PHARMACOL NEW YORK NY 00000
Titolo Testata:
The Journal of pharmacology and experimental therapeutics
fascicolo: 3, volume: 270, anno: 1994,
pagine: 1246 - 1255
SICI:
0022-3565(1994)270:3<1246:BAPCOM>2.0.ZU;2-Q
Fonte:
ISI
Lingua:
ENG
Soggetto:
ADENYLATE-CYCLASE ACTIVITY; GUINEA-PIG BRAIN; NG108-15 HYBRID-CELLS; PERTUSSIS TOXIN TREATMENT; IRREVERSIBLE OPIATE AGONISTS; BLASTOMA SH-SY5Y CELLS; GTP-BINDING PROTEIN; RAT OLFACTORY-BULB; GUANINE-NUCLEOTIDE; NALOXONE BENZOYLHYDRAZONE;
Tipo documento:
Review
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
111
Recensione:
Indirizzi per estratti:
Citazione:
K.M. Standifer et al., "BIOCHEMICAL AND PHARMACOLOGICAL CHARACTERIZATION OF MU-OPIOID, DELTA-OPIOID AND KAPPA(3)-OPIOID RECEPTORS EXPRESSED IN BE(2)-C NEUROBLASTOMA-CELLS", The Journal of pharmacology and experimental therapeutics, 270(3), 1994, pp. 1246-1255

Abstract

Total opioid binding in the human neuroblastoma cell line BE(2)-C hasa density similar to that found in brain, with a B, value of 383 +/- 60 fmol/mg protein and a K-D of 0.4 +/- 0.07 nM for the nonselective opioid antagonist H-3-diprenorphine. Selective assays reveal a binding distribution of mu (38%), delta (16%) and kappa(3) (43%) opioid receptors. There is no observable kappa(1) or kappa(2) binding. The sum of the B-max values in the selective binding assays (370 +/- 39 fmol/mg protein) approximates closely that observed with H-3-diprenorphine, suggesting that mu, delta and kappa(3) sites account for most of the binding. The binding selectivities of various opiates and opioid peptides in the BE(2)C cells are similar to those in rat brain. Delta and mu binding are defined easily by traditional selective ligands. The binding profiles also distinguish clearly mu from kappa(3) binding. The selective mu ligand DAMGO competes with mu binding over 35-fold more potently than kappa(3) binding, whereas morphine shows a 10-fold selectivity. Functionally, selective mu, delta and kappa(3) agonists inhibit forskolin-stimulated cAMP accumulation through distinct receptor mechanismsthat are pertussis toxin-sensitive. In addition to demonstrating thatBE(2)-C cells provide a useful model system for studying mu, kappa(3)and delta receptors, these studies confirm that kappa(3) receptors represent a pharmacologically distinct receptor class in this cell line.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 04/07/20 alle ore 04:46:18