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Titolo:
MOLECULAR PHARMACOLOGY OF SOMATOSTATIN RECEPTORS
Autore:
VIOLLET C; PREVOST G; MAUBERT E; FAIVREBAUMAN A; GARDETTE R; KORDON C; LOUDES C; SLAMA A; EPELBAUM J;
Indirizzi:
CTR PAUL BROCA,INSERM,U159,2TER RUE ALESIA F-75014 PARIS FRANCE CTR PAUL BROCA,INSERM,U159 F-75014 PARIS FRANCE FAC SCI CAEN,PSYCHOPHYSIOL LAB CAEN FRANCE
Titolo Testata:
Fundamental and clinical pharmacology
fascicolo: 2, volume: 9, anno: 1995,
pagine: 107 - 113
SICI:
0767-3981(1995)9:2<107:MPOSR>2.0.ZU;2-V
Fonte:
ISI
Lingua:
ENG
Soggetto:
RAT-BRAIN; FUNCTIONAL-CHARACTERIZATION; ADENYLYL-CYCLASE; G-PROTEINS; CLONING; EXPRESSION; PITUITARY; SUBTYPES; ANALOGS; IDENTIFICATION;
Keywords:
STRUCTURE; PHARMACOLOGY; 2ND-MESSENGER COUPLING; TISSUE EXPRESSION; NEUROENDOCRINE TUMORS;
Tipo documento:
Review
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
65
Recensione:
Indirizzi per estratti:
Citazione:
C. Viollet et al., "MOLECULAR PHARMACOLOGY OF SOMATOSTATIN RECEPTORS", Fundamental and clinical pharmacology, 9(2), 1995, pp. 107-113

Abstract

Somatostatin was discovered for its ability to inhibit growth hormone(GH) secretion. Later, it was found to be widely distributed in otherbrain regions, in which it fulfills a neuromodulatory role, and in several organs of the gastrointestinal tract where it can act as a paracrine factor or as a true circulating factor. In mammals, two moleculesof 14 (somatostatin 14) and 28 (somatostatin 28) amino acids are the only biologically active members of the family. They originate from a single gene which gives rise to a single propeptide alternately cleaved in different tissues. In 1992, a major breaktrough in our understanding of somatostatin functions was made with the cloning of five different receptor genes (sstr1 to sstr5) which belong to the seven transmembrane domain receptor family. Their closer relatives are opioid receptors. In first approximation, the tissular expression of the sstrs matches quite well with the distribution of somatostatin binding sites in the ''classical'' targets of the peptide ie brain, pituitary pancreatic islets and adrenals. The pharmacology of GH inhibition is very closeto sstr2 binding but other actions of somatostatins have not yet beenattributed clearly to a single receptor subtype. All clinically relevant agonists tested so far (octreotide, lanreotide and vapreotide) areselective of sstr2 being less potent on sstr3 and inactive for sstr1 and sstr4. Surprisingly, rat sstr5 displays nanomolar affinities for octreotide and vapreotide while these agonists are only active at much higher concentrations on human sstr5. Ah five receptors can be more orless efficiently coupled to inhibition of adenylate cyclase activity in transfected cell systems. However, the transduction of somatostatinantisecretory and antiproliferative actions through multiple intracellular effecters and their relation to the diversity of the receptors remain to be established as yet.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 04/04/20 alle ore 14:05:50