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Titolo:
TACHYKININ PEPTIDES AFFECT DIFFERENTLY THE 2ND-MESSENGER PATHWAYS AFTER BINDING TO CHO-EXPRESSED HUMAN NK-1 RECEPTORS
Autore:
SAGAN S; CHASSAING G; PRADIER L; LAVIELLE S;
Indirizzi:
UNIV PARIS 06,LAB CHIM ORGAN BIOL,CNRS URA 493,4 PL JUSSIEU F-75005 PARIS FRANCE RHONE POULENC RORER F-94403 VITRY FRANCE
Titolo Testata:
The Journal of pharmacology and experimental therapeutics
fascicolo: 3, volume: 276, anno: 1996,
pagine: 1039 - 1048
SICI:
0022-3565(1996)276:3<1039:TPADT2>2.0.ZU;2-8
Fonte:
ISI
Lingua:
ENG
Soggetto:
GUINEA-PIG ILEUM; SUBSTANCE-P ANTAGONIST; CORTICAL ASTROCYTES; SELECTIVE AGONISTS; RAT; NK1; NONPEPTIDE; POTENT; MOUSE; INHIBITION;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
41
Recensione:
Indirizzi per estratti:
Citazione:
S. Sagan et al., "TACHYKININ PEPTIDES AFFECT DIFFERENTLY THE 2ND-MESSENGER PATHWAYS AFTER BINDING TO CHO-EXPRESSED HUMAN NK-1 RECEPTORS", The Journal of pharmacology and experimental therapeutics, 276(3), 1996, pp. 1039-1048

Abstract

The human NK-I receptor transfected in Chinese hamster ovary (CHO) cells was studied with use of different tachykinin analogs: Substance P,[Pro(9)]SP, [Sar(9), Met(O-2)(11)]SP, [Gly(9) Psi(CH2CH2) Leu(10)]SP,Ac-Arg;septide, septide, [Gly(9) Psi(CH2CH2) Gly(10)]SP, NKA [pGlu(6)]SP(6-11) and [Lys(5)]NKA(4-10). Binding experiments with [H-3][Pro(9)]SP discriminated two classes of peptides with either high affinity (K-i in the nanomolar range) for the human NK-1 receptor or with low affinity (K-i in the micromolar range); this second group of peptides included NKA and [pGlu(6)]SP(G-II). In spite of these differences, both peptide families evoked potent stimulation of phosphatidylinositol hydrolysis (EC(50) in the nanomolar range). In contrast, only NK-1 agonists, with high affinity, stimulated with great potency cyclic AMP formation (EC(50) from 8 to 50 nM), whereas the second family of peptides were only weak agonists (EC(50) in the micromolar range). RP 67580, CP 96345 and GR 94800, a NK-2 antagonist, were either competitive or uncompetitive inhibitors of inositol phosphates or cyclic AMP formations induced by [Pro(9)]SP: septide or NKA, independently of the agonist or the response studied. Thus, NKA, the presumed NK-2 endogenous peptide that may be co-released with SP, and the enzymatically produced C-terminal fragment of SP, [pGlu(6)]SP(6-11), may trigger specific pharmacological responses via the NK-1 receptor, at nanomolar concentrations, and thus regulate the action of SP at the NK-1 receptor.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 30/03/20 alle ore 00:51:36