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Titolo:
The mycotoxin paxilline inhibits the cerebellar inositol 1,4,5-trisphosphate receptor
Autore:
Longland, CL; Dyer, JL; Michelangeli, F;
Indirizzi:
Univ Birmingham, Sch Biochem, Birmingham B15 2TT, W Midlands, England UnivBirmingham Birmingham W Midlands England B15 2TT W Midlands, England
Titolo Testata:
EUROPEAN JOURNAL OF PHARMACOLOGY
fascicolo: 3, volume: 408, anno: 2000,
pagine: 219 - 225
SICI:
0014-2999(20001124)408:3<219:TMPITC>2.0.ZU;2-3
Fonte:
ISI
Lingua:
ENG
Soggetto:
ACTIVATED POTASSIUM CHANNELS; CALCIUM-RELEASE; ENDOPLASMIC-RETICULUM; CA2+ RELEASE; MICROSOMES; TRISPHOSPHATE; CONDUCTANCE; BLOCKERS; KINETICS; STORES;
Keywords:
InsP(3) receptor; Ca2+ signalling; paxilline; mycotoxin;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
24
Recensione:
Indirizzi per estratti:
Indirizzo: Michelangeli, F Univ Birmingham, Sch Biochem, POB 363, Birmingham B15 2TT,W Midlands, England Univ Birmingham POB 363 Birmingham W Midlands England B15 2TT
Citazione:
C.L. Longland et al., "The mycotoxin paxilline inhibits the cerebellar inositol 1,4,5-trisphosphate receptor", EUR J PHARM, 408(3), 2000, pp. 219-225

Abstract

Paxilline, a tremorgenic alkaloid mycotoxin produced by Penicillium paxilline, is a reversible inhibitor of the cerebellar inositol 1,4,5-trisphophate (InsP(3)) receptor. It inhibits the amount or extent of InsP(3)-induced Ca2+ release (IICR), at sub-maximal concentrations of InsP(3), in a biphasicmanner consistent with two inhibition constants (K-i's 6.7 and greater than or equal to 400 muM) As paxilline does not affect InsP(3) binding to the receptor, it can be considered a non-competitive inhibitor. The fact that IICR is biphasic has been interpreted as there being two populations of InsP(3)-sensitive Ca2+ stores, which release Ca2+ in either a fast or slow fashion. This study has shown that the rate constants for Ca2+ release from both the fast and slow populations are reduced by paxilline (100 muM) by about70% and 60%, respectively. Detailed analysis of the way different concentrations of paxilline inhibit the rate constants for Ca2+ release indicates that the population of Ca2+ stores that contribute to the slower phase of Ca2+ release is more sensitive to the inhibitory action of paxilline. (C) 2000 Elsevier Science B.V. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 16/07/20 alle ore 15:06:42