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Titolo:
Apparent species differences in the kinetic properties of P2X(7) receptors
Autore:
Hibell, AD; Kidd, EJ; Chessell, IP; Humphrey, PPA; Michel, AD;
Indirizzi:
Univ Cambridge, Dept Pharmacol, Glaxo Inst Appl Pharmacol, Cambridge CB2 1QJ, England Univ Cambridge Cambridge England CB2 1QJ col, Cambridge CB2 1QJ, England
Titolo Testata:
BRITISH JOURNAL OF PHARMACOLOGY
fascicolo: 1, volume: 130, anno: 2000,
pagine: 167 - 173
SICI:
0007-1188(200005)130:1<167:ASDITK>2.0.ZU;2-M
Fonte:
ISI
Lingua:
ENG
Soggetto:
EXTRACELLULAR ATP; PLASMA-MEMBRANE; PORE FORMATION; PATCH-CLAMP; CELLS; RAT; MACROPHAGES; ADENOSINE; CLONING;
Keywords:
P2X(7); ATP; ion channel;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
18
Recensione:
Indirizzi per estratti:
Indirizzo: Michel, AD Univ Wales Coll Cardiff, Welsh Sch Pharm, Dept Pharmacol, King Edward VII Ave, Cardiff CF1 3XF, S Glam, Wales Univ Wales Coll Cardiff KingEdward VII Ave Cardiff S Glam Wales CF1 3XF
Citazione:
A.D. Hibell et al., "Apparent species differences in the kinetic properties of P2X(7) receptors", BR J PHARM, 130(1), 2000, pp. 167-173

Abstract

1 Apparent species differences in the responses of recombinant P2X(7) receptors to repeated application of 2'- and 3'-O-(4-benzoylbenzoyl)-ATP (BzATP) have been investigated.2 Repeated application of 100 mu M BzATP resulted in a progressive increase in current magnitude (current growth) at mouse and human, but not rat P2X(7) receptors.3 Current growth was thought to reflect progressive dilation of the P2X(7)ion-channel to a pore permeable to large molecules (MW < 900), suggesting that channel dilation was not occurring at the rat P2X(7) receptor. However, 100 mu M BzATP produced a rapid influx of YO-PRO-1 (MW375) in cells expressing rat or human P2X(7) receptors.4 There were, however, species differences in agonist potency such that 100 mu M BzATP was a supra-maximal concentration at rat, but not human or mouse, P2X(7) receptors. Importantly, when sub-maximal concentrations of BzATPor ATP were examined, current growth occurred at rat P2X(7) receptors.5 The rate of current growth and YO-PRO-1 accumulation increased with agonist concentration and appeared more rapid at rat and human, than at mouse P2X(7) receptors.6 The potency of BzATP and ATP was 1.5-10 fold lower in naive cells than in cells repeatedly exposed to ATP.7 This study demonstrates that current growth occurs at mouse, rat and human P2X(7) receptors but only when using sub-maximal concentrations of agonist. Previously, current growth was thought to reflect the progressive increase in pore diameter of the P2X(7) receptor ion channel, however, the results of this study suggest a progressive increase in agonist potency may alsocontribute.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 04/12/20 alle ore 19:22:51