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Titolo:
Serum constituents can affect 2 '-& 3 '-O-(4-benzoylbenzoyl)-ATP potency at P2X(7) receptors
Autore:
Michel, AD; Xing, M; Humphrey, PPA;
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: 7, volume: 132, anno: 2001,
pagine: 1501 - 1508
SICI:
0007-1188(200104)132:7<1501:SCCA2'>2.0.ZU;2-M
Fonte:
ISI
Lingua:
ENG
Soggetto:
TRANSFORMED MOUSE FIBROBLASTS; 3'-O-(4-BENZOYL)BENZOYL ADENOSINE 5'-TRIPHOSPHATE; FATTY-ACID ANALOG; PHARMACOLOGICAL CHARACTERIZATION; NUCLEOTIDE RECEPTOR; ARACHIDONIC-ACID; BINDING-SITES; ATP; RAT; ALBUMIN;
Keywords:
BzATP; bovine serum albumin; P2X(7) receptor;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
28
Recensione:
Indirizzi per estratti:
Indirizzo: Michel, AD Univ Cambridge, Dept Pharmacol, Glaxo Inst Appl Pharmacol, Tennis Court Rd, Cambridge CB2 1QJ, England Univ Cambridge Tennis Court Rd Cambridge England CB2 1QJ gland
Citazione:
A.D. Michel et al., "Serum constituents can affect 2 '-& 3 '-O-(4-benzoylbenzoyl)-ATP potency at P2X(7) receptors", BR J PHARM, 132(7), 2001, pp. 1501-1508

Abstract

1 2 '-& 3 ' -O-(4-benzoylbenzoyl)-ATP (BzATP) is the prototypic agonist for P2X(7) receptors. In this study we demonstrate that bovine serum albumin (BSA) can affect the potency of BzATP at P2X receptors.2 BzATP potency (pEC(50)) to stimulate ethidium accumulation in cells expressing recombinant P2X7 receptors varied between 6.5 and 4, depending upon the species orthologue studied and ionic conditions employed. BSA (0.1-1 mgml(-1)) and foetal bovine serum (FBS, 1-10% v v(-1)) inhibited responses to BzATP but only when the BzATP pEC(50) exceeded 5.3 BSA did not block ATP-stimulated ethidium accumulation, suggesting its effects were independent of P2X(7) receptor blockade.4 BSA did not cause breakdown of nucleotides, although FBS (10% v v(-1)) exhibited appreciable nucleotidase activity and caused significant breakdownof ATP.5 In the presence of BSA, lipids such as 11-((5-dimethylaminonaphthalene-1-sulphonyl)amino)undecanoic acid (DAUDA) and arachidonic acid (AA) markedlyincreased BzATP potency. Lipids had no affect on ATP potency in the presence of BSA and had little effect on responses to BzATP in the absence of BSA.6 These results suggested that the reduction in BzATP potency by BSA was due to BzATP binding to BSA and that lipids prevented this binding. Consistent with this hypothesis, BzATP inhibited binding of the fluorescent lipid, DAUDA, to BSA.7 In conclusion, BSA and lipids can markedly affect BzATP potency at P2X(7) receptors but this is probably a consequence of BzATP binding to BSA. This finding has important implications when using BzATP in vivo or in the presence of albumin.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 24/11/20 alle ore 14:02:19