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Titolo:
Inhibitory potencies of 1,4-dihydropyridine calcium antagonists to P-glycoprotein-mediated transport: Comparison with the effects on CYP3A4
Autore:
Katoh, M; Nakajima, M; Yamazaki, H; Yokoi, T;
Indirizzi:
Kanazawa Univ, Fac Pharmaceut Sci, Div Drug Metab, Kanazawa, Ishikawa 9200934, Japan Kanazawa Univ Kanazawa Ishikawa Japan 9200934 wa, Ishikawa 9200934, Japan
Titolo Testata:
PHARMACEUTICAL RESEARCH
fascicolo: 10, volume: 17, anno: 2000,
pagine: 1189 - 1197
SICI:
0724-8741(200010)17:10<1189:IPO1CA>2.0.ZU;2-U
Fonte:
ISI
Lingua:
ENG
Soggetto:
OVERLAPPING SUBSTRATE SPECIFICITIES; TRANSCELLULAR TRANSPORT; MULTIDRUG-RESISTANCE; CYTOCHROME-P450 3A; CELL-LINE; CYCLOSPORINE; DIGOXIN; DOXORUBICIN; VINBLASTINE; CANCER;
Keywords:
P-glycoprotein; 1,4-dihydropyridine calcium antagonists; inhibition; cytochrome P450 3A4;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
24
Recensione:
Indirizzi per estratti:
Indirizzo: Yokoi, T Kanazawa Univ, Fac Pharmaceut Sci, Div Drug Metab, Takara Machi 13-1, Kanazawa, Ishikawa 9200934, Japan Kanazawa Univ Takara Machi 13-1 Kanazawa Ishikawa Japan 9200934 n
Citazione:
M. Katoh et al., "Inhibitory potencies of 1,4-dihydropyridine calcium antagonists to P-glycoprotein-mediated transport: Comparison with the effects on CYP3A4", PHARM RES, 17(10), 2000, pp. 1189-1197

Abstract

Purpose. Recently, we clarified the inhibitory effects of 13 kinds of 1,4-dihydropyridine calcium antagonists on human cytochrome P450 (CYP) 3A4. It has been reported that the substrates and/or inhibitors are overlapped between CYP3A4 and P-glycoprotein (P-gp). The purpose of this study was to investigate the inhibitory effects of 13 kinds of 1,4-dihydropyridine calcium antagonists on P-gp-mediated transport in order to evaluate the overlapping specificity of the inhibitors between P-gp and CYP3A4. Methods. The transcellular transports of [H-3]daunorubicin or [H-3]digoxinby monolayers of LLC-GA5-COL150 cells in which P-gp was overexpressed weremeasured in the presence or absence of the 1,4-dihydropyridine calcium antagonists. Results. The transport of [H-3]daunorubicin was strongly inhibited by manidipine, barnidipine, benidipine, (-)-efonidipine, nicardipine, (+)-efonidipine, and amlodipine with the IC50 values of 4.6, 8.6, 9.5, 17.3, 17.5, 20.6, and 22.0 muM, respectively. The transport of [H-3]digoxin was strongly inhibited by benidipine, nicardipine, barnidipine, and manidipine. Conclusions. It was clarified that 13 kinds of 1,4-dihydropyridine calciumantagonists have different inhibitory potencies and substrate specificities to the transport of [H-3]daunorubicin or [H-3]digoxin. Some compounds didnot demonstrate the overlapping specificity for inhibition between P-gp and CYP3A4. It was also clarified that nicardipine, benidipine, manidipine, and barnidipine were strong inhibitors of P-gp as well as CYP3A4.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 22/01/20 alle ore 07:28:39