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Titolo:
KINETICS AND SODIUM INDEPENDENCE OF [H-3] TIAZOFURIN BLOOD TO BRAIN TRANSPORT IN THE GUINEA-PIG
Autore:
REDZIC ZB; MARKOVIC ID; JOVANOVIC SS; GASIC JM; MITROVIC DM; ZLOKOVICS BV; RAKIC LM;
Indirizzi:
UNIV BELGRADE SCH MED,INST BIOCHEM,2 PASTEROVA YU-11000 BELGRADE YUGOSLAVIA ICN GALENIKA INST,DEPT BIOMED RES BELGRADE YUGOSLAVIA FAC BIOL BELGRADE,DEPT MOL BIOL BELGRADE YUGOSLAVIA UNIV BELGRADE SCH MED,INST PHYSIOL BELGRADE YUGOSLAVIA UNIV SO CALIF,SCH MED,DEPT NEUROL SURG LOS ANGELES CA 90033
Titolo Testata:
Methods and findings in experimental and clinical pharmacology
fascicolo: 6, volume: 18, anno: 1996,
pagine: 413 - 418
SICI:
0379-0355(1996)18:6<413:KASIO[>2.0.ZU;2-K
Fonte:
ISI
Lingua:
ENG
Soggetto:
SATURABLE MECHANISM; IMP DEHYDROGENASE; TIAZOFURIN; BARRIER; METABOLISM;
Keywords:
TIAZOFURIN; GUINEA PIG; BLOOD-BRAIN BARRIER; TRANSPORT KINETICS; BRAIN UPTAKE;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
15
Recensione:
Indirizzi per estratti:
Citazione:
Z.B. Redzic et al., "KINETICS AND SODIUM INDEPENDENCE OF [H-3] TIAZOFURIN BLOOD TO BRAIN TRANSPORT IN THE GUINEA-PIG", Methods and findings in experimental and clinical pharmacology, 18(6), 1996, pp. 413-418

Abstract

Tiazofurin is a nucleoside analog with potent antitumor activity. Theobjective of this study was to define the kinetic parameters of tiazofurin transport from blood into the guinea pig brain. The second aim was to define kinetic parameters of tiazofurin transport inhibition by adenosine (K-i and K-d(a)), as well as whether tiazofurin blood-to-brain transport was performed in countertransport with Na+. In order to determine these parameters, the in situ method of perfusion of guinea pig brain was used. Addition of increasing concentrations of unlabelledtiazofurin to perfusing medium (0.05-2.7 mmol/l) caused progressive decrease of [H-3]-tiazofurin brain clearance with K-m values ranging from 119.57 +/- 40.12 to 150.17 +/- 51.68 x 10(-6) mol/l. Maximal transport capacity ranged from 325.03 +/- 113.93 to 417.50 +/- 151.53 pmol/min/g. Introduction of adenosine into the perfusing medium (0.005-0.2 mmol/l) caused similar but more rapid decrease of [H-3]-tiazofurin brain clearance (K-i = 6.36 +/- 3.14 x 10(-6) mol/l for nucleus caudate and 11.74 +/- 4.85 x 10(-6) mol/l for cerebral cortex). Therefore, it seems that transport system for adenosine plays the main role in tiazofurin brain uptake, but another transport mechanism is also involved in this process. Depletion of perfusing medium from sodium ions did not cause significant change in volume of distribution values for [H-3]-tiazofurin in guinea pig cerebral cortex.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 20/01/21 alle ore 14:32:31