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РЖ ВИНИТИ 76 (BI31) 95.07-04Т3.021

Walle, U. K.
Stereoselective sulphate conjugation of salbutamol in humans: comparison of hepatic, intestinal and platelet activity [Text] / U. K. Walle, G. R. Pesola, T. Walle // Brit. J. Clin. Pharmacol. - 1993. - Vol. 35, N 4. - P413- 418 . - ISSN 0306-5251
Перевод заглавия: Стереоселективность сульфатпроизводных салбутамола у людей: сравнение активности печени, кишечника и тромбоцитов
Аннотация: The oral bioavailability of the 'бета'[2]-adrenoceptor agonist salbutamol has been proposed to be stereoselective, presumably due to presystemic sulphate conjugation. In the present study we examined the stereochemistry of the sulphation reaction in vitro using human tissue preparations. Sulphation of salbutamol was studied with partially purified hepatic M and P form phenol sulphotransferases (PSTs), 100,000 g cytosol of jejunal mucosa and platelet homogenate. The cosubstrate PAP{3}{5}S was used as the sulphate donor. The acceptor substrate was either (+)-, (-)-or ('+-')-salbutamol. Sulphation was catalyzed by the M form PST of the liver but not the P form. The sulphation efficiency (V[m][a][x]/К[m]) was 11.9-fold greater for the (-)-than for the (+)-enantiomer, due entirely to a lower apparent K[m] for (-)-salbutamol, 103 'мю'm, than for (+)-salbutamol, 1394 'мю'м. Sulphation by the jejunal muosa (n=3) was very similar to that of the M form PST with the efficiency being 9.8-fold greater for the (-)enantiomer and apparent K[m] values 95 'мю'м and 889 'мю'м for (-)- and (+)-salbutamol, respectively. Sulphation by the platelet (n=3) was also very similar to that of the M form PST with the efficiency being 9.9-fold greater for the (-)-enantiomer and apparent K[m] values 141 'мю'м and 1190 'мю'м for (-)- and (+)-salbutamol, respectively. The sulphation of racemic ('+-')-salbutamol by all three preparations behaved as would be predicted from the individual enantiomers alone, if the enantiomers in the racemic mixture are regarded as two different substrates competing for the same binding site. These findings suggest the potential for large enantioselectivity in the oral bioavailability of salbumatol, with lower blood concentrations of the pharmacologically more active (-)-enantiomer.

ГРНТИ	76.31.29

ВИНИТИ 761.31.29.02.09
Рубрики: САЛБУТАМОЛ
СУЛЬФАТПРОИЗВОДНЫЕ
БИОДОСТУПНОСТЬ
ПЕЧЕНЬ
ТОНКИЙ КИШЕЧНИК
ТРОМБОЦИТЫ
АКТИВНОСТЬ
БОЛЬНЫЕ

Доп.точки доступа:
Pesola, G.R.; Walle, T.

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