In Vitro Studies on Species Differences in Befunolol-metabolizing Activities

Tohno, Masao; Kajikawa, Norio; Yamamoto, Tadashi; Ofuji, Tatsuya

doi:10.1248/yakushi1947.100.9_933

Cited by 2 publications

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“…Among the species tested, the rabbit exhibited the highest acetohexamide reductase activity. Similar results have been obtained for the in vitro metabolic reduction of a variety of ketone-containing drugs: 7,8) In an attempt to elucidate the properties of cytosolic acetohexamide reductase, the effects of specific inhibitors on the activity were compared between the rabbit and the rat. The sensitivities to specific inhibitors of acetohexamide reductases in the liver and kidney cytosols of the rabbit were evidently different from those of the rat (Table I).…”

Section: Discussionsupporting

confidence: 59%

Species difference in the in vitro metabolic reduction of acetohexamide.

Imamura

Kojima

Otagiri

1988

CHEMICAL & PHARMACEUTICAL BULLETIN

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Species difference in the in vitro metabolic reduction of acetohexamide, an oral antidiabetic drug, was investigated using the rabbit, guinea pig, hamster, rat and mouse. The rabbit exhibited the highest acetohexamide reductase activity in cytosol of the liver and kidney among the species tested. The sensitivities to specific inhibitors of cytosolic acetohexamide reductase in the liver and kidney of the rabbit were different from those of the rat. Furthermore, species difference in acetohexamide reductase activity was found in the microsomes of the liver and kidney; only the rat and guinea pig showed significant activity.

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Section: Discussionsupporting

confidence: 59%

Species difference in the in vitro metabolic reduction of acetohexamide.

Imamura

Kojima

Otagiri

1988

CHEMICAL & PHARMACEUTICAL BULLETIN

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Clinical pharmacology of a new ?-adrenoceptor blocking drug, befunolol

Ebihara

Tawara

et al. 1982

Eur J Clin Pharmacol

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Repeated doses of a new beta-adrenoceptor blocking agent, befunolol, were administered orally to adult male volunteers for a cross-over comparison with propranolol. The beta-adrenoceptor blocking activity of befunolol was greater than that of propranolol when assessed by the percentage reduction in exercise-induced tachycardia. The elimination half-life of drug was significantly prolonged on repeated administration of propranolol, but not of befunolol. The percentage reduction in exercise-induced tachycardia was highly correlated with the log plasma level of each drug. Both drugs produced a significant reduction in pre-exercise systolic and diastolic blood pressure, and significant attenuation of exercise-induced rise in systolic blood pressure.

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In Vitro Studies on Species Differences in Befunolol-metabolizing Activities

Cited by 2 publications

References 0 publications

Species difference in the in vitro metabolic reduction of acetohexamide.

Species difference in the in vitro metabolic reduction of acetohexamide.

Clinical pharmacology of a new ?-adrenoceptor blocking drug, befunolol

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