The metabolism of bifluranol by rat, dog and ferret

Author:

POPE D J1,GILBERT A P1,EASTER D J1,CHAN R P1,TURNER J C1,GOTTFRIED S1,PARKE D V2

Affiliation:

1. Biorex Laboratories Ltd, Biorex House, Canonbury Villas, London, N1 2HB

2. Department of Biochemistry, University of Surrey, Guildford, Surrey, UK

Abstract

Abstract The synthesis of monohydroxy- and dihydroxy-bifluranol, and of glucuronide and sulphate conjugates of bifluranol are described. Bifluranol administered orally to rats, ferrets and dogs at a dosage of 50 to 200 μg kg−1 is mostly excreted in the faeces as unchanged bifluranol and bifluranol monosulphate, disulphate and monoglucuronide. The bifluranol is well absorbed and is mostly excreted in the bile, as six different conjugates, including a glucuronide sulphate found in all 3 species, and a glucuronide phosphate found only in ferret and dog bile. Hydroxylation of the aromatic rings occurs in the rat, to an extent of about 8% of the dose, but was not detected in ferret or dog.

Publisher

Oxford University Press (OUP)

Subject

Pharmaceutical Science,Pharmacology

Cited by 5 articles. 订阅此论文施引文献 订阅此论文施引文献,注册后可以免费订阅5篇论文的施引文献,订阅后可以查看论文全部施引文献

1. Uses of Fluorine in Chemotherapy;Organofluorine Chemistry;1994

2. Hepatic mixed-function oxidases of ferret;Xenobiotica;1992-01

3. Comparative Behavioral Toxicity of Physostigmine in Ferrets and Rats;Journal of the American College of Toxicology;1986-07

4. Bifluranol in the treatment of benign prostatic hyperplasia (BPH);The Prostate;1985

5. Chapter 33. Drug Metabolism;Annual Reports in Medicinal Chemistry;1982

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