Isolation, identification and in vitro synthesis of conjugates of penbutolol and its metabolites

K H Lehr; P Damm; H W Fehlhaber; P Hajdù

Isolation, identification and in vitro synthesis of conjugates of penbutolol and its metabolites

Arzneimittelforschung. 1987 Nov;37(11):1222-4.

Authors

K H Lehr¹, P Damm, H W Fehlhaber, P Hajdù

Affiliation

¹ Hoechst Aktiengesellschaft, Frankfurt/Main (Fed. Rep. of Germany).

PMID: 3440029

Abstract

The metabolites of 1-tert.-butylamino-3-(2-cyclopentylphenoxy)propan-2-ol (penbutolol Betapressin) penbutolol 2-glucuronide, 4'-OH-penbutolol 2-glucuronide, 4'-OH-penbutolol 4'-sulfate and 1''-dehydropenbutolol 2-glucuronide were isolated from the urine of patients, purified by high-performance liquid chromatography and characterised by 1H-NMR and mass spectroscopy. Penbutolol 2-glucuronide and 4'-OH-penbutolol 4'-glucuronide were synthesised in vitro from penbutolol and 4'-OH-penbutolol, respectively, using glucuronyltransferase.

MeSH terms

Animals
Biotransformation
Cattle
Glucuronates / metabolism
Humans
In Vitro Techniques
Mass Spectrometry
Penbutolol / metabolism*
Penbutolol / urine
Propanolamines / metabolism*
Rabbits
Rats
Sulfates / metabolism

Substances

Glucuronates
Propanolamines
Sulfates
Penbutolol