Metabolism of the Synthetic Prostaglandin Alfaprostol in Cows, Pigs, and Rats

Metabolism of a thromboxane A2 antagonist (+/-)-5-(Z)-7-(3-endo-phenylsulphonylaminobicyclo[2.2.1]hept-2- exoyl)- heptenoic acid (S-145) in isolated rat hepatocytes was examined by high-performance liquid chromatography and gas chromatography/mass spectrometry. As the hydrophobic metabolites, bis-nor S-145, tetra-nor S-145 and bis-nordihydro S-145 were identified, and two other products were estimated to be monohydroxylated S-145 and dehydrogenated S-145. On the basis of kinetics of S-145 metabolism, a metabolic pathway of S-145 in isolated hepatocytes is tentatively proposed.

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Metabolism of a thromboxane A2 antagonist in isolated rat hepatocytes

Higaki

Tonda

Takahashi

et al. 1989

Biol. Mass Spectrom.

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Pharmacokinetics of nocloprost in human volunteers and its relation to dose

Täuber¹,

Brudny-Klöppel²,

Jakobs³

et al. 1993

Eur J Clin Pharmacol

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The pharmacokinetics and absolute bioavailability of nocloprost, a synthetic PGE2-analogue with cytoprotective properties, was investigated in human volunteers as a function of the dose. Ten young male volunteers received nocloprost 5 micrograms i.v. and 100, 200 and 400 micrograms p.o. in random order at weekly intervals. Serum nocloprost levels were monitored for up to 12 h after each dose, using a specific, validated assay. After nocloprost 5 micrograms i.v. the highest serum level of 373 pg.ml-1 was found in the first sample 5 min after injection, and the subsequent decline showed one or two phases, with half-lives of 4 and 49 min. The AUC was 89 pg.h.ml-1, the total plasma clearance was 13.2 ml.min-1.kg-1, and the volume of distribution at steady state was 0.16 l.kg-1. After oral administration the maximum serum level and AUC increased in proportion to the dose. tmax showed a wide scatter, with an average value of about 30 min independent of the dose. Although not detectable in every subject, post maximum serum levels declined biphasically, with half-lives of ca 10 and 35-40 min. The absolute bioavailability after oral administration averaged about 2% and was independent of the dose.

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Novel synthetic approach to alfaprostol key intermediates via Stille coupling with an alkyne

Monteiro

Imramovský

Pauk

et al. 2017

Tetrahedron Letters

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Metabolism of the Synthetic Prostaglandin Alfaprostol in Cows, Pigs, and Rats

Cited by 4 publications

References 6 publications

Metabolism of a thromboxane A2 antagonist in isolated rat hepatocytes

Metabolism of a thromboxane A2 antagonist in isolated rat hepatocytes

Pharmacokinetics of nocloprost in human volunteers and its relation to dose

Novel synthetic approach to alfaprostol key intermediates via Stille coupling with an alkyne

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