Ion-pair high-performance liquid chromatography separation of β-endorphin-(6–17) from fourteen fragments

Janssen, P. S. L.; Nispen, J. W. Van; Melgers, P. A. T. A.; Hamelinck, R. L. A. E.

doi:10.1007/bf02341271

Cited by 8 publications

(1 citation statement)

References 19 publications

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“…The elution pattern was recorded on a Hewlett Packard 5880 A series printer/plotter; determination of the retention times and integration of the peakareas were done with the built-in data system Chromatographic conditions were adapted to those reported. by Janssen et al (10).…”

Section: High Performance Liquid Chromatographymentioning

confidence: 99%

Des-enkephalin-γ-endorphin (DEγE): Pharmacokinetics in dogs after intravenous and subcutaneous administration

Verhoef¹,

Wildenberg²

1989

European Journal of Drug Metabolism and Pharmacokinetics

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After intravenous dosing in dogs [3H-Lys9]-DE gamma E (Org 5878) was very rapidly eliminated from the circulation. Disappearance of the neuropeptide from blood followed a biphasic decay with half-lives of 0.6 +/- 0.1 min (+/- S.D.; alpha-phase) and 2.4 +/- 1.0 min (beta-phase). The central volume of distribution ranged between 0.05 and 0.23 l.kg-1. The mean blood clearance rate amounted to 0.15 l.min-1.kg-1, which is indicative of extensive hepatic and extrahepatic metabolism of DE gamma E. In contrast to intravenous dosing, subcutaneous injection of [3H]-DE gamma E in dogs resulted in low but relatively long-lasting peptide levels in blood. Peak values were found at 5-10 min, whereafter they declined to the limit of detection at 1.5-2 h. The bioavailability of DE gamma E for this route of administration was shown to be 20-23%.

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Section: High Performance Liquid Chromatographymentioning

confidence: 99%

Des-enkephalin-γ-endorphin (DEγE): Pharmacokinetics in dogs after intravenous and subcutaneous administration

Verhoef¹,

Wildenberg²

1989

European Journal of Drug Metabolism and Pharmacokinetics

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Des-enkephalin-γ-endorphin (DEγE): Biotransformation in rat, dog and human plasma

Verhoef¹,

Wildenberg²,

Nispen³

1986

European Journal of Drug Metabolism and Pharmacokinetics

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Biotransformation of [3H-Lys9] DE gamma E was investigated after in vitro incubation of the tritiated peptide with rat, dog and human plasma. In addition, its metabolite profile in blood was studied following intravenous administration to rats and dogs. Half-lives for the in vitro disappearance of DE gamma E in plasma were 13.0 +/- 0.8 min (dog), 15.7 +/- 1.2 min (rat) and 19.2 +/- 0.9 min (human), indicating very rapid degradation of the peptide by proteolytic enzymes. Biotransformation products were identified on the basis of co-chromatography on HPLC with synthetic reference peptides. The six principal fragments appeared to be beta-endorphin (beta E) sequences 7-17, 8-17, 9-17, 6-15, 7-15 and 8-15. The abundance of beta E6-15, beta E7-15 and beta E8-15 in rat and human plasma suggests preferential, subsequent carboxypeptidase and aminopeptidase mechanisms, whereas in dog plasma DE gamma E is predominantly degraded by aminopeptidase activities (major peptide metabolites: beta E7-17 and beta E8-17). In the in vivo studies with rats and dogs the same radioactive peptide fragments were detected in blood as found in the in vitro experiments with plasma. In both species their blood levels were already maximal within a minute after intravenous administration of the parent peptide, thereafter they declined rapidly. 3H-Lysine was the main radioactive metabolite in vivo, exceeding 70% of total radioactivity in rat and dog blood 10 min after 3H-DE gamma E dosing.

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Capillary zone electrophoresis of pharmaceutical peptides

Langenhuizen

Janssen

1993

Journal of Chromatography A

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Ion-pair high-performance liquid chromatography separation of β-endorphin-(6–17) from fourteen fragments

Cited by 8 publications

References 19 publications

Des-enkephalin-γ-endorphin (DEγE): Pharmacokinetics in dogs after intravenous and subcutaneous administration

Des-enkephalin-γ-endorphin (DEγE): Pharmacokinetics in dogs after intravenous and subcutaneous administration

Des-enkephalin-γ-endorphin (DEγE): Biotransformation in rat, dog and human plasma

Capillary zone electrophoresis of pharmaceutical peptides

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