title: [Synthesis, pharmacokinetics, and metabolism of the C-terminal tripeptide of dermorphin and its diastereomer].
abstract: A tritium-labeled C-terminal fragment of dermorphin (H-Tyr-13,4-3HJPro-Ser-NH2) and its isomer (H-Tyr-D-[3,4-3H]Pro-Ser-NH2) with molar radioactivity of 35 Ci/mmol were synthesized, and their pharmacokinetics and metabolism in rat organs were studied after their intramuscular injections. The tripeptides were detected in the blood only for 5 min after the injection, and maximum contents of both compounds (approximately 5% of the total amount of the injected label) were registered in the kidneys after 20 min. Both stereomers were shown to penetrate into the brain. We failed to detect any radioactive metabolite, except proline, due to rapid proteolytic degradation of these peptides.
authors.forename: P S
authors.initials: PS
authors.lastname: Gromovykh
authors.forename: L S
authors.initials: LS
authors.lastname: Guzevatykh
authors.forename: K V
authors.initials: KV
authors.lastname: Shevchenko
authors.forename: L A
authors.initials: LA
authors.lastname: Andreeva
authors.forename: L Iu
authors.initials: LIu
authors.lastname: Alfeeva
authors.forename: V P
authors.initials: VP
authors.lastname: Shevchenko
authors.forename: I Iu
authors.initials: IIu
authors.lastname: Nagaev
authors.forename: T A
authors.initials: TA
authors.lastname: Voronina
authors.forename: N F
authors.initials: NF
authors.lastname: Miasoedov
mesh_terms: D000701:Analgesics, Opioid / Q000138:chemical synthesis / Q000378:metabolism / Q000493:pharmacokinetics*; D000818:Animals; D001921:Brain / Q000378:metabolism*; D009842:Oligopeptides / Q000138:chemical synthesis / Q000378:metabolism / Q000493:pharmacokinetics*; D018847:Opioid Peptides / Q000138:chemical synthesis / Q000378:metabolism / Q000493:pharmacokinetics*; D051381:Rats; D013237:Stereoisomerism; D014018:Tissue Distribution
chemical_list: D000701:Analgesics, Opioid; D009842:Oligopeptides; D018847:Opioid Peptides; C526698:tyrosyl-prolyl-serinamide; C030058:dermorphin