Research Article

Exploratory pharmacokinetics and brain distribution study of a neuropeptide FF antagonist by liquid chromatography/atmospheric pressure ionization tandem mass spectrometry†

  1. Laszlo Prokai*,
  2. Alevtina D. Zharikova,
  3. Tamás Janáky§,
  4. Katalin Prokai-Tatrai

Article first published online: 24 NOV 2000

DOI: 10.1002/1097-0231(20001230)14:24<2412::AID-RCM180>3.0.CO;2-3

Issue

Rapid Communications in Mass Spectrometry

Rapid Communications in Mass Spectrometry

Volume 14, Issue 24, pages 2412–2418, 30 December 2000

Additional Information

How to Cite

Prokai, L., Zharikova, A. D., Janáky§, T., Prokai-Tatrai, K. (2000), Exploratory pharmacokinetics and brain distribution study of a neuropeptide FF antagonist by liquid chromatography/atmospheric pressure ionization tandem mass spectrometry. Rapid Communications in Mass Spectrometry, 14: 2412–2418. doi: 10.1002/1097-0231(20001230)14:24<2412::AID-RCM180>3.0.CO;2-3

Author Information

  1. Center for Drug Discovery, College of Pharmacy, University of Florida, Gainesville, FL, USA

*UF Center for Drug Discovery, P.O. Box 100497, Health Science Center, Gainseville, FL 32610-0497 USA

  • †

    Presented at the 48th ASMS Conference on Mass Spectrometry and Allied Topics, Long Beach, CA, June 15, 2000

Publication History

  1. Issue published online: 24 NOV 2000
  2. Article first published online: 24 NOV 2000
  3. Manuscript Accepted: 28 OCT 2000
  4. Manuscript Received: 26 OCT 2000

Funded by

  • National Institutes of Health, Bethesada, MD, USA. Grant Number: DA 10543; RR 12023

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Abstract

Dansyl-Pro-Gln-Arg-NH2, an N-terminally modified tripeptide amide and a putative neuropeptide FF antagonist, was amenable to both positive-ion ESI and APCI. The protonated molecule yielded several fragment ions upon collision-induced dissociation in a quadrupole ion trap instrument for the development of LC/MS/MS assay methods. ESI clearly outperformed APCI in limits of detection, and was the method of choice for coupling with narrow-bore reversed-phase liquid chromatography to assess the pharmacokinetic profile and brain concentration of the neuropeptide FF antagonist in experimental animals. While plasma could be analyzed after rapid sample preparation, brain tissue required cleanup (solid phase extraction) and preconcentration before injection, and the assay was prone to matrix interference. This study indicated a rapid disappearance of dansyl-Pro-Gln-Arg-NH2 from the plasma and the brain, and modest CNS bioavailability after intravenous administration to rats. Copyright © 2000 John Wiley & Sons, Ltd.

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