Nuclear Medicine and Biology
Volume 36, Issue 4 , Pages 389-393 , May 2009

Application of highly sensitive UPLC–MS to determine biodistribution at tracer doses: validation with the 5-HT1A ligand [18F]FPWAY

Received 13 August 2008 ,Revised 12 December 2008 ,Accepted 12 January 2009.

References 

  1. Phelps ME. PET: physics, instrumentation and scanners. New York: Springer; 2006;
  2. Welch MJ, Redvanly CS. Handbook of Radiopharmaceuticals. 1st ed.. New York: Wiley; 2002;
  3. Stöcklin G, Pike VW. Radiopharmaceuticals for positron emission tomography — methodological aspects. 1st ed.. Dordrecht, Netherlands: Kluwer Acedemic Press; 1993;
  4. Giovacchini G, Lang L, Ma Y, Herscovitch P, Eckelman W, Carson RE. Differential effects of the selective serotonin reuptake inhibitor paroxetine on raphe and cortical 5-HT1A binding; A PET study in monkey with [18F]FPWAY. Neuroimage. 2004;22(Suppl 2):T25–T26
  5. Lang L, Jagoda E, Schmall B, Sassaman M, Ma Y, et al. Fluoro analogs of WAY-100635 with varying pharmacokinetics properties. Nucl Med Biol. 2000;27:457–462
  6. Lang L, Jagoda E, Schmall B, Sassaman M, Ma Y, Eckelman WC. Fluoro analogs of WAY-100635 with varying pharmacokinetics properties. Nucl Med Biol. 2000;27(5):457–462
  7. Fletcher A, Clif IA, Dourish CT. Silent 5-TH1A receptor antagonist: utility as research and therapeutic agents. TIPS. 1993;141:441–448
  8. Ma Y, Kiesewetter D, Lang L, Eckelman WC. Application of LC-MS to the analysis of new radiopharmaceuticals. Mol Imaging Biol. 2003;5(6):397–403
  9. Ma Y, Lang L, Kiesewetter D, Jagoda E, Eckelman WC. Species differences in metabolites of PET ligands — serotonergic 5-HT1A receptor antagonists, 3-trans and 3-cis-FCWAY. Nucl Med Biol. 2006;33:1013–1019
  10. Matusch A, Meyer P, Bier D, Holschbach M, Woitalla D, Elmenhorst D, et al. Metabolism of the A1 adenosine receptor PET ligand [18F]CPFPX by CYP1A2: implications for bolus/infusion PET studies. Nucl Med Biol. 2006;33:891–898
  11. Ma Y, Kiesewetter DO, Lang L, Der Margaret , Huang BX, Carson RE, et al. Determination of [18F]FC-WAY, [18F]FP-TZTP, and their metabolites in plasma using rapid and efficient liquid–liquid and solid phase extractions. Nucl Med Biol. 2003;30:235–240
  12. Chernet E, Martin LJ, Li D, Need AB, Barth VN, Rash KS, et al. Use of LC/MS to assess brain tracer distribution in preclinical, in vivo receptor occupancy studies: dopamine D2, serotonin 2A and NK-1 receptors as examples. Life Sci. 2005;78:340–346
  13. Barth VN, Chernet E, Martin LJ, Need AB, Rash KS, Morin M, et al. Comparison of rat dopamine D2 receptor occupancy for a series of antipsychotic drugs measured using radiolabeled or nonlabeled raclopride tracer. Life Sci. 2006;78:3007–3012
  14. Mathis CA, Simpson NR, Mahmood K, Kinahan PE, Mintun MA. [11C]WAY 100635: a radioligand for imaging 5-HT1A receptors with positron emission tomography. Life Sci. 1994;403–407
  15. Pike VW, McCarron JA, Lammertsma AA, Hume SP, Poole K, et al. First delineation of 5-HT1A receptors in human brain with PET and [11C]WAY-100635. Eur J Pharmacol. 1995;283:R1–R3
  16. Lang L, Jagoda E, Schmall B, Vuong BK, Adams HR, et al. The development of fluorine-18-labeled 5-HT1A antagonists. J Med Chem. 1999;42:1576–1586
  17. Carson RE, Lang L, Watabe H, Der MG, Adams HR, et al. PET evaluation of [(18)F]FCWAY, an analog of the 5-HT(1A) receptor antagonist, WAY-100635. Nucl Med Biol. 2000;27:493–497
  18. Lang L, Jagoda E, Ma Y, Sassaman MB, Eckelman WC. Synthesis and in vivo biodistribution of F-18 labeled 3-cis-, 3-trans-, 4-cis-, and 4-trans fluorocyclohexane derivatives of WAY 100635. Bioorg Med Chem. 2006;14:3737–3748

PII: S0969-8051(09)00002-X

doi: 10.1016/j.nucmedbio.2009.01.002

Nuclear Medicine and Biology
Volume 36, Issue 4 , Pages 389-393 , May 2009