First evaluation of [11C]R116301 as an in vivo tracer of NK1 receptors in man

Molecular Imaging and Biology

Volumn 11, Issue 4, 2009, Pages 241-245

  Wolfensberger, Saskia P A ^a   van Berckel, Bart N M ^a   Airaksinen, Anu J ^a,c   Maruyama, Kaoru ^a,d   Lubberink, Mark ^a   Boellaard, Ronald ^a   Carey, William D H ^b   Reddingius, Wieb ^b   Veltman, Dick J ^a   Windhorst, Albert D ^a   Leysen, Josée E ^a,b   Lammertsma, Adriaan A ^a  

^a VU UNIVERSITY MEDICAL CENTER   (Netherlands)

^b JANSSEN RESEARCH AND DEVELOPMENT   (Belgium)

^c UNIVERSITY OF HELSINKI   (Finland)

^d OSAKA UNIVERSITY GRADUATE SCHOOL OF MEDICINE   (Japan)

Author keywords

11C R116301; NK1 receptor; PET; SUV

Indexed keywords

APREPITANT; CONTRAST MEDIUM; N1 (2,6 DIMETHYLPHENYL) 2 (4 [2 BENZYL 1 [3,5 I (TRIFLUOROMETHYL)BENZOYL]HEXAHYDRO 4 PYRIDINYL]PIPERAZINO]ACETAMIDE; N1 (2,6 DIMETHYLPHENYL) 2 (4 [2 BENZYL 1 [3,5 I (TRIFLUOROMETHYL)BENZOYL]HEXAHYDRO 4 PYRIDINYL]PIPERAZINO]ACETAMIDE C 11; NEUROKININ 1 RECEPTOR; NEUROKININ 1 RECEPTOR ANTAGONIST; R 116301; RADIOLIGAND; UNCLASSIFIED DRUG; BUTANOL; CARBON; LIGAND; MORPHOLINE DERIVATIVE; R116301; RADIOPHARMACEUTICAL AGENT;

ADULT; ARTICLE; CEREBELLUM; CONTROLLED STUDY; CORPUS STRIATUM; DRUG CLEARANCE; DRUG RECEPTOR BINDING; DRUG UPTAKE; FEMALE; HUMAN; HUMAN EXPERIMENT; IMAGE ANALYSIS; IN VIVO STUDY; MALE; POSITRON EMISSION TOMOGRAPHY; PRIORITY JOURNAL; SINGLE DRUG DOSE; BRAIN; IMAGE PROCESSING; METABOLISM; METHODOLOGY; MIDDLE AGED; PILOT STUDY; SCINTISCANNING;

ADULT; BRAIN; BUTANOLS; CARBON ISOTOPES; FEMALE; HUMANS; IMAGE PROCESSING, COMPUTER-ASSISTED; LIGANDS; MALE; MIDDLE AGED; MORPHOLINES; PILOT PROJECTS; POSITRON-EMISSION TOMOGRAPHY; RADIOPHARMACEUTICALS; RECEPTORS, NEUROKININ-1;

EID: 67649411594     PISSN: 15361632     EISSN: 18602002     Source Type: Journal    
DOI: 10.1007/s11307-009-0204-5     Document Type: Article

References (35)

1. Otsuka M, Yoshioka K (1993) Neurotransmitter functions of mammalian tachykinins. Physiol Rev 73:229-308
2. Quartara L, Maggi CA (1997) The tachykinin NK1 receptor. Part I: Ligands and mechanisms of cellular activation. Neuropeptides 31:537-563
3. Quartara L, Maggi CA (1998) The tachykinin NK1 receptor. Part II: distribution and pathophysiological. Neuropeptides 32:1-49
4. Hargreaves R (2002) Imaging substance P receptors (NK1) in the living human brain using positron emission tomography. J Clin Psychiatry 63(Suppl 11):18-24
5. Hietala J, Nyman MJ, Eskola I et al (2005) Visualization and quantification of neurokinin-1 (NK1) receptors in the human brain. Mol Imag Biol 7:262-272
6. Farthing MJG (2004) Novel agents for the control of secretory diarrhoea. Expert Opin Investig Drugs Expert 13:777-785
7. Hosoki R, Yanagisawa M, Onishi Y, Yoshioka K, Otsuka M (1998) Pharmacological profiles of new orally active nonpeptide tachykinin NK1 receptor antagonists. Eur J Pharmacol 341:235-241
8. Walpole CSJ, Brown MCS, James IF et al (1998) Comparative, general pharmacology of SDZ NKT 343, a novel, selective NK1 receptor antagonist. Br J Pharmacol 124:83-92
9. De Felipe C, Herrero JF, O'Brien JA et al (1998) Altered nociception, analgesia and aggression in mice lacking the receptor for substance P. Nature 392:394-397
10. Kent JM, Mathew SJ, Gorman JM (2002) Molecular targets in the treatment of anxiety. Biol Psychiatry 52:1008-1030
11. Kramer MS, Cutler N, Feighner J et al (1998) Distinct mechanism for antidepressant activity by blockade of central substance P receptors. Science 281:1640-1645
12. Krishnan KRR (2002) Clinical experience with substance P receptor (NK1) antagonists in depression. J Clin Psychiatry 63:25-29
13. Rupniak NM (2002) Elucidating the antidepressant actions of substance P (NK1 receptor) antagonists. Curr Opin Investig Drugs 3:257-261
14. Keller M, Montgomery S, Ball W et al (2006) Lack of efficacy of the substance P (neurokinin(1) receptor) antagonist aprepitant in the treatment of major depressive disorder. Biol Psychiatry 59:216-223
15. Dando TM, Perry CM (2004) Aprepitant-A review of its use in the prevention of chemotherapy-induced nausea and vomiting. Drugs 64:777-794
16. Hesketh PJ, Grunberg SM, Gralla RJ et al (2003) The oral neurokinin-1 antagonist aprepitant for the prevention of chemotherapy-induced nausea and vomiting: A multinational, randomized, double-blind, placebo-controlled trial in patients receiving high-dose cisplatin-The Aprepitant Protocol 052 Study Group. J Clin Oncol 21:4112-4119
17. Breeman WAP, VanHagen MP, VisserWisselaar HA et al (1996) In vitro and in vivo studies of substance P receptor expression in rats with the new analog [indium-111-DTPA-Arg(1)]substance P. J Nucl Med 37:108-117
18. Delrosario RB, Mangner TJ, Gildersleeve DL et al (1993) Synthesis of a nonpeptide C-11 labeled substance-P antagonist for PET studies. Nucl Med Biol 20:545-547
19. Livni E, Babich JW, Desai MC et al (1995) Synthesis of a C-11 labeled Nk1 receptor-ligand for PET studies. Nucl Med Biol 22:31-36
20. Francis BE, Swain C, Sabin V, Burns HD (1994) Radioiodinated L-703,606 - a potent, selective antagonist to the human NK(1) receptor. Appl Radiat Isotopes 45:97-103
21. Solin O, Eskola O, Hamill TG et al (2004) Synthesis and characterization of a potent, selective, radiolabeled substance-P antagonist for NK1 receptor quantitation: ([F-18]SPA-RQ). Mol Imag Biol 6:373-384
22. Bergstrom M, Fasth KJ, Kilpatrick G et al (2000) Brain uptake and receptor binding of two [C-11]labelled selective high affinity NK1-antagonists, GR203040 and GR205171-PET studies in rhesus monkey. Neuropharmacology 39:664-670
23. Bergstrom M, Hargreaves RJ, Burns HD et al (2004) Human positron emission tomography studies of brain neurokinin 1 receptor occupancy by aprepitant. Biol Psychiatry 55:1007-1012
24. Van der Mey M, Janssen CGM, Janssens FE et al (2005) Synthesis and biodistribution of [C-11]R116301, a promising PET ligand for central NK1 receptors. Bioorg Med Chem 13:1579-1586
25. Megens AA, Ashton D, Vermeire JC et al (2002) Pharmacological profile of (2R-trans)-4-[1-[3,5-bis(trifluoromethyl)benzoyl]-2-(phenylmethyl)-4 -piper idinyl]-N-(2,6-dimethylphenyl)-1-acetamide (S)-hydroxybutanedioate (R116301), an orally and centrally active neurokinin-1 receptor antagonist. J Pharmacol Exp Ther 302:696-709
26. First MB, Spitzer RL, Gibbon M, Williams JBW (1996) Structured clinical interview for DSM-IV clinical version (SCID-I/CV). American Psychiatric Press, Washington, DC
27. Brix G, Zaers J, Adam LE et al (1997) Performance evaluation of a whole-body PET scanner using the NEMA protocol. J Nucl Med 38:1614-1623
28. Boellaard R, van Lingen A, van Balen SCM, Hoving BG, Lammertsma AA (2001) Characteristics of a new fully programmable blood sampling device for monitoring blood radioactivity during PET. Eur J Nucl Med 28:81-89
29. Defrise M, Kinahan PE, Townsend DW, Michel C, Sibomana M, Newport DF (1997) Exact and approximate rebinning algorithms for 3-D PET data. IEEE Trans Med Imag 16:145-158
30. Maes F, Collignon A, Vandermeulen D, Marchal G, Suetens P (1997) Multimodality image registration by maximization of mutual information. IEEE Trans Med Imag 16:187-198
31. West J, Fitzpatrick JM, Wang MY et al (1997) Comparison and evaluation of retrospective intermodality brain image registration techniques. J Comput Assist Tomogr 21:554-566
32. Zhang YY, Brady M, Smith S (2001) Segmentation of brain MR images through a hidden Markov random field model and the expectation-maximization algorithm. IEEE Trans Med Imag 20:45-57
33. Hoekstra CJ, Paglianiti I, Hoekstra OS et al (2000) Monitoring response to therapy in cancer using [F-18]-2-fluouo-2-deoxy-D-glucose and positron emission tomography: An overview of different analytical methods. Eur J Nucl Med 27:731-743
34. Nyman MJ, Eskola O, Kajander J et al (2007) Gender and age affect NK1 receptors in the human brain-a positron emission tomography study with [F-18]SPA-RQ. J Comput Assist Tomogr 10:219-229
35. Griffante C, Carletti R, Andreetta F, Corsi M (2006) [3H]GR205171 displays similar NK1 receptor binding profile in gerbil and human brain. Br J Pharmacol 148:39-45