Synthesis and characterization of a potent, selective, radiolabeled substance-P antagonist for NK1 receptor quantitation: ([18F]SPA-RQ)

Molecular Imaging and Biology

Volumn 6, Issue 6, 2004, Pages 373-384

  Solin, Olof ^a   Eskola, Olli ^a   Hamill, Terence G ^b   Bergman, Jörgen ^a   Lehikoinen, Pertti ^a   Grönroos, Tove ^a   Forsback, Sarita ^a   Haaparanta, Merja ^a   Viljanen, Tapio ^a   Ryan, Christine ^b   Gibson, Raymond ^b   Kieczykowski, Gerard ^b   Hietala, Jarmo ^a   Hargreaves, Richard ^b   Burns, H Donald ^b  

^a TURKU PET CENTRE   (Finland)

^b MERCK RESEARCH LABORATORIES   (United States)

Author keywords

F 18; Fluorine 18; Neutokinin 1 receptor; NK1 receptor imaging; PET occupancy; Substance P antagonist

Indexed keywords

[2 FLUOROMETHOXY 5 (5 TRIFLUOROMETHYLTETRAZOL 1 YL)BENZYL](2 PHENYLPIPERIDIN 3 YL)AMINE; BROMOFLUOROMETHANE F 18; FLUORINE 18; FLUOROMETHANE F 18; NEUROKININ 1 RECEPTOR; NEUROKININ 1 RECEPTOR ANTAGONIST; PHENOL DERIVATIVE; SUBSTANCE P ANTAGONIST; TRIFLUOROACETIC ACID; UNCLASSIFIED DRUG;

ALKYLATION; ANIMAL EXPERIMENT; ARTICLE; BINDING AFFINITY; BLOOD BRAIN BARRIER; BRAIN CORTEX; CONTROLLED STUDY; CORPUS STRIATUM; DRUG DETERMINATION; DRUG DISTRIBUTION; DRUG PENETRATION; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG SELECTIVITY; DRUG SPECIFICITY; DRUG STRUCTURE; DRUG SYNTHESIS; GAS CHROMATOGRAPHY; GUINEA PIG; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HUMAN; ISOTOPE LABELING; LIQUID CHROMATOGRAPHY; MALE; MASS SPECTROMETRY; NEUROIMAGING; NON INVASIVE MEASUREMENT; NONHUMAN; POSITRON EMISSION TOMOGRAPHY; PRIORITY JOURNAL; PROTON NUCLEAR MAGNETIC RESONANCE; QUANTITATIVE ANALYSIS; RHESUS MONKEY;

ANIMALS; BRAIN; FLUORINE RADIOISOTOPES; GUINEA PIGS; HUMANS; HYDROCARBONS, BROMINATED; HYDROCARBONS, FLUORINATED; MACACA MULATTA; MALE; MOLECULAR STRUCTURE; POSITRON-EMISSION TOMOGRAPHY; RECEPTORS, NEUROKININ-1; SENSITIVITY AND SPECIFICITY; SPECTRUM ANALYSIS; SUBSTANCE P; TISSUE DISTRIBUTION;

CAVIA PORCELLUS; MACACA MULATTA; SUS SCROFA;

EID: 10244242680     PISSN: 15361632     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.mibio.2004.08.001     Document Type: Article

References (25)

1. C.A. Maggi R. Patacchini P. Rovero et al. Tachykinin receptors and tachykinin receptor antagonist J. Auton. Pharmacol. 13 1993 23-93
2. 1 receptor. Part I: ligands and mechanisms of cellular activation Neuropeptides 31 1997 537-563
3. 1 receptor. Part II: distribution and pathophysiological roles Neuropeptides 32 1998 1-49
4. M. Otsuka K. Yoshioka Neurotransmitter functions of mammalian tachykinins Physiol. Rev. 73 1993 229-308
5. T. Harrison A.P. Owens B.J. Williams et al. An orally active, water-soluble neurokinin-1 receptor antagonist suitable for both intravenous and oral clinical administration J. Med. Chem. 44 2001 4296-4299
6. 1 receptor antagonists Eur. J. Pharmacol. 341 1998 235-241
7. S. Iyengar P.A. Hipskind D.R. Gehlert et al. LY303870, a centrally active neurokinin-1 antagonist with a long duration of action J. Pharmacol. Exp. Ther. 280 1997 774-785
8. D. Regoli F. Nantel Pharmacology of neurokinin receptors Biopolymers 31 1997 774-785
9. 1 receptor antagonist Br. J. Pharmacol. 124 1998 83-92
10. C. Walpole S.Y. Ko M. Brown et al.
11. 1) receptor Science 251 1991 435-437
12. 1 receptor J. Pharmacol. Exp. Ther. 277 1996 900-908
13. M.S. Kramer N. Cutler J. Feighner et al. Distinct mechanism for antidepressant activity by blockade of central substance P receptors Science 281 1998 1640-1645
14. R.M. Navari R.R. Reinhardt R.J. Gralla et al. Reduction of cisplatin-induced emesis by a selective neurokinin-1-receptor antagonist N. Eng. J. Med. 340 1999 190-195
15. 1) antagonists Trends Pharmacol. Sci. 20 1999 485-490
16. L. Friedman NK-1 antagonists: The next generation of depression therapy Curr. Psych. 1 3 2002
17. C. De Felipe J.F. Herrero J.A. O'Brien et al. Altered nociception, analgesia and aggression in mice lacking the receptor for substance P Nature 392 1998 394-397
18. W. Breeman M. VanHagen H. Visser-Wisselaar et al. In vitro and in vivo studies of substance P receptor expression in rats with the new analogue (Indium-111-DTPA-Arg)substance P J. Nucl. Med. 37 1996 108-117
19. R.B. Del Rosario T.J. Mangner D.L. Gildersleeve et al. Synthesis of a nonpeptide carbon-11 labeled substance P antagonist for PET studies Nucl. Med. Biol. 20 4 1993 545-547
20. 1 receptor ligand for PET studies Nucl. Med. Biol. 22 1 1995 31-36
21. 1 receptor Appl. Radiat. Isot. 45 1 1994 97-103
22. 1-antagonists, GR203040 and GR205171 - PET studies in rhesus monkey Neuropharm. 39 2000 664-670
23. M.C. Desai S.L. Lefkowitz P.F. Thadeio et al. Discovery of a potent substance P antagonist: Recognition of the key molecular determinant J. Med. Chem. 35 26 1992 4911-4913
24. 18F]bromofluoromethane at high specific radioactivity Appl. Radiat. Isot. 54 2001 927-933
25. 18F]fluoromethyliodide, a synthetic precursor for fluoromethylation of radiopharmaceuticals Appl. Radiat. Isot. 52 2000 55-61