Synonym
SP203; SP 203; SP-203.
IUPAC/Chemical Name
3-fluoro-5-[2-[2-(fluoromethyl)-1,3-thiazol-4-yl]ethynyl]benzonitrile
InChi Key
WTLBLIGPXACYET-UHFFFAOYSA-N
InChi Code
InChI=1S/C13H6F2N2S/c14-6-13-17-12(8-18-13)2-1-9-3-10(7-16)5-11(15)4-9/h3-5,8H,6H2
SMILES Code
N#CC1=CC(C#CC2=CSC(CF)=N2)=CC(F)=C1
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
Preparing Stock Solutions
The following data is based on the
product
molecular weight
260.26
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
1: Lohith TG, Tsujikawa T, Siméon FG, Veronese M, Zoghbi SS, Lyoo CH, Kimura Y, Morse CL, Pike VW, Fujita M, Innis RB. Comparison of two PET radioligands, [(11)C]FPEB and [(11)C]SP203, for quantification of metabotropic glutamate receptor 5 in human brain. J Cereb Blood Flow Metab. 2016 Jan 1:271678X16668891. doi: 10.1177/0271678X16668891. [Epub ahead of print] PubMed PMID: 27629098.
2: Siméon FG, Liow JS, Zhang Y, Hong J, Gladding RL, Zoghbi SS, Innis RB, Pike VW. Synthesis and characterization in monkey of [11C]SP203 as a radioligand for imaging brain metabotropic glutamate 5 receptors. Eur J Nucl Med Mol Imaging. 2012 Dec;39(12):1949-58. doi: 10.1007/s00259-012-2205-x. Epub 2012 Aug 11. PubMed PMID: 22885775.
3: Kimura Y, Siméon FG, Zoghbi SS, Zhang Y, Hatazawa J, Pike VW, Innis RB, Fujita M. Quantification of metabotropic glutamate subtype 5 receptors in the brain by an equilibrium method using 18F-SP203. Neuroimage. 2012 Feb 1;59(3):2124-30. doi: 10.1016/j.neuroimage.2011.10.028. Epub 2011 Oct 19. PubMed PMID: 22032949; PubMed Central PMCID: PMC3254783.
4: Kimura Y, Siméon FG, Hatazawa J, Mozley PD, Pike VW, Innis RB, Fujita M. Biodistribution and radiation dosimetry of a positron emission tomographic ligand, 18F-SP203, to image metabotropic glutamate subtype 5 receptors in humans. Eur J Nucl Med Mol Imaging. 2010 Oct;37(10):1943-9. doi: 10.1007/s00259-010-1447-8. Epub 2010 Jun 29. PubMed PMID: 20585776; PubMed Central PMCID: PMC3207261.
5: Shetty HU, Zoghbi SS, Siméon FG, Liow JS, Brown AK, Kannan P, Innis RB, Pike VW. Radiodefluorination of 3-fluoro-5-(2-(2-[18F](fluoromethyl)-thiazol-4-yl)ethynyl)benzonitrile ([18F]SP203), a radioligand for imaging brain metabotropic glutamate subtype-5 receptors with positron emission tomography, occurs by glutathionylation in rat brain. J Pharmacol Exp Ther. 2008 Dec;327(3):727-35. doi: 10.1124/jpet.108.143347. Epub 2008 Sep 19. Erratum in: J Pharmacol Exp Ther. 2009 Mar;328(3):1019. PubMed PMID: 18806125; PubMed Central PMCID: PMC2679677.