DPA-713 or N,N-diethyl-2-(4-methoxyphenyl)-5,7-dimethylpyrazolo[1,5-a]pyrimidine-3-acetamide is a selective ligand for the translocator protein (TSPO).[1][2]
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| Formula | C21H26N4O2 |
| Molar mass | 366.465 g·mol−1 |
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The binding affinity of DPA-713 for TSPO is reported as Ki = 4.7 ± 0.2 nM.[1][2]
DPA-713 has been radiolabelled with carbon-11 as a potential radiotracer for imaging the TSPO using positron emission tomography (PET).[3][4][5] Radiation dosimetry and biodistribution of [11C]DPA-713 have been assessed in healthy volunteers, indicating that [11C]DPA-713 is a suitable radiotracer for imaging the TSPO in humans.[6][7]
See also
editReferences
edit- ^ a b Selleri S, Bruni F, Costagli C, Costanzo A, Guerrini G, Ciciani G, Costa B, Martini C (2001). "2-Arylpyrazolo[1,5-a]pyrimidin-3-yl acetamides. New potent and selective peripheral benzodiazepine receptor ligands". Bioorg. Med. Chem. 9 (10): 2661–2671. doi:10.1016/S0968-0896(01)00192-4.
- ^ a b Reynolds A, Hanani R, Hibbs D, Damont A, Da Pozzo E, Selleri S, Dollé F, Martini C, Kassiou M (October 2010). "Pyrazolo[1,5-a]pyrimidine acetamides: 4-Phenyl alkyl ether derivatives as potent ligands for the 18 kDa translocator protein (TSPO)". Bioorganic & Medicinal Chemistry Letters. 20 (19): 5799–802. doi:10.1016/j.bmcl.2010.07.135. PMID 20727749.
- ^ James ML, Fulton RR, Henderson DJ, Eberl S, Meikle SR, Thomson S, Allan RD, Dolle F, Fulham MJ, Kassiou M (November 2005). "Synthesis and in vivo evaluation of a novel peripheral benzodiazepine receptor PET radioligand". Bioorganic & Medicinal Chemistry. 13 (22): 6188–94. doi:10.1016/j.bmc.2005.06.030. PMID 16039131.
- ^ Thominiaux C, Dollé F, James ML, Bramoullé Y, Boutin H, Besret L, Grégoire MC, Valette H, Bottlaender M, Tavitian B, Hantraye P, Selleri S, Kassiou M (May 2006). "Improved synthesis of the peripheral benzodiazepine receptor ligand [11C]DPA-713 using [11C]methyl triflate". Applied Radiation and Isotopes. 64 (5): 570–3. doi:10.1016/j.apradiso.2005.12.003.
- ^ Boutin H, Chauveau F, Thominiaux C, Gregoire MC, James ML, Trebossen R, Hantraye P, Dolle F, Tavitian B, Kassiou M (2007). "11C-DPA-713: A Novel Peripheral Benzodiazepine Receptor PET Ligand for In Vivo Imaging of Neuroinflammation". J. Nucl. Med. 48 (4): 573–581. doi:10.2967/jnumed.106.036764.
- ^ Endres CJ, Pomper MG, James M, Uzuner O, Hammoud DA, Watkins CC, Reynolds A, Hilton J, Dannals RF, Kassiou M (August 2009). "Initial evaluation of 11C-DPA-713, a novel TSPO PET ligand, in humans". Journal of Nuclear Medicine. 50 (8): 1276–82. doi:10.2967/jnumed.109.062265. PMC 2883612. PMID 19617321.
- ^ Endres CJ, Coughlin JM, Gage KL, Watkins CC, Kassiou M, Pomper MG (February 2012). "Radiation dosimetry and biodistribution of the TSPO ligand 11C-DPA-713 in humans". Journal of Nuclear Medicine. 53 (2): 330–5. doi:10.2967/jnumed.111.094565. PMC 3274766. PMID 22241913.