DPA-713

DPA-713
Identifiers
CAS Number 386297-97-8
Chemical and physical data
Formula C21H26N4O2
Molar mass 366.46 g/mol

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]

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] Radiation dosimetry and biodistribution of [11C]DPA-713 have been assessed in healthy volunteers, indicating that [11C]DPA-713 is a suitable radioatracer for imaging the TSPO in humans.[5][6]

See also

References

  1. 1 2 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.
  2. 1 2 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)". Bioorg. Med. Chem. Lett. 20 (19): 5799–802. doi:10.1016/j.bmcl.2010.07.135. PMID 20727749.
  3. ↑ 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 (2006). "Improved synthesis of the peripheral benzodiazepine receptor ligand [11C]DPA-713 using [11C]methyl triflate". Appl. Radiat. Isotopes. 64 (5): 570–573. doi:10.1016/j.apradiso.2005.12.003.
  4. ↑ 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.
  5. ↑ Endres CJ, Pomper MG, James M, Uzuner O, Hammoud DA, Watkins CC, Reynolds A, Hilton J, Dannals RF, Kassiou M (2009). "Initial Evaluation of 11C-DPA-713, a Novel TSPO PET Ligand, in Humans". J. Nucl. Med. 50 (8): 1276–1282. doi:10.2967/jnumed.109.062265.
  6. ↑ Endres CJ, Coughlin JM, Gage KL, Watkins CC, Kassiou M, Pomper MG (2012). "Radiation Dosimetry and Biodistribution of the TSPO Ligand 11C-DPA-713 in Humans". J. Nucl. Med. 53 (2): 330–335. doi:10.2967/jnumed.111.094565.
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