Chemistry:DPA-713
From HandWiki
Short description: Chemical compound
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| Formula | C21H26N4O2 |
| Molar mass | 366.465 g·mol−1 |
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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][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
References
- ↑ 1.0 1.1 "2-Arylpyrazolo[1,5-a]pyrimidin-3-yl acetamides. New potent and selective peripheral benzodiazepine receptor ligands". Bioorg. Med. Chem. 9 (10): 2661–2671. 2001. doi:10.1016/S0968-0896(01)00192-4.
- ↑ 2.0 2.1 "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. October 2010. doi:10.1016/j.bmcl.2010.07.135. PMID 20727749.
- ↑ "Synthesis and in vivo evaluation of a novel peripheral benzodiazepine receptor PET radioligand". Bioorganic & Medicinal Chemistry 13 (22): 6188–94. November 2005. doi:10.1016/j.bmc.2005.06.030. PMID 16039131.
- ↑ "Improved synthesis of the peripheral benzodiazepine receptor ligand [11C]DPA-713 using [11C]methyl triflate". Applied Radiation and Isotopes 64 (5): 570–3. May 2006. doi:10.1016/j.apradiso.2005.12.003.
- ↑ "11C-DPA-713: A Novel Peripheral Benzodiazepine Receptor PET Ligand for In Vivo Imaging of Neuroinflammation". J. Nucl. Med. 48 (4): 573–581. 2007. doi:10.2967/jnumed.106.036764.
- ↑ "Initial evaluation of 11C-DPA-713, a novel TSPO PET ligand, in humans". Journal of Nuclear Medicine 50 (8): 1276–82. August 2009. doi:10.2967/jnumed.109.062265. PMID 19617321.
- ↑ "Radiation dosimetry and biodistribution of the TSPO ligand 11C-DPA-713 in humans". Journal of Nuclear Medicine 53 (2): 330–5. February 2012. doi:10.2967/jnumed.111.094565. PMID 22241913.
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