DPA-713
DPA-713![]() | |
식별자 | |
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CAS 번호 | |
PubChem CID | |
켐스파이더 | |
유니 | |
화학 및 물리 데이터 | |
공식 | C21H26N4O2 |
몰 질량 | 366.465 g/g−1/g |
3D 모델(JSmol) | |
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DPA-713 또는 N, N-디에틸-2-(4-메톡시페닐)-5,7-디메틸피라졸로[1,5-a]피리미딘-3-아세트아미드는 트랜스로케이터단백질(TSPO)[1][2]의 선택적 배위자이다.
TSPO에 대한 DPA-713의 결합 친화력은 K = 4.7 ± 0.2nM으로 [1][2]보고되었다i.
DPA-713은 양전자방출단층촬영(PET)[3][4][5]을 사용하여 TSPO를 촬영하기 위한 잠재적 방사선 트레이서로서 탄소-11로 방사선을 쬐었다.[C]DPA-713의 11방사선량 측정과 생물 분포는 건강한 지원자를 대상으로 평가되었으며,11 이는 [C]DPA-713이 인간의 [6][7]TSPO 영상촬영에 적합한 방사선 추적기임을 나타낸다.
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레퍼런스
- ^ 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.