| 词条 | DPA-714 |
| 释义 |
| IUPAC_name = N,N-diethyl-2-[4-(2-fluoroethoxy)phenyl]-5,7-dimethylpyrazolo[1,5-a]pyrimidine-3-acetamide | image = DPA-714.tif | tradename = | pregnancy_AU = | pregnancy_US = | pregnancy_category = | legal_AU = | legal_CA = | legal_UK = | legal_US = | legal_status = | routes_of_administration = | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion = | CAS_number_Ref = | CAS_number = 958233-07-3 | ATC_prefix = | ATC_suffix = | PubChem = | DrugBank_Ref = | DrugBank = | ChemSpiderID_Ref = | ChemSpiderID = 23328478 | ChEMBL = 512306 | C=22 | H=27 | N=4 | O=2 | F=1 | molecular_weight = 398.47 g/mol | smiles = CCN(CC)C(=O)Cc1c(nn2c1nc(cc2C)C)c3ccc(cc3)OCCF | StdInChI = 1S/C22H27FN4O2/c1-5-26(6-2)20(28)14-19-21(17-7-9-18(10-8-17)29-12-11-23)25-27-16(4)13-15(3)24-22(19)27/h7-10,13H,5-6,11-12,14H2,1-4H3 | StdInChIKey = FLZZFWBNYJNHMY-UHFFFAOYSA-N }}DPA-714 or N,N-diethyl-2-[4-(2-fluoroethoxy)phenyl]-5,7-dimethylpyrazolo[1,5-a]pyrimidine-3-acetamide is a selective ligand for the translocator protein (TSPO) currently under evaluation for several clinical applications.[1] For this reason, a practical, multigram synthetic route for its preparation has been described.[2] The binding affinity of DPA-714 for TSPO is reported as Ki = 7.0 ± 0.4 nM.[3][4] [18F]DPA-714 is currently under investigation as a potential radiopharmaceutical for imaging TSPO in living systems using positron emission tomography (PET). DPA-714, along with other members of the DPA class of TSPO ligands, has been shown to decrease microglial activation and increase neuronal survival in a quinolinic acid rat model of excitotoxic neurodegeneration, suggesting potential neuroprotective effects.[5] See also
References1. ^{{cite journal |vauthors=Reynolds A, Hanani R, Hibbs D, Damont A, Da Pozzo E, Selleri S, Dollé F, Martini C, Kassiou M | title = Pyrazolo[1,5-a]pyrimidine acetamides: 4-Phenyl alkyl ether derivatives as potent ligands for the 18 kDa translocator protein (TSPO) | journal = Bioorg. Med. Chem. Lett. | volume = 20 | issue = 19 | pages = 5799–802 |date=October 2010 | pmid = 20727749 | doi = 10.1016/j.bmcl.2010.07.135 }} 2. ^{{Cite journal | last1 = Banister | first1 = S. D. | last2 = Wilkinson | first2 = S. M. | last3 = Hanani | first3 = R. | last4 = Reynolds | first4 = A. J. | last5 = Hibbs | first5 = D. E. | last6 = Kassiou | first6 = M. | doi = 10.1016/j.tetlet.2012.05.044 | title = A practical, multigram synthesis of the 2-(2-(4-alkoxyphenyl)-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)acetamide (DPA) class of high affinity translocator protein (TSPO) ligands | journal = Tetrahedron Letters | volume = 53 | issue = 29 | pages = 3780 | year = 2012 | pmid = | pmc = }} 3. ^{{cite journal |vauthors=James ML, Fulton RR, Vercoullie J, Henderson DJ, Garreau L, Chalon S, Dolle F, Costa B, Selleri S, Guilloteau D, Kassiou M | title = DPA-714, a new translocator protein-specific ligand: synthesis, radiofluorination, and pharmacologic characterization | journal = J. Nucl. Med. | volume = 49 | issue = 5 | pages = 814–22 |date=May 2008 | pmid = 18413395 | doi = 10.2967/jnumed.107.046151 | url = }} 4. ^{{cite journal |vauthors=Damont A, Hinnen F, Kuhnast B, Schöllhorn-Peyronneau MA, James M, Luus C, Tavitian B, Kassiou M, Dollé F | title = Radiosynthesis of [18F]DPA-714, a selective radioligand for imaging the translocator protein (18 kDa) with PET | volume = 51 | issue = 7 | pages = 286–292 | year = 2008 | pmid = | doi = 10.1002/jlcr.1523 | journal = Journal of Labelled Compounds and Radiopharmaceuticals}} 5. ^{{cite journal |vauthors=Leaver KR, Reynolds A, Bodard S, Guilloteau D, Chalon S, Kassiou M | title = Effects of Translocator Protein (18 kDa) Ligands on Microglial Activation and Neuronal Death in the Quinolinic-Acid-Injected Rat Striatum | volume = 3 | issue = 2 | pages = 114–119 | year = 2011 | doi = 10.1021/cn200099e | pmid = 22860181 | journal = ACS Chemical Neuroscience | pmc = 3369788 }} 2 : Pyrazolopyrimidines|TSPO ligands |
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