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| | 2-Pyrrolidinone, 1-[(3-methyl-4-pyridinyl)methyl]-4-(3,4,5-trifluorophenyl)-, (4R)- Basic information |
| | 2-Pyrrolidinone, 1-[(3-methyl-4-pyridinyl)methyl]-4-(3,4,5-trifluorophenyl)-, (4R)- Chemical Properties |
| Boiling point | 474.1±45.0 °C(Predicted) | | density | 1.329±0.06 g/cm3(Predicted) | | pka | 5.49±0.18(Predicted) | | form | Solid | | color | White to off-white |
| | 2-Pyrrolidinone, 1-[(3-methyl-4-pyridinyl)methyl]-4-(3,4,5-trifluorophenyl)-, (4R)- Usage And Synthesis |
| Uses | UCB-J is a positron emission tomography (PET) radioligand for the synaptic vesicle protein 2A (SV2A)[1][2][3][4]. | | in vivo | UCB-J exhibits high free fraction (0.46 ± 0.02) and metabolizes at a moderate rate (39% ± 5% and 24% ± 3% parent remaining at 30 and 90 min) in plasma[3].
UCB-J displays high uptake and fast kinetics in the monkey brain[3].
When the animal is pretreated with UCB-J (150 μg/kg, iv), the whole brain SUV decreases to the same level as centrum semiovale, indicating the in vivo binding specificity of [18F]7 to SV2A[4].
| | References | [1] Jol Mercier, et al. Discovery of heterocyclic nonacetamide synaptic vesicle protein 2A (SV2A) ligands with single-digit nanomolar potency: opening avenues towards the first SV2A positron emission tomography (PET) ligands. ChemMedChem. 2014 Apr;9(4):693-8. DOI:10.1002/cmdc.201300482 [2] Aline Delva, et al. Loss of Presynaptic Terminal Integrity in the Substantia Nigra in Early Parkinson's Disease. Mov Disord. 2020 Aug 7. DOI:10.1002/mds.28216 [3] Nabeel B Nabulsi, et al. Synthesis and Preclinical Evaluation of 11C-UCB-J as a PET Tracer for Imaging the Synaptic Vesicle Glycoprotein 2A in the Brain. J Nucl Med. 2016 May;57(5):777-84. DOI:10.2967/jnumed.115.168179 [4] Zhengxin Cai, et al. Synthesis and Preclinical Evaluation of an 18 F-Labeled Synaptic Vesicle Glycoprotein 2A PET Imaging Probe: [ 18 F]SynVesT-2. ACS Chem Neurosci. 2020 Feb 19;11(4):592-603. DOI:10.1021/acschemneuro.9b00618 |
| | 2-Pyrrolidinone, 1-[(3-methyl-4-pyridinyl)methyl]-4-(3,4,5-trifluorophenyl)-, (4R)- Preparation Products And Raw materials |
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