76778-24-0
Chemical Structure
GBR-13119
- CAS No.: 76778-24-0
- Formula:C28H33FN2O
- Molecular Weight:432.57
InChIKey: NRFRVJIPDSIXRE-UHFFFAOYSA-N
SMILES: FC1=CC=C(C(C2=CC=CC=C2)OCCN3CCN(CCCC4=CC=CC=C4)CC3)C=C1
Biological Activity: GBR-13119 is a blood-brain barrier-permeable inhibitor of the presynaptic dopamine uptake system. GBR-13119 binds to dopamine uptake sites with high selectivity, without being affected by other neurotransmitter reuptake inhibitors. GBR-13119 exhibits a lipophilic systemic distribution profile with extremely low defluorination in rats, while it shows a differential characteristic of slow striatal washout in the brain of primates. GBR-13119 can serve as a PET tracer to achieve visualized imaging of the striatum in primates, and can reflect MPTP-induced dopaminergic neuron degeneration through reduced uptake. GBR-13119 can be widely applied to studies related to Parkinson's disease and dopaminergic neuron degeneration[1][2].
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GBR-13119 | GBR-13119 is a blood-brain barrier-permeable inhibitor of the presynaptic dopamine uptake system. GBR-13119 binds to dopamine uptake sites with high selectivity, without being affected by other neurotransmitter reuptake inhibitors. GBR-13119 exhibits a lipophilic systemic distribution profile with extremely low defluorination in rats, while it shows a differential characteristic of slow striatal washout in the brain of primates. GBR-13119 can serve as a PET tracer to achieve visualized imaging of the striatum in primates, and can reflect MPTP-induced dopaminergic neuron degeneration through reduced uptake. GBR-13119 can be widely applied to studies related to Parkinson's disease and dopaminergic neuron degeneration. | |||||||||||||||||||||
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References
- [1]. Kilbourn M R, et al. Biodistribution, dosimetry, metabolism and monkey PET studies of [18F] GBR 13119. Imaging the dopamine uptake system in vivo[J]. International Journal of Radiation Applications and Instrumentation. Part B. Nuclear Medicine and Biology, 1989, 16(6): 569-576.
- [2]. Kilbourn MR, et al. Regional brain distribution of [18F]GBR 13119, a dopamine uptake inhibitor, in CD-1 and C57BL/6 mice. Eur J Pharmacol. 1989;166(2):331-334. [Content Brief]
