2. GPCR/G Protein Neuronal Signaling
  3. Dopamine Receptor
  4. 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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GBR-13119

GBR-13119 Chemical Structure

CAS No. : 76778-24-0

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Description

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].

In Vivo

[18F]GBR-13119 (7-10 μCi; i.v.; single dose) exhibits regional brain distribution consistent with dopaminergic neuron localization in healthy CD-1 and C57BL/6 mice, with striatum/cerebellum ratios greater than 3 at 60 minutes post-injection[2].
[18F]GBR-13119 (7-10 μCi; i.v.; single dose) shows significantly reduced striatum/cerebellum ratios (≈50% reduction) in MPTP-lesioned C57BL/6 mice, indicating its ability to detect dopaminergic neuron degeneration[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: CD-1 Mice (male, 20-25 g); C57BL/6 (female, 25-30 g)[2]
Dosage: 7-10 μCi
Administration: i.v.; single dose
Result: Exhibited striatum radioactivity of 2.8 %ID/g, cortex radioactivity of 0.98 %ID/g, cerebellum radioactivity of 0.66 %ID/g, blood radioactivity of 0.89 %ID/g, striatum/cerebellum ratio of 4.24, striatum/cortex ratio of 2.98, and striatum/blood ratio of 3.3 in CD-1 mice at 60 minutes post-injection.
Exhibited striatum radioactivity of 2.9 %ID/g, cortex radioactivity of 1.13 %ID/g, cerebellum radioactivity of 0.86 %ID/g, blood radioactivity of 0.70 %ID/g, striatum/cerebellum ratio of 3.35, striatum/cortex ratio of 2.51, and striatum/blood ratio of 4.4 in C57BL/6 mice at 60 minutes post-injection.
Animal Model: C57BL/6 Mice with Dopaminergic neuron degeneration (male, 10 weeks old, chronic MPTP lesioning via 30 mg/kg s.c. twice daily for 4 days)[2]
Dosage: 7-10 μCi
Administration: i.v.; single dose
Result: Exhibited striatum radioactivity of 0.63 %ID/g and 0.93 %ID/g, cortex radioactivity of 0.45 %ID/g and 0.75 %ID/g, cerebellum radioactivity of 0.39 %ID/g and 0.52 %ID/g, blood radioactivity of 0.49 %ID/g and 0.56 %ID/g, striatum/cerebellum ratio of 1.61 and 1.79, striatum/cortex ratio of 1.4 and 1.24, and striatum/blood ratio of 1.29 and 1.67 in MPTP-lesioned mice at 60 minutes post-injection.
Showed an approximately 50% reduction in striatum/cerebellum ratio compared to control C57BL/6 mice.
Molecular Weight

432.57

Formula

C28H33FN2O
CAS No.
SMILES

FC1=CC=C(C(C2=CC=CC=C2)OCCN3CCN(CCCC4=CC=CC=C4)CC3)C=C1
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Keywords:

GBR-1311976778-24-0GBR13119GBR 13119Dopamine Receptorratspresynaptic dopamine uptake sitescerebellumdopaminergic neuron degenerationprimate brainMPTP-treated miceblood-brain barrierneuronal dopamine uptake systemstriatumparkinson's diseaseInhibitorinhibitorinhibit

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