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Art. -Nr.: HY-183665

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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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CAS. Nr.: 76778-24-0
Formel: C₂₈H₃₃FN₂O
Molecular Weight:432.57

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

GBR-13119 Chemical Structure

CAS. Nr.: 76778-24-0

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

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Biologische Aktivität

Beschreibung

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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.

Chemical Information

CAS. Nr. 76778-24-0
Molecular Weight 432.57
Formel C₂₈H₃₃FN₂O
SMILES

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

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[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]

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Molecular Weight Molecular Weight

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Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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GBR-13119

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