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GBR 12783 dihydrochloride

Names

[ CAS No. ]:
67469-75-4

[ Name ]:
GBR 12783 dihydrochloride

[Synonym ]:
2,9,10(1H)-Anthracenetrione,6-ethyl-4,5-dihydroxy-1,1,3,7-tetramethyl
Kenpaullone
garvatin B quinone

Biological Activity

[Description]:

GBR 12783 dihydrochloride is a specific, potent and selective dopamine uptake inhibitor that inhibits the [3H]dopamine uptake by rat and mice striatal synaptosomes with IC50s of 1.8 nM and 1.2 nM, respectively. GBR 12783 dihydrochloride can improve memory performance and increase hippocampal acetylcholine release in rats[1][2].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Dopamine Receptor
Signaling Pathways >> Neuronal Signaling >> Dopamine Receptor
Research Areas >> Neurological Disease

[In Vivo]

GBR 12783 (10 mg/kg; intraperitoneal injection; for 100 minutes; male Sprague-Dawley rats) treatment reinforces specifically dopamine transmission only at synapses instantaneously active, increases hippocampal ACh release and improves memory performance in a passive avoidance task[1]. Animal Model: Male Sprague-Dawley rats (180-200 g)[1] Dosage: 10 mg/kg Administration: Intraperitoneal injection; for 100 minutes Result: For a moderate electric shock intensity (0.4 mA), improveed retention performance, increased hippocampal acetylcholine release in vivo.

[References]

[1]. Nail-Boucherie K, et al. The specific dopamine uptake inhibitor GBR 12783 improves learning of inhibitory avoidance and increases hippocampal acetylcholine release. Brain Res Cogn Brain Res. 1998 Oct;7(2):203-5.

[2]. Bonnet JJ, et al. GBR 12783, a potent and selective inhibitor of dopamine uptake: biochemical studies in vivo and ex vivo. Eur J Pharmacol. 1986 Feb 18;121(2):199-209.

Chemical & Physical Properties

[ Molecular Formula ]:
C28H34Cl2N2O

[ Molecular Weight ]:
485.48800

[ Exact Mass ]:
484.20500

[ PSA ]:
15.71000

[ LogP ]:
6.60340

Safety Information

[ Hazard Codes ]:
Xi

Synthetic Route


Related Compounds