GBR 12783 dihydrochloride

Names

[ Name ]:
GBR 12783 dihydrochloride

[Synonym ]:
1-[2-(Diphenylmethoxy)ethyl]-4-[(2E)-3-phenylprop-2-en-1-yl]piperazine dihydrochloride
1-[2-(Diphenylmethoxy)ethyl]-4-[(2E)-3-phenyl-2-propen-1-yl]piperazine dihydrochloride
Piperazine, 1-[2-(diphenylmethoxy)ethyl]-4-[(2E)-3-phenyl-2-propen-1-yl]-, hydrochloride (1:2)

Biological Activity

[Description]:

GBR 12783 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 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

[ Density]:
1.085 g/cm3

[ Boiling Point ]:
550.5ºC at 760 mmHg

[ Molecular Formula ]:
C₂₈H₃₂N₂O

[ Molecular Weight ]:
485.488

[ Flash Point ]:
148.1ºC

[ Exact Mass ]:
484.204834

[ PSA ]:
15.71000

[ LogP ]:
6.60340

[ Index of Refraction ]:
1.601

[ Storage condition ]:
-20°C

Safety Information

[ HS Code ]:
2933599090

Customs

[ HS Code ]: 2933599090

[ Summary ]:
2933599090. other compounds containing a pyrimidine ring (whether or not hydrogenated) or piperazine ring in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%