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SKF 83822 hydrobromide

Names

[ CAS No. ]:
74115-10-9

[ Name ]:
SKF 83822 hydrobromide

Biological Activity

[Description]:

SKF83822 hydrobromide is a potent dopamine D1 receptor agonist. SKF83822 hydrobromide activates Gs/olf/adenylyl cyclase (AC)-coupled D1 receptors, but not phospholipase C (PLC)-coupled D1-like receptors[1].

[Related Catalog]:

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

[Target]

D1 Receptor


[In Vitro]

SKF83822 (1 μM) increases DARPP-32 phosphorylation in Neostriatal slices. Treatment with SKF83822 for 5 min stimulates DARPP-32 Thr34 phosphorylation maximally at a concentration of 100 μM with a half maximal effect at ∼1 μM. SKF83822 (1 μM) does not affect the phosphorylation of DARPP-32 at Thr75, Ser97 or Ser130[1]. Western Blot Analysis[1] Cell Line: Neostriatal slices Concentration: 1 μM Incubation Time: 0, 0.5, 2, 5, and 10 minutes Result: Treatment with 1 μM increased the level of phospho-Thr34 DARPP-32, maximally by ∼6-fold within 2 min of incubation.

[In Vivo]

SKF83822 activates dopamine D1 receptors coupled to Gαs/olf and downstream cyclase activity. SKF83822 produces a locomotor response in both rodent and non-human primate models without affecting stereotypy, intense grooming, or dyskinesia. An acute injection of SKF83822 (0.4 mg/kg; i.p.) induced a greater than threefold increase in locomotor activity relative to the baseline period for each genotype[1]. Animal Model: Gαq knockout mice[1] Dosage: 0.4 mg/kg Administration: Result: There was a significant increase in locomotor activity in each genotype.

[References]

[1]. Mahomi Kuroiwa, et al. Regulation of DARPP-32 phosphorylation by three distinct dopamine D1-like receptor signaling pathways in the neostriatum. J Neurochem. 2008 Nov;107(4):1014-26.

[2]. Aliya L Frederick, et al. Neurobehavioral phenotyping of G(αq) knockout mice reveals impairments in motor functions and spatial working memory without changes in anxiety or behavioral despair. Front Behav Neurosci. 2012 Jun 19;6:29.

Chemical & Physical Properties

[ Molecular Formula ]:
C20H23BrClNO2

[ Molecular Weight ]:
424.76

[ Exact Mass ]:
423.06000

[ PSA ]:
43.70000

[ LogP ]:
5.13160

Safety Information

[ Symbol ]:

GHS06, GHS09

[ Signal Word ]:
Danger

[ Hazard Statements ]:
H301-H400

[ Precautionary Statements ]:
P273-P301 + P310

[ RIDADR ]:
UN2811 - class 6.1 - PG 3 - EHS - Toxic solids, organic, n.o.s., HI: all

Related Compounds