SKF 83959 HYDROBROMIDE

Names

[ Name ]:
SKF 83959 HYDROBROMIDE

[Synonym ]:
6-Chloro-2,3,4,5-tetrahydro-3-methyl-1-(3-methylphenyl)-1H-3-benzazepine-7,8-diol

Biological Activity

[Description]:

SKF83959 is a potent and selective dopamine D1-like receptor partial agonist. SKF83959 Ki values for rat D1, D5, D2 and D3 receptors are 1.18, 7.56, 920 and 399 nM, respectively. SKF83959 is a potent allosteric modulator of sigma (σ)-1 receptor. SKF83959 belongs to benzazepine family and has improvements on cognitive dysfunction. SKF83959 can be used for the research of Alzheimer's disease and depression[1][2][3][4].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Dopamine Receptor

Signaling Pathways >> Neuronal Signaling >> Dopamine Receptor

Research Areas >> Neurological Disease

Signaling Pathways >> GPCR/G Protein >> Sigma Receptor

[Target]

D1 Receptor:1.18 nM (Ki)

D5 Receptor:7.56 nM (Ki)

D2 Receptor:920 nM (Ki)

D3 Receptor:399 nM (Ki)

Sigma (σ)-1

[In Vitro]

SKF83959 (10~250 μM) stimulates PIP2 hydrolysis in membranes. SKF83959 (0.1~10 μM; PC12 cell) changes the EC50 value of SKF81297 from 0.5 nM in control tissue to 31.6 nM, 251.2 nM and 631.0 nM[2].

[In Vivo]

SKF83959 (0.5 and 1 mg/kg; i.p.; 1 hour) reverses the scopolamine-induced cognitive impairments in the passive avoidance task and Y-Maze test[1]. SKF83959 (1 mg/kg; i.p.; 30 minutes) induced memory enhancing effects are prevented by brain-derived neurotrophic factor system blockade[1]. SKF83959 has anti-amnesic activities and restores the scopolamine-decreased BDNF signaling pathway in the hippocampus in mice[1]. Animal Model: Male ICR male mice (8 weeks)[1] Dosage: 0.5 and 1 mg/kg Administration: I.p.; 1 hour Result: Reversed the scopolamine-induced cognitive impairments in the passive avoidance task and Y-Maze test. Animal Model: Male ICR male mice (8 weeks)[1] Dosage: 1 mg/kg Administration: I.p.; 30 minutes Result: The memory enhancing effects were prevented by BDNF system blockade.

[References]

[1]. Sheng G, et al. SKF83959 Has Protective Effects in the Scopolamine Model of Dementia. Biol Pharm Bull. 2018;41(3):427-434.

[2]. Jin LQ, et al. SKF83959 selectively regulates phosphatidylinositol-linked D1 dopamine receptors in rat brain. J Neurochem. 2003;85(2):378-386.

[3]. Neumeyer JL, et al. Receptor affinities of dopamine D1 receptor-selective novel phenylbenzazepines. Eur J Pharmacol. 2003;474(2-3):137-140.

[4]. Guo L, et al. SKF83959 is a potent allosteric modulator of sigma-1 receptor. Mol Pharmacol. 2013;83(3):577-586.

Chemical & Physical Properties

[ Density]:
1.249g/cm3

[ Boiling Point ]:
464.6ºC at 760 mmHg

[ Molecular Formula ]:
C₁₈H₂₁BrClNO₂

[ Molecular Weight ]:
398.72200

[ Flash Point ]:
234.8ºC

[ Exact Mass ]:
397.04400

[ PSA ]:
43.70000

[ LogP ]:
4.57540

[ Index of Refraction ]:
1.619

MSDS

Click to get detail MSDS

Safety Information

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ RIDADR ]:
NONH for all modes of transport

Articles

SKF83959 is a potent allosteric modulator of sigma-1 receptor.

Mol. Pharmacol. 83(3) , 577-86, (2013)

SKF83959 (3-methyl-6-chloro-7,8-hydroxy-1-[3-methylphenyl]-2,3,4,5-tetrahydro-1H-3-benzazepine), an atypical dopamine receptor-1 (D(1) receptor) agonist, has shown many D(1) receptor-independent effec...

The D₁ dopamine receptor agonist, SKF83959, attenuates hydrogen peroxide-induced injury in RGC-5 cells involving the extracellular signal-regulated kinase/p38 pathways.

Mol. Vis. 18 , 2882-95, (2012)

Oxidative stress is widely implicated in the death of retinal ganglion cells associated with various optic neuropathies. Agonists of the dopamine D(1) receptor have recently been found to be potential...

Phosphatidylinositol-linked novel D(1) dopamine receptor facilitates long-term depression in rat hippocampal CA1 synapses.

Neuropharmacology 57(2) , 164-71, (2009)

Recent work has demonstrated that a phosphatidylinositol (PI)-linked D(1) dopamine receptor selective agonist, SKF83959, mediates phosphatidylinositol hydrolysis via activation of phospholipase C(beta...

Related Compounds

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