DC Chemicals Limited
China
Product Name: SKF-83959 HBr
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Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

67287-95-0

67287-95-0 structure

Name: SKF 83959 hydrobromide
Chemical Name: 6-Chloro-3-methyl-1-(3-methylphenyl)-2,3,4,5-tetrahydro-1H-3-benz azepine-7,8-diol hydrobromide (1:1)
CAS Number: 67287-95-0
Molecular Formula: C₁₈H₂₁BrClNO₂
Molecular Weight: 398.72200
Catalog: Signaling Pathways GPCR/G Protein Dopamine Receptor
Create Date: 2016-05-08 20:21:32
Modify Date: 2024-01-08 23:38:07
SKF83959 hydrobromide is a potent and selective dopamine D1-like receptor partial agonist. SKF83959 hydrobromide Ki values for rat D1, D5, D2 and D3 receptors are 1.18, 7.56, 920 and 399 nM, respectively. SKF83959 hydrobromide is a potent allosteric modulator of sigma (σ)-1 receptor. SKF83959 hydrobromide belongs to benzazepine family and has improvements on cognitive dysfunction. SKF83959 hydrobromide can be used for the research of Alzheimer's disease and depression[1][2][3][4].

Name	6-Chloro-3-methyl-1-(3-methylphenyl)-2,3,4,5-tetrahydro-1H-3-benz azepine-7,8-diol hydrobromide (1:1)
Synonyms	6-chloro-9H-purine-2-sulfonyl fluoride 2-fluorosulfonyl-6-chloropurine 6-chloranyl-7H-purine-2-sulfonyl fluoride 6-Chlor-purin-2-sulfonylfluorid 6-Chloro-1H-Purine-2-sulfonyl fluoride

Description	SKF83959 hydrobromide is a potent and selective dopamine D1-like receptor partial agonist. SKF83959 hydrobromide Ki values for rat D1, D5, D2 and D3 receptors are 1.18, 7.56, 920 and 399 nM, respectively. SKF83959 hydrobromide is a potent allosteric modulator of sigma (σ)-1 receptor. SKF83959 hydrobromide belongs to benzazepine family and has improvements on cognitive dysfunction. SKF83959 hydrobromide 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 hydrobromide (10~250 μM) stimulates PIP2 hydrolysis in membranes. SKF83959 hydrobromide (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 hydrobromide (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 hydrobromide (1 mg/kg; i.p.; 30 minutes) induced memory enhancing effects are prevented by brain-derived neurotrophic factor system blockade[1]. SKF83959 hydrobromide 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.