1. GPCR/G Protein
    Neuronal Signaling
  2. Dopamine Receptor
    Sigma Receptor
  3. SKF 83959 hydrobromide

SKF 83959 hydrobromide 

Cat. No.: HY-103412 Purity: 99.86%
Handling Instructions

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.

For research use only. We do not sell to patients.

SKF 83959 hydrobromide Chemical Structure

SKF 83959 hydrobromide Chemical Structure

CAS No. : 67287-95-0

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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].

IC50 & Target[3][4]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

398.72

Formula

C₁₈H₂₁BrClNO₂

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 20 mg/mL (50.16 mM; Need ultrasonic and warming)

DMF : 20 mg/mL (50.16 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5080 mL 12.5401 mL 25.0803 mL
5 mM 0.5016 mL 2.5080 mL 5.0161 mL
10 mM 0.2508 mL 1.2540 mL 2.5080 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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SKF 83959 hydrobromide
Cat. No.:
HY-103412
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