1. GPCR/G Protein
    Neuronal Signaling
  2. Dopamine Receptor
    Sigma Receptor
  3. SKF83959

SKF83959 

Cat. No.: HY-130344
Handling Instructions

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.

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

SKF83959 Chemical Structure

SKF83959 Chemical Structure

CAS No. : 80751-85-5

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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].

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 (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].

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

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].

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

317.81

Formula

C₁₈H₂₀ClNO₂

CAS No.
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SKF83959
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HY-130344
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