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SKF83959

Cat. No. M10768
SKF83959 Structure
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Biological Activity

SKF83959 is a potent selective dopamine D1-like Receptor partial agonist. SKF83959 Ki to rats D1,D5,D2AND D3 The values are 1.18, 7.56, 920, and 399 nM, respectively. SKF83959 is a potent sigma (σ)-1 receptor allosteric modulator. SKF83959 belongs to the benzazepine family and has an improving effect on cognitive dysfunction. SKF83959 can be used to study Alzheimer's disease and depression.

Chemical Information
Molecular Weight 398.72
Formula C18Cl1H20N1O2
CAS Number 67287-95-0
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Pei-Pei Liu, et al. Int J Neuropsychopharmacol. Task-Dependent Effects of SKF83959 on Operant Behaviors Associated With Distinct Changes of CaMKII Signaling in Striatal Subareas

[2] Pei-Pei Liu, et al. Chin J Physiol. Lack of effect of dopamine receptor blockade on SKF83959-altered operant behavior in male rats

[3] Fu-Feng Chen, et al. Brain Res. SKF83959, an agonist of phosphatidylinositol-linked dopamine receptors, prevents renewal of extinguished conditioned fear and facilitates extinction

[4] Gaofeng Sheng, et al. Biol Pharm Bull. SKF83959 Has Protective Effects in the Scopolamine Model of Dementia

[5] Bo Jiang, et al. Int J Neuropsychopharmacol. SKF83959 produces antidepressant effects in a chronic social defeat stress model of depression through BDNF-TrkB pathway

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