SKF38393 hydrochloride is a selective agonist of the D1DR (dopamine D1 receptor). SKF-38393 HCl is an activator of D5DR. SKF38393 is a synthetic compound of the benzazepine chemical class which acts as a selective D1/D5 receptor partial agonist. SKF38393 HCl has stimulant and anorectic effects. SKF-38393 hydrochloride enhances the frequency of mEPSCs in a concentration-dependent manner.
|Cell lines||MCF-7, MDA-MB231 and MCF-10 cells|
|Preparation method||Examine the effects of a specific dopamine agonist, SKF 38393, against MCF-7 cells. MDA-MB231 and MCF-10 cells were used as negative controls. The breast cancer in vitro screening procedure involved the plating of MCF-7, MDA-MB231 and MCF-10 cells in a 96-well plate assay. After 1 day, the cells were exposed to SKF 38393 for 2 days and cell growth was determined by the Alamar blue dye reagent method. The optical density data was analyzed and IC50 values determined. The results indicated that SKF 38393 caused a significant decrease in proliferation of MCF-7 cells. The IC50 value was 0.1 +/- 0.03 mu M. The results also indicated no significant effect on MDA-MB231 and MCF-10 cells.|
|Incubation time||2 days|
|Animal models||Male Wistar rats|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|Solubility||DMSO: ≥ 30 mg/mL|
Role of the basolateral amygdala dopamine receptors in arachidonylcyclopropylamide-induced fear learning deficits.
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Performance- and task-dependent effects of the dopamine D1/D5 receptor agonist SKF 38393 on learning and memory in the rat.
Amico F, et al. Eur J Pharmacol. 2007 Dec 22;577(1-3):71-7. PMID: 17900561.
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Picomolar affinity of 125I-SCH 23982 for D1 receptors in brain demonstrated with digital subtraction autoradiography.
Altar CA, et al. J Neurosci. 1987 Jan;7(1):213-22. PMID: 2949066.
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