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SCH-23390 maleate

Cat. No. M30773
SCH-23390 maleate Structure
Synonym:

R-(+)-SCH-23390 maleate

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Quality Control & Documentation
Biological Activity

SCH-23390 maleate (R-(+)-SCH-23390 maleate) is a potent and selective dopamine D1-like receptor antagonist with Kis of 0.2 nM and 0.3 nM for the D1 and D5 receptor, respectively. SCH-23390 maleate is a potent and high efficacy human 5-HT2C receptor agonist with a Ki of 9.3 nM. SCH-23390 maleate also binds with high affinity to the 5-HT2 and 5-HT1C receptors. SCH-23390 maleate inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with an IC50 of 268 nM.

Chemical Information
Molecular Weight 403.86
Formula C21H22ClNO5
CAS Number 87134-87-0
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
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] Pelin Tanyeri, et al. Pharmacol Biochem Behav. Effects of ziprasidone, SCH23390 and SB277011 on spatial memory in the Morris water maze test in naive and MK-801 treated mice

[2] Florence C Heath, et al. Psychopharmacology (Berl). Dopamine D1-like receptor signalling in the hippocampus and amygdala modulates the acquisition of contextual fear conditioning

[3] K Kobayashi, et al. Neuropharmacology. An increase in the in vivo binding of [3H]SCH 23390 induced by MK-801 in the mouse striatum

[4] H Kuribara, et al. Jpn J Pharmacol. SCH 23390 equivalently, but YM-09151-2 differentially reduces the stimulant effects of methamphetamine, MK-801 and ketamine: assessment by discrete shuttle avoidance in mice

[5] J F Marshall, et al. J Neural Transm Gen Sect. Dopamine-glutamate interactions in methamphetamine-induced neurotoxicity

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