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OSU6162 hydrochloride

Cat. No. M8064
OSU6162 hydrochloride Structure
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Biological Activity

OSU6162 (PNU-96391) is a dopamine stabilizer, a drug that can stimulate or inhibit dopaminergic signaling depending on the dopaminergic tone. Dopaminergic stabilizers have been proposed to act as partial dopamine receptor agonists or as antagonists with both dopamine and behavioral stabilizing activity. Although affinity is not high (in vitro binding affinity for dopamine D2 receptor has a Ki of 447 nM), OSU6162 shows a high level of receptor occupancy.

Chemical Information
Molecular Weight 317.87
Formula C15H23NO2S·HCl
CAS Number 156907-84-5
Solubility (25°C) Water: ≥16 mg/mL
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] Dominic Dougall, et al. Pharmacotherapy for chronic cognitive impairment in traumatic brain injury

[2] J Matthew Hutzler, et al. Effect of carbonate anion on cytochrome P450 2D6-mediated metabolism in vitro: the potential role of multiple oxygenating species

[3] Larry C Wienkers, et al. Multiple cytochrome P450 enzymes responsible for the oxidative metabolism of the substituted (S)-3-phenylpiperidine, (S,S)-3-[3-(methylsulfonyl)phenyl]-1-propylpiperidine hydrochloride, in human liver microsomes

[4] A Ekesbo, et al. Motor effects of (-)-OSU6162 in primates with unilateral 6-hydroxydopamine lesions

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