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ASP8062

Cat. No. M40713
ASP8062 Structure
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Biological Activity

ASP8062 is an orally active GABAB receptor-positive altered modulator (PAM) that can be used in studies related to opioid-related disorder (OUD).

Chemical Information
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] Shinobu Akuzawa et al. J Pharmacol Sci. Effect of ASP8062 on morphine self-administration and morphine-induced respiratory suppression in monkeys

[2] Elizabeth M Burnette et al. Drugs. Novel Agents for the Pharmacological Treatment of Alcohol Use Disorder

[3] Mototsugu Ito et al. J Psychopharmacol. A phase 1 study to assess potential interaction between ASP8062 and alcohol in healthy adult subjects

[4] Colin N Haile et al. Psychopharmacology (Berl). The GABAB receptor positive allosteric modulator ASP8062 reduces operant alcohol self-administration in male and female Sprague Dawley rats

[5] Mark Walzer et al. Psychopharmacology (Berl). A randomized phase 1 single-dose polysomnography study of ASP8062, a GABAB receptor positive allosteric modulator

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