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COR659 

Cat. No. M30274
COR659  Structure
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Biological Activity

COR659 is a potent and effective GABAB positive allosteric modulator (PAM). COR659 suppresses alcohol and chocolate self-administration in rats.

Chemical Information
Molecular Weight 337.82
Formula C16H16ClNO3S
CAS Number 544450-68-2
Form Solid
Solubility (25°C) DMSO 25 mg/mL (ultrasonic)
Storage 4°C, protect from light, dry, sealed
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] Irene Lorrai, et al. Am J Drug Alcohol Abuse. Development of tolerance upon repeated administration with the GABAB receptor positive allosteric modulator, COR659, on alcohol drinking in rodents

[2] Irene Lorrai, et al. Psychopharmacology (Berl). Reducing effect of the novel positive allosteric modulator of the GABAB receptor, COR659, on binge-like alcohol drinking in male mice and rats

[3] Carla Lobina, et al. Behav Brain Res. Suppressing effect of the novel positive allosteric modulator of the GABAB receptor, COR659, on locomotor hyperactivity induced by different drugs of abuse

[4] Paola Maccioni, et al. Alcohol. Anti-addictive properties of COR659 - Additional pharmacological evidence and comparison with a series of novel analogues

[5] Paola Maccioni, et al. Psychopharmacology (Berl). Suppressing effect of COR659 on alcohol, sucrose, and chocolate self-administration in rats: involvement of the GABAB and cannabinoid CB1 receptors

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