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AM4113

Cat. No. M8674
AM4113 Structure
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Biological Activity

AM4113 is a Cannabinoid CB-1 neutral antagonist. AM4113 reduced reward and reinstatement of drug-seeking behavior, reducing cue-induced reinstatement in monkeys trained to self-administer cocaine.

Chemical Information
Molecular Weight 380.66
Formula C17H12Cl3N3O
CAS Number 614726-85-1
Solubility (25°C) DMSO: 2 mg/mL (warmed)
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] Miguel Lujn, et al. CB1 receptor antagonist AM4113 reverts the effects of cannabidiol on cue and stress-induced reinstatement of cocaine-seeking behaviour in mice

[2] Basma G Eid, et al. Interference with TGFβ1-Mediated Inflammation and Fibrosis Underlies Reno-Protective Effects of the CB1 Receptor Neutral Antagonists AM6545 and AM4113 in a Rat Model of Metabolic Syndrome

[3] Basma G Eid, et al. Effects of the CB1 Receptor Antagonists AM6545 and AM4113 on Insulin Resistance in a High-Fructose High-Salt Rat Model of Metabolic Syndrome

[4] Xiang-Hu He, et al. Cannabinoid CB 1 receptor neutral antagonist AM4113 inhibits heroin self-administration without depressive side effects in rats

[5] T U C Jrbe, et al. Intrinsic effects of AM4113, a putative neutral CB1 receptor selective antagonist, on open-field behaviors in rats

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