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NESS 0327 

Cat. No. M30173
NESS 0327  Structure
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Biological Activity

NESS 0327 is a cannabinoid antagonist with high selectivity for the cannabinoid CB1 receptor. NESS 0327 is more than 60,000-fold selective for the CB1 receptor.

Chemical Information
Molecular Weight 489.82
Formula C24H23Cl3N4O
CAS Number 494844-07-4
Form Solid
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] Sabrine Bilel, et al. Br J Pharmacol. Cognitive dysfunction and impaired neuroplasticity following repeated exposure to the synthetic cannabinoid JWH-018 in male mice

[2] Alba Navarro-Romero, et al. Neurobiol Dis. Cannabinoid type-1 receptor blockade restores neurological phenotypes in two models for Down syndrome

[3] Maria Paola Mascia, et al. Eur J Pharmacol. Differential modulation of GABA(A) receptor function by aryl pyrazoles

[4] Simone Tambaro, et al. Eur J Pharmacol. Modulation of ATP-mediated contractions of the rat vas deferens through presynaptic cannabinoid receptors

[5] Stefania Ruiu, et al. J Pharmacol Exp Ther. Synthesis and characterization of NESS 0327: a novel putative antagonist of the CB1 cannabinoid receptor

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Keywords: NESS 0327  supplier, Cannabinoid, inhibitors, activators


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