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NS 9283 

Cat. No. M30881
NS 9283  Structure
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Biological Activity

NS9283 is a positive positive allosteric modulator of (α4)3(β2)2 nicotinic ACh receptors. NS9283 can be used in a series of neurological conditions such as attention deficit hyperactivity disorder (ADHD), schizophrenia, Parkinson's disease and Alzheimer's disease.

Chemical Information
Molecular Weight 248.24
Formula C14H8N4O
CAS Number 913830-15-6
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
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] Jingyi Wang, et al. Neuropsychopharmacology. Promoting activity of (α4)3(β2)2 nicotinic cholinergic receptors reduces ethanol consumption

[2] Simone Mazzaferro, et al. Cell Mol Life Sci. Potentiation of a neuronal nicotinic receptor via pseudo-agonist site

[3] Boris Lamotte d'Incamps, et al. J Neurosci. Stoichiometry of the Heteromeric Nicotinic Receptors of the Renshaw Cell

[4] Simone Mazzaferro, et al. J Biol Chem. α4β2 Nicotinic Acetylcholine Receptors: RELATIONSHIPS BETWEEN SUBUNIT STOICHIOMETRY AND FUNCTION AT THE SINGLE CHANNEL LEVEL

[5] Chang Z Zhu, et al. Biochem Pharmacol. Potentiation of analgesic efficacy but not side effects: co-administration of an α4β2 neuronal nicotinic acetylcholine receptor agonist and its positive allosteric modulator in experimental models of pain in rats

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Keywords: NS 9283  supplier, AChR/AChE, inhibitors, activators


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