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Cevimeline

Cat. No. M20957
Cevimeline Structure
Synonym:

AF 102B; SNI 2011; SNK 508

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Biological Activity

Cevimeline (AF 102B, SNI 2011, SNK 508) is a parasympathomimetic agent that act as an agonist at the muscarinic acetylcholine receptors M1 and M3.

Chemical Information
Molecular Weight 244.78
Formula C10H18ClNOS.1/2H2O
CAS Number 153504-70-2
Solubility (25°C) DMSO 40 mg/mL
Water 40 mg/mL
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] Mei Han, et al. J Psychopharmacol. Cevimeline co-treatment attenuates olanzapine-induced metabolic disorders via modulating hepatic M3 muscarinic receptor: AMPKα signalling pathway in female rats

[2] Patrik Oleksak, et al. Int J Mol Sci. Neuropharmacology of Cevimeline and Muscarinic Drugs-Focus on Cognition and Neurodegeneration

[3] No authors listed. Cevimeline

[4] Marta Tanasiewicz, et al. Adv Clin Exp Med. Xerostomia of Various Etiologies: A Review of the Literature

[5] Juliane Weber, et al. Drugs. Cevimeline

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Keywords: Cevimeline, AF 102B; SNI 2011; SNK 508 supplier, AChR/AChE, inhibitors, activators


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