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Cevimeline hydrochloride

Cat. No. M22086
Cevimeline hydrochloride Structure
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Quality Control & Documentation
Biological Activity

Cevimeline hydrochloride is a quinidine derivative of acetylcholine and a selective, orally active agonist of muscarinic acetylcholine receptors M1 and M3, with a spirocyclic moiety in its structure, which crosses the blood-brain barrier.

Chemical Information
Molecular Weight 235.77
Formula C10H18ClNOS
CAS Number 107220-28-0
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] Manuel Ramos-Casals, et al. Ann Rheum Dis. EULAR recommendations for the management of Sjögren's syndrome with topical and systemic therapies

[2] No authors listed. Cevimeline

[3] Ramya S. Pakala, et al. Cholinergic Medications

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

[5] Akira Shiozawa. Nihon Yakurigaku Zasshi. [Cevimeline hydrochloride hydrate (Saligren capsule 30 mg): a review of its pharmacological profiles and clinical potential in xerostomia]

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