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Proteins and Peptides

(+)-Cevimeline (hydrochloride hemihydrate)

Product Sizes
1 mg
£ POA
HY-76772A-1MG
5 mg
£ POA
HY-76772A-5MG
10mM/1mL
£ POA
HY-76772A-10MM
About this Product
SKU:
HY-76772A
Additional Names:
(+)-SNI-2011; (+)-AF102B (hydrochloride hemihydrate)
Extra Details:
(+)-Cevimeline hydrochloride hemihydrate ((+)-SNI-2011); a potent muscarinic receptor agonist; is a candidate therapeutic drug for xerostomia in Sjogren's syndrome. IC50 value: Target: mAChR The general pharmacol. properties of this drug on the gastrointestinal; urinary; and reproductive systems and other tissues were investigated in mice; rats; guinea pigs; rabbits; and dogs. The in vitro metab. of SNI-2011 was also evaluated with rat and dog liver microsomes. After oral administration; plasma concns. of SNI-2011 reached to Cmax within 1 h in both species; suggesting that SNI-2011 was quickly absorbed; and then decreased with a t1/2 of 0.4-1.1 h. The bioavailability was 50% and 30% in rats and dogs; resp. Major metabolites in plasma were both S- and N-oxidized metabolites in rats and only N-oxidized metabolite in dogs; indicating that a large species difference was obsd. in the metab. of SNI-2011. Sex difference was also obsd. in the pharmacokinetics of SNI-2011 in rats; but not in dogs. In the in vitro study; chem. inhibition and pH-dependent studies revealed that the sulfoxidn. and N-oxidn. of SNI-2011 were mediated by cytochrome P 450 (CYP) and flavin-contg. monooxygenase (FMO); resp.; in both species. In addn.; CYP2D and CYP3A were mainly responsible for the sulfoxidn. in rat liver microsomes.
Molecular Weight:
244.78
Purity:
99.03
Research Area:
Neurological Disease
Shipping Conditions:
Ambient
Storage Conditions:
4[o]C (Powder; sealed storage; away from moisture)
Type:
Proteins, Peptides, Small Molecules & Other Biomolecules: Small Molecules
Pathway:
GPCR/G Protein;Neuronal Signaling
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