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Cevimeline hydrochloride hemihydrate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Cevimeline hydrochloride hemihydrate图片
CAS NO:153504-70-2
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Cevimeline hydrochloride hemihydrate (SNI-2011) 是乙酰胆碱的奎宁环衍生物,是一种选择性和口服活性的毒蕈碱 M1 和 M3 受体激动剂。
Cas No.153504-70-2
别名盐酸西维美林半水合物; SNI-2011; AF102B hydrochloride hemihydrate
化学名(2R,5R)-2-methylspiro[1,3-oxathiolane-5,3'-1-azabicyclo[2.2.2]octane];hydrate;dihydrochloride
Canonical SMILESCC1OC2(CN3CCC2CC3)CS1.O.Cl
分子式C10H20ClNO2S
分子量253.79
溶解度Soluble in DMSO
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Cevimeline hydrochloride hemihydrate is a novel and selective agonist of muscarinic acetylcholine receptor [1].

Muscarinic acetylcholine receptors (mAChRs) are acetylcholine receptors and mediate serous-saliva secretion and tear secretion. It is more sensitive to muscarine than nicotine [1].

Cevimeline hydrochloride hemihydrate induced contractions of isolated guinea pig ilea and trachea with EC50 values of 3.5 and 3 μM, respectively. Binding studies indicated that Cevimeline hydrochloride hemihydrate was a potent and highly selective M1-type muscarinic agonist. Also, it had a higher affinity for M1 receptors than other M1 agonists [2].

In normal rats and mice, X-irradiated saliva secretion defective rats and two strains of autoimmune disease mice, intraduodenal administrations of SNI-2011 (3-30 mg/kg) increased saliva and tear secretions in a dose-dependent way, which suggested that Cevimeline hydrochloride hemihydrate directly stimulated muscarinic receptors in salivary and lacrimal glands for saliva and tear secretions [1].

References:
[1].  Iga Y, Arisawa H, Ogane N, et al. (+/-)-cis-2-methylspiro[1,3-oxathiolane-5,3'-quinuclidine] hydrochloride, hemihydrate (SNI-2011, cevimeline hydrochloride) induces saliva and tear secretions in rats and mice: the role of muscarinic acetylcholine receptors. Jpn J Pharmacol, 1998, 78(3): 373-380.
[2].  Fisher A, Brandeis R, Karton I, et al. (+-)-cis-2-methyl-spiro(1,3-oxathiolane-5,3') quinuclidine, an M1 selective cholinergic agonist, attenuates cognitive dysfunctions in an animal model of Alzheimer's disease. J Pharmacol Exp Ther, 1991, 257(1): 392-403.

 
 
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