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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
规格:98%
分子量:253.79
包装与价格:
包装价格(元)
10mg电议
25mg电议
50mg电议
1g电议

产品介绍
Agonist of muscarinic receptor (M1/M3)
CAS:153504-70-2
分子式:C10H20ClNO2S
分子量:253.79
纯度:98%
存储:Store at -20°C

Background:

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].


参考文献:
[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.