Cevimeline hydrochloride|107220-28-0|(盐酸西维美林; AF102B hydrochloride)-陌孚医药/Medlife

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Cevimeline hydrochloride (Synonyms: 盐酸西维美林; AF102B hydrochloride)

目录号: PL06853

CAS No. :107220-28-0

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中文名称	Cevimeline hydrochloride
中文别名	十七烷基 2-乙酰氨基-3,4,6-三-O-乙酰-2-脱氧-βD-吡喃葡糖苷;西维美林盐酸;盐酸西维美林;西维美林-D4盐酸盐盐;((+/-)-顺式-2-甲基螺[1,3-氧硫杂环戊烷-5,3'-奎宁环]盐酸半水合物
英文名称	Cevimeline hydrochloride
英文别名	Spiro[1-azabicyclo[2.2.2]octane-3,5'-[1,3]oxathiolane],2'-methyl-, hydrochloride (1:1), (2'R,3R)-rel-;Cevimeline Hydrochloride Salt;2-methylspiro[1,3-oxathiolane-5,3'-1-azabicyclo[2.2.2]octane],hydrochloride;CEVIMELINE;Cevimeline hydrochloride;Spiro[1-azabicyclo[2.2.2]octane-3,5'-[1,3]oxathiolane],2'-methyl-, hydrochloride (1:1), (2'R,3...;AF-102B hydrochloride;SNI-2011 hydrochloride;Saligren;cis-2-Methylspiro[1,3-oxathiolane-5,3'-quinuclidine] hydrochloride;AF 102B;Evoxac;FKS 508;SND 5008;SNI 2011;SNK 508;(2'R,3R)-rel-2'-Methyl- spiro[1-azabicyclo[2.2.2]octane-3,5'-[1,3]oxathiolane] hydrochloride;CeviMelin;CeviMeline hydrochloride Saligren
Cas No.	107220-28-0
分子式	C₁₀H₁₇NOs^.HCl
分子量	235.77
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情

Cevimeline hydrochloride (AF102B hydrochloride) 是一种乙酰胆碱的奎尼丁衍生物，也是一种选择性的和口服活性的毒蕈碱型 M1 和 M3 受体激动剂。Cevimeline hydrochloride 可刺激唾液腺分泌，并可用作口干症的一种催涎剂。Cevimeline hydrochloride 可穿过血脑屏障。

生物活性

Cevimeline hydrochloride (AF102B hydrochloride) is a quinuclidine derivative of acetylcholine and a selective and orally active muscarinic M1 and M3 receptor agonist. Cevimeline hydrochloride stimulates secretion by the salivary glands and can be used as a sialogogue for xerostomia. Cevimeline hydrochloride can cross the blood-brain barrier (BBB).

性状

Solid

IC50 & Target[1][2]

Muscarinic M1 and M3 receptor

体外研究(In Vitro)

In digested parotid cells, Cevimeline (0.1-100 μM) increases the intracellular Ca concentration. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Cevimeline (0.008-0.016 mg/kg; intraperitoneal injection; male Wistar rats) treatment shows slowly increasing and lasting salivation, and increased blood flow increment in the parotid gland and pressor response. Cevimeline inhibits angiotensin II-induced water intake and neuronal activity in the subfornical organ at 0.016 mg/kg. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ClinicalTrial

参考文献

[1]. Witsell DL, et al. Effectiveness of cevimeline to improve oral health in patients with postradiation xerostomia.Head Neck. 2012 Aug;34(8):1136-42. doi: 10.1002/hed.21894. Epub 2012 Jan 9.
[2]. Kondo Y, et al.Cevimeline-induced monophasic salivation from the mouse submandibular gland: decreased Na+ content in saliva results from specific and early activation of Na+/H+ exchange.J Pharmacol Exp Ther. 2011 Apr;337(1):267-74. Epub 2011 Jan 14.

溶解度数据	In Vitro: H₂O : ≥ 50 mg/mL (212.07 mM)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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