鹽酸西維美林半水合物作用機(jī)制 - Medchemexpress - MCE中國(guó)

1、Product Data SheetCevimeline hydrochloride hemihydrateCat. No.: HY-76772CAS No.: 153504-70-2分式: CHNOS.HCl./HO分量: 244.78作靶點(diǎn): mAChR作通路: GPCR/G Protein; Neuronal Signaling儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) H2O : 50 mg/mL (204.27 mM)* means soluble, but satur

2、ation unknown.SolventMass1 mg 5 mg 10 mgConcentration制備儲(chǔ)備液1 mM 4.0853 mL 20.4265 mL 40.8530 mL5 mM 0.8171 mL 4.0853 mL 8.1706 mL10 mM 0.4085 mL 2.0427 mL 4.0853 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?6 個(gè)內(nèi)使，-20C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?1 個(gè)內(nèi)使。BIOLOG

3、ICAL ACTIVITY物活性 Cevimeline hydrochloride hemihydrate (SNI-2011) 種酰膽堿的奎尼丁衍物，也 種選擇性的和服活性的 毒蕈堿型 M1 和 M3 受體激動(dòng)劑。Cevimeline hydrochloride hemihydrate 可刺激唾液腺分泌，并可作癥的種催涎劑。Cevimeline hydrochloride hemihydrate 可穿過腦屏障。IC & Target Muscarinic M1 and M3 receptor1體外研究 In digested parotid cells, Cevimeline (0.1-10

4、0 M) increases the intracellular Ca2+ concentration1.體內(nèi)研究Cevimeline (0.008-0.016 mg/kg; intraperitoneal injection; male Wistar rats) treatment shows slowly increasing andangiotensin II-induced water intake and neuronal activity in the subfornical organ at 0.016 mg/kg1.lasting salivation, and increas

5、ed blood flow increment in the parotid gland and pressor response. Cevimeline inhibitsPage 1 of 2 www.MedChemEAnimal Model: Male Wistar rats (8-week-old) injected with angiotensin-II1Dosage: 0.008 mg/kg, 0.016 mg/kgAdministration: Intraperitoneal injectionResult: Showed slowly increasing and lasting

6、 salivation, and increased blood flow incrementin the parotid gland and pressor response.REFERENCES1. Ono K, et al. Distinct effects of cevimeline and pilocarpine on salivary mechanisms, cardiovascular response and thirst sensation in rats.Arch Oral Biol.2012 Apr;57(4):421-8. Epub 2011 Nov 17.2. Wit

7、sell 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 9.3. Kondo Y, et al.Cevimeline-induced monophasic salivation from the mouse submandibular gland: decreased Na+ content

8、in saliva results from specificand early activation of Na+/H+ exchange.J Pharmacol Exp Ther. 2011 Apr;337(1):267-74. Epub 2011 Jan 14.4. Voskoboynik B, et al.Cevimeline (Evoxac) overdose.J Med Toxicol. 2011 Mar;7(1):57-9.5. Mitoh Y, et al. Effects of cevimeline on excitability of parasympathetic preganglionic neurons in the superior salivatory nucleus of rats. Auton Neurosci.2017 Sep;206:1-7.McePdfHeightCaution: Product has not been fully validated for medical applications. For research