Cevimeline |
Catalog No.GC14215
One-Click Copy Product Info
|
Un agonista del receptor muscarínico.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 107233-08-9
Sample solution is provided at 25 µL, 10mM.
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Cevimeline is a potent direct-acting muscarinic receptor agonist with oral bioavailability [1]. Cevimeline can bind and activate M1 and M3 muscarinic receptors, and can cross the blood-brain barrier (BBB) to positively influence tau pathology and reduce the levels of amyloid-β (Aβ) peptide [2]. Cevimeline has been widely used to enhance the function of salivary glands and to increase the excitability of neurons in animal models[3].
In vitro, Cevimeline (10µM) treatment for 2 minutes significantly increased the calcium ion concentration within the rat parotid gland cells[4].
In vivo, Cevimeline treatment via oral administration at a dose of 10mg/kg/day for 7 days restored the level of AQP5 protein in the submandibular gland of rats, which had been decreased by parasympathectomy [5]. Oral administration of Cevimeline three times a day at a dose of 9mg/kg for 2 weeks reversed olanzapine-induced body weight gain and decreased feeding efficiency in female rats[6]. A single intraperitoneal injection of 10mg/kg dose of Cevimeline for 20 minutes significantly induced salivary secretion in diabetic mice and increased amylase activity[7].
References:
[1] Ono M, Takamura E, Shinozaki K, et al. Therapeutic effect of cevimeline on dry eye in patients with Sjögren's syndrome: a randomized, double-blind clinical study[J]. American journal of ophthalmology, 2004, 138(1): 6-17.
[2] Oleksak P, Novotny M, Patocka J, et al. Neuropharmacology of cevimeline and muscarinic drugs—focus on cognition and neurodegeneration[J]. International Journal of Molecular Sciences, 2021, 22(16): 8908.
[3] Ueda H, Mitoh Y, Ichikawa H, et al. Cevimeline enhances the excitability of rat superior salivatory neurons[J]. The Journal of Medical Investigation, 2009, 56(Supplement): 267-269.
[4] Ono K, Inagaki T, Iida T, et al. Distinct effects of cevimeline and pilocarpine on salivary mechanisms, cardiovascular response and thirst sensation in rats[J]. Archives of oral biology, 2012, 57(4): 421-428.
[5] Li X, Azlina A, Karabasil M R, et al. Degradation of submandibular gland AQP5 by parasympathetic denervation of chorda tympani and its recovery by cevimeline, an M3 muscarinic receptor agonist[J]. American Journal of Physiology-Gastrointestinal and Liver Physiology, 2008, 295(1): G112-G123.
[6] Lian J, Deng C. The dosage-dependent effects of cevimeline in preventing olanzapine-induced metabolic side-effects in female rats[J]. Pharmacology Biochemistry and Behavior, 2020, 191: 172878.
[7] ISHII H, NAKAGAWA Y, SHIGA T, et al. Effects of Cevimeline hydrochloride on salivary secretion in streptozotocin-induced diabetic Balb/cA mice[J]. ORAL THERAPEUTICS AND PHARMACOLOGY, 2001, 20(2): 86-91.
| Cell experiment [1]: | |
Cell lines | Rat parotid gland cells |
Preparation Method | Rat parotid gland cells were immediately removed from deep anaesthesia of rats and placed in cold balanced salt solution (BSS) containing: 120mM NaCl, 5mM KCl, 1mM Na2HPO4, 2mM CaCl2, 1mM MgCl2, 10mM glucose, 20mM HEPES (adjusted to pH 7.4 by NaOH), and 0.5% bovine serum albumin. After mincing, the material was then digested for 30min at 37 °C with 50U/ml collagenase in BSS, and the suspension was gently passed through a pipette 10 times every 10min. After filtering through a 150μm nylon mesh, the cell preparations were loaded with 2μM fura-2AM, which was suspended in 10ml of BSS, and incubated for 30min at room temperature. After dispersing the cell preparation on poly-d-lysine-coated glass-bottom dishes, the dishes were mounted on the stage of an inverted fluorescence microscope and perfused with BSS at a rate of 1ml/min at 36 °C. The excitation of fura-2 was induced every second by an alternate illumination of 340 and 380nm light, and the resultant fluorescence (510-550nm) was collected using an objective lens and a silicon-intensified target camera. Different concentrations of Cevimeline (0, 1, 10, and 100µM) were applied to cells by superfusion. Record the calcium ion concentration data every two minutes. |
Reaction Conditions | 0, 1, 10, and 100µM; 2min |
Applications | Cevimeline treatment dose-dependently increased the calcium ion concentration within the rat parotid gland cells. |
| Animal experiment [2]: | |
Animal models | Male Sprague-Dawley rats |
Preparation Method | Male Sprague-Dawley rats (7 weeks old), weighing 170-190g, were kept in temperature-controlled (21°C-25°C) and humidity-maintained (40%-70%) rooms with a 12-h light/dark cycle. Water and food were provided freely. Cervical sympathetic trunk denervation (CSTD) or chorda tympani denervation (CTD) were performed under anesthesia with pentobarbital sodium (50mg/kg). Cevimeline (10mg/kg; p.o.), pilocarpine (0.3mg/kg; p.o.), or chloroquine diphosphate (50mg/kg; p.o.) was administered every day for 7 days starting from the 15th day after the operation. On the 21st day after the operation, the rats were killed and the submandibular glands were immediately dissected to determine AQP protein and mRNA levels. |
Dosage form | 10mg/kg/day for 7 days; p.o. |
Applications | Cevimeline treatment enhanced the levels of AQP5 protein and mRNA in the submandibular glands of rats after parasympathectomy. |
References: | |
| Cas No. | 107233-08-9 | SDF | |
| Chemical Name | (2R,5R)-2-methylspiro[1,3-oxathiolane-5,3'-1-azabicyclo[2.2.2]octane] | ||
| Canonical SMILES | CC1OC2(CN3CCC2CC3)CS1 | ||
| Formula | C10H17NOS | M.Wt | 199.32 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 5.0171 mL | 25.0853 mL | 50.1706 mL |
| 5 mM | 1.0034 mL | 5.0171 mL | 10.0341 mL |
| 10 mM | 501.7 μL | 2.5085 mL | 5.0171 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)