GLPBio

Cevimeline (hydrochloride)

Catalog No.: GC43232Purity:>98.00%Synonyms: AF 102B, SNI 2011, SNK 508
COASDSData Sheet
Cevimelin (Hydrochlorid) (AF102B-Hydrochlorid) ist ein Chinuclidin-Derivat von Acetylcholin und ein selektiver und oral wirksamer muskarinischer M1- und M3-Rezeptoragonist.

Die Produkte sind ausschließlich für Forschungszwecke bestimmt. Nicht zur Anwendung am Menschen. Wir verkaufen nicht an Patienten.

Cevimeline (hydrochloride)
Cas No.: 107220-28-0
1mgIn Stock
$30.00
1
5mgIn Stock
$94.00
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10mgIn Stock
$137.00
1
50mgIn Stock
$539.00
1
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    632, 686–694 (2024)
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    618, 1017–1023 (2023)
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    610, 366–372 (2022)
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    Cell
    187(9):2288-2304 (2024)
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    Cell
    183(7):1867-1883 (2020)
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    31, 1291–1307 (2021)

Beschreibung (Description)

Cevimeline (hydrochloride) is a potent direct-acting muscarinic receptor agonist with oral bioavailability [1]. Cevimeline (hydrochloride) 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 (hydrochloride) 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 (hydrochloride) (10µM) treatment for 2 minutes significantly increased the calcium ion concentration within the rat parotid gland cells[4].

In vivo, Cevimeline (hydrochloride) 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 (hydrochloride) 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 (hydrochloride) 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 (hydrochloride) 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 (hydrochloride) 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 (hydrochloride) 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 (hydrochloride) 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 (hydrochloride), 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 (hydrochloride) 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) hydrochloride on salivary secretion in streptozotocin-induced diabetic Balb/cA mice[J]. ORAL THERAPEUTICS AND PHARMACOLOGY, 2001, 20(2): 86-91.

Protokoll (Protocol)

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 (hydrochloride) (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 (hydrochloride) 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 (hydrochloride) (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 (hydrochloride) treatment enhanced the levels of AQP5 protein and mRNA in the submandibular glands of rats after parasympathectomy.

References:
[1] Ono K, Inagaki T, Iida T, et al. Distinct effects of Cevimeline (hydrochloride) and pilocarpine on salivary mechanisms, cardiovascular response and thirst sensation in rats[J]. Archives of oral biology, 2012, 57(4): 421-428.
[2] 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 (hydrochloride), an M3 muscarinic receptor agonist[J]. American Journal of Physiology-Gastrointestinal and Liver Physiology, 2008, 295(1): G112-G123.

Produktdokumente (Product Documents)

Purity:>98.00%Appearance:A solid
COASDSData Sheet

Chemische Eigenschaften (Chemical Properties)

CAS-Nr.
107220-28-0
Synonyme
AF 102B, SNI 2011, SNK 508
SMILES
C[C@@H](SC1)O[C@@]21CN3CCC2CC3.Cl
Summenformel
C10H17NOS•HCl
Molekulargewicht
235.8
Löslichkeit
DMF: 3 mg/ml,DMSO: 5 mg/ml,Ethanol: 5 mg/ml,PBS (pH 7.2): 10 mg/ml
Lagerung
Store at -20°C
Allgemeine Hinweise
Wählen Sie anhand der Löslichkeitsdaten des Produkts ein geeignetes Lösungsmittel. Aliquotieren Sie die Stammlösung nach der Herstellung, um wiederholte Gefrier-Auftau-Zyklen zu vermeiden.
Verwenden Sie Stammlösungen bei Lagerung bei -80°C innerhalb von 6 Monaten bzw. bei -20°C innerhalb von 1 Monat.
Zur Verbesserung der Löslichkeit das Röhrchen auf 37°C erwärmen und für eine angemessene Dauer beschallen.
Versandbedingungen
Evaluierungsmuster werden mit Kühlakkus versandt. Andere verfügbare Größen werden bei Raumtemperatur oder auf Anfrage mit Kühlakkus versandt.

Rechner (Calculators)Molarität / Verdünnung / Molekulargewicht / Einheitenumrechnung / In-vivo-Formulierung / Löslichkeit

g/mol

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