| Bioactivity | 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[1][2][3][4]. Cevimeline hydrochloride can cross the blood-brain barrier (BBB)[5]. |
| Target | Muscarinic M1 and M3 receptor |
| Invitro | In digested parotid cells, Cevimeline (0.1-100 μM) increases the intracellular Ca2+ concentration[1]. |
| 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[1]. Animal Model: |
| Name | Cevimeline hydrochloride |
| CAS | 107220-28-0 |
| Formula | C10H18ClNOS |
| Molar Mass | 235.77 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| Reference | [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. [3]. 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. [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. |
Cevimeline hydrochloride
CAS: 107220-28-0 F: C10H18ClNOS W: 235.77
Cevimeline hydrochloride (AF102B hydrochloride) is a quinuclidine derivative of acetylcholine and a selective and orally
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