Cevimeline

Names

[ Name ]:
Cevimeline

[Synonym ]:
3]oxathiolane]
CevimelineHClSalt
CEVIMELINE, HYDROCHLORIDE SALT
(2R,2'R)-2'-Methylspiro[4-azabicyclo[2.2.2]octane-2,5'-[1,3]oxathiolane]
cis-2'-Methylspiro[4-azabicyclo[2.2.2]octane-2,5'-[1,3]oxathiolane]
Evoxac
AF-102B
(2R,2'R)-2'-Methylspiro[4-azabicyclo[2.2.2]octan-2,5'-[1,3]oxathiolan]
(2R,2'R)-Cevimeline
Cevimeline
(2R,2'R)-rel-2'-Methylspiro[4-azabicyclo[2.2.2]octane-2,5'-[1,3]oxathiolane]
3R)-rel
Spiro[1-azabicyclo[2.2.2]octane-3,5'-[1,3]oxathiolane], 2'-methyl-, (2'R,3R)-
SNI-2011

Biological Activity

[Description]:

Cevimeline (Evoxac) is a parasympathomimetic and muscarinic agonist, with particular effect on M3 receptors; used in the treatment of dry mouth associated with sjogren's syndrome.IC50 value:Target: M3 receptor

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> mAChR

Signaling Pathways >> Neuronal Signaling >> mAChR

Research Areas >> Neurological Disease

[References]

[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]. 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.

[3]. 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.

[4]. Voskoboynik B, et al.Cevimeline (Evoxac) overdose.J Med Toxicol. 2011 Mar;7(1):57-9.

[5]. Tajiri S, et al. Dosage form design and in vitro/in vivo evaluation of cevimeline extended-release tablet formulations.Int J Pharm. 2010 Jan 4;383(1-2):99-105. Epub 2009 Sep 10.

[Related Small Molecules]