| Identification | Back Directory | [Name]
CEVIMELINE, HYDROCHLORIDE SALT | [CAS]
107233-08-9 | [Synonyms]
Evoxac
AF-102B
3R)-rel-
SNI-2011
Hsdb 7286
Cevimeline
3]oxathiolane]
CevimelineHClSalt
CeviMeline(Evoxac)
2-Methyspiro(1,3-oxathiol
2-methyspiro(1,3-oxathiolane-5,3)quinuclidine
(+/-)-cis-2-Methylspiro[1,3-oxathiolane-5,3quinuclidine
(+/-)-cis-2-Methylspiro[1,3-oxathiolane-5,3'-quinuclidine]
Spiro[1-azabicyclo[2.2.2]octane-3,5'-[1,3]oxathiolane], 2'-methyl-, cis-
Spiro[1-azabicyclo[2.2.2]octane-3,5'-[1,3]oxathiolane], 2'-methyl-, (2'R,3R)-rel- | [Molecular Formula]
C10H18ClNOS | [MDL Number]
MFCD01961045 | [MOL File]
107233-08-9.mol | [Molecular Weight]
235.77 |
| Chemical Properties | Back Directory | [Appearance]
Off-White Solid | [Melting point ]
195-197°C | [Boiling point ]
308.5±42.0 °C(Predicted) | [density ]
1.19 | [storage temp. ]
Sealed in dry,Store in freezer, under -20°C | [solubility ]
Soluble in DMSO | [form ]
Powder | [pka]
9.51±0.40(Predicted) | [CAS DataBase Reference]
107233-08-9 |
| Hazard Information | Back Directory | [Chemical Properties]
Off-White Solid | [Uses]
A muscarinic M1 and M3 receptor agonist. Sialagogue | [Biological Activity]
cevimeline is a muscarinic receptor agonist especially on the m1 and m3 receptors. [1]cevimeline has been approved for use against symptoms of dry mouth by activating the m3 receptors of the parasympathetic nervous system. cevimeline is effective and safe in improving symptoms of dry eye with 20 mg three times per day [2]. cevimeline increased the intracellular ca+ level in parotid gland acinar cells over 1 μm and rat, enhanced the excitability via muscarinic receptors, thereby, cevimeline alleviates dry mouth symptoms by stimulating secretion by the salivary glands. cevimeline has a longer duration of salivation[3]. cevimeline plays a part in alzheimer’s disease. cevimeline decreased aβ (1–40) level in the cerebrospinal fluid (csf) at 1 mg/kg without changing α-apps in rabbit and significantly decreased csf aβ in ad patients.[4] | [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: | Male Wistar rats (8-week-old) injected with angiotensin-II[1] | | Dosage: | 0.008 mg/kg, 0.016 mg/kg | | Administration: | Intraperitoneal injection | | Result: | Showed slowly increasing and lasting salivation, and increased blood flow increment in the parotid gland and pressor response.
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| [IC 50]
mAChR1; mAChR3 | [storage]
Store at -20°C | [References]
1. f. b. vivino, i. al-hashimi, z. khan, f. g. leveque, p. l. salisbury, 3rd, t. k. tran-johnson, c. c. muscoplat, m. trivedi, b. goldlust and s. c. gallagher, arch intern med 1999, 159, 174-181. 2. m. ono, e. takamura, k. shinozaki, t. tsumura, t. hamano, y. yagi and k. tsubota, am j ophthalmol 2004, 138, 6-17. 3. k. ono, t. inagaki, t. iida, r. hosokawa and k. inenaga, j med invest 2009, 56 suppl, 375. 4. a. fisher, z. pittel, r. haring, n. bar-ner, m. kliger-spatz, n. natan, i. egozi, h. sonego, i. marcovitch and r. brandeis, j mol neurosci 2003, 20, 349-356. |
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