ChemicalBook > CAS DataBase List > CEVIMELINE, HYDROCHLORIDE SALT
CEVIMELINE, HYDROCHLORIDE SALT
CEVIMELINE, HYDROCHLORIDE SALT
- CAS No.107233-08-9
- Chemical Name:CEVIMELINE, HYDROCHLORIDE SALT
- CBNumber:CB1490161
- Molecular Formula:C10H17NOS
- Formula Weight:199.31
- MOL File:107233-08-9.mol
CEVIMELINE, HYDROCHLORIDE SALT Property
- 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
- NCI Dictionary of Cancer Terms Evoxac
- FDA UNII K9V0CDQ56E
- NCI Drug Dictionary Evoxac
- ATC code N07AX03
Safety
- Hazardous Substances Data :107233-08-9(Hazardous Substances Data)
- Symbol(GHS)
- Signal word
- Hazard statements
- Precautionary statements
CEVIMELINE, HYDROCHLORIDE SALT Chemical Properties,Usage,Production
- 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. - IC 50 mAChR1; mAChR3
- 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.
CEVIMELINE, HYDROCHLORIDE SALT Preparation Products And Raw materials
Raw materials
Preparation Products
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107233-08-9, CEVIMELINE, HYDROCHLORIDE SALTRelated Search:
- Pharmaceuticals
- Neurochemicals
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- Heterocycles
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- 药靶配体
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- C10H17NOSHCl
- C10H18ClNOS
- 顺式-2-甲基-1'-氮杂螺[[1,3]氧硫杂戊烷-5,3'-双环[2.2.2]辛烷]
- 顺式-2-甲基-1'-氮杂螺[[1,3]氧硫杂戊烷-5,3'-双环[2.2.2]辛烷
- 盐酸西维美林杂质
- 西维美林
- 107233-08-9
- Cevimeline (AF-102B)
- cis-2-Methyl-1'-azaspiro[[1,3]oxathiolane-5,3'-bicyclo[2.2.2]octane
- rac,cis-Cevimeline
- AF-102B;FKS-508
- CeviMeline(Evoxac)
- 2-Methyspiro(1,3-oxathiol
- 3R)-rel-
- 3]oxathiolane]
- Hsdb 7286
- (+/-)-cis-2-Methylspiro[1,3-oxathiolane-5,3'-quinuclidine]
- Cevimeline
- SNI-2011
- Evoxac
- AF-102B
- 2-methyspiro(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-
- (+/-)-cis-2-Methylspiro[1,3-oxathiolane-5,3quinuclidine
- CevimelineHClSalt