Cevimelinehydrochloride

Cevimelinehydrochloride Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung

Although it was initially developed as a cognition enhancer, cevimeline was launched in the US for the treatment of dry mouth symptoms (xerostomia) in patients with Sjogren’s syndrome. Cevimeline is a racemic mixture of cis-oxathiolanes that can be obtained with a three step synthesis starting from quinuclidin-3-one followed by separation from its 9-12- fold less potent trans-diastereomer, This conformationally rigid analog of acetylcholine is a dual muscarinic M₁/M₃ agonist, selective versus M₂, M₄ and M₅ receptors. It is the fifth M, agonist that has failed in clinical trials against Alzheimer’s disease. On the contrary, the sialagogic effects of cevimeline caused by its stimulation of M₃ receptors in salivary and lacrimal glands were demonstrated in randomized double-blind placebo-controlled clinical trials (30 mg t.i.d. oral dose). Cevimeline (l-3 mg/kg i.v.) was as potent in dogs as pilocarpine (0.1-0.3 mg/kg i.v.), the only prior drug efficacious against xerostomia associated with Sjogren’s syndrome, but the effects of cevimeline lasted around 2-fold longer. No cardiovascular side effects were reported with cevimeline, unlike pilocarpine which has a 40-fold higher affinrty for the M₂ receptor. Cevimeline seems to bind extensively to tissues (volume of distribution 6 L/kg in man) since it was found to be less than 20% bound to human plasma proteins. It is metabolized into the cis and transsulfoxide, a glucuronide conjugate and the N-oxide.

Verwenden

Treatment of cancer.

Allgemeine Beschreibung

Cevimeline (Evoxac) iscis-2 -methylspiro {1-azabicyclo [2.2.2] octane-3, 5' -[1,3]oxathiolane} hydrochloride, hydrate (2:1). Cevimeline has amolecular weight of 244.79 and is a white to off white crystallinepowder. It is freely soluble in alcohol, chloroform, andwater. Cevimeline is a cholinergic agonist which binds to theM3 muscarinic receptor subtype, which results in an increasesecretion of exocrine glands, such as salivary and sweatglands. Because of these effects, it was approved for use in thetreatment of dry mouth associated with Sj?gren syndrome. Bystimulating the salivary muscarinic receptors cevimeline promotessecretion thereby alleviating dry-mouth in these patients.Cevimeline is metabolized by the isozymes CYP2D6and CYP3A3 and CYP3A4. It has a half-life of 5 hours.

Cevimelinehydrochloride Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte

Cevimelinehydrochloride Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

Firmenname	Telefon	E-Mail	Land	Produktkatalog	Edge Rate
career henan chemical co	+86-0371-86658258	sales@coreychem.com	China	29914	58
Chongqing Chemdad Co., Ltd	+86-023-61398051 +8613650506873	sales@chemdad.com	China	39916	58
CONIER CHEM AND PHARMA LIMITED	+8618523575427	sales@conier.com	China	49390	58
TargetMol Chemicals Inc.	+1-781-999-5354 +1-00000000000	marketing@targetmol.com	United States	19892	58
HANGZHOU CLAP TECHNOLOGY CO.,LTD	86-571-88216897,88216896 13588875226	sales@hzclap.com	CHINA	6313	58
AFINE CHEMICALS LIMITED	0571-85134551	info@afinechem.com	CHINA	15377	58
Hefei Hirisun Pharmatech Co., Ltd	+8615056975894	shawn@hirisunpharm.com	CHINA	9923	58
Dayang Chem (Hangzhou) Co.,Ltd.	571-88938639 +8617705817739	info@dycnchem.com	CHINA	52867	58
Guangzhou TongYi biochemistry technology Co.,LTD	+8613073028829	mack@tongyon.com	China	2996	58
Hefei TNJ Chemical Industry Co.,Ltd.	0551-65418684 +8618949823763	sales@tnjchem.com	China	25363	58

153504-70-2()Verwandte Suche:

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• (2R,5R)-2-Methylspiro[1,3-oxathiolane-5,8'-1-azabicyclo[2.2.2]octane] hydrate dihydrochloride
• CeviMeline hydrochloride heMihydrates
• Cevimeline HCl 1/2H2o
• cis-2-Methylspiro(1,3-oxathiolane-5,3')quinuclidine hydrochloride hydrate (2:2:1)
• Unii-p81Q6V85np
• Cevimeline HCl hemihydrate
• CevimelineHCl
• Cevimelinehydrochloride
• C07772
• Cevimeline hydrochloride hemihydrate
• Spiro[1-azabicyclo[2.2.2]octane-3,5'-[1,3]oxathiolane], 2'-methyl-, hydrochloride, hydrate (2:1), cis-
• Spiro[1-azabicyclo[2.2.2]octane-3,5'-[1,3]oxathiolane], 2'-methyl-, hydrochloride, hydrate (2:2:1), (2'R,3R)-rel-
• (+/-)-cis-2-Methylspiro[1,3-oxathiolane-5,3'-quinuclidine] hydrochloride hemihydrate
• AF-102B,SNI-2011
• Cevimeline hydrochloride（AF-102B, Evoxac）
• CS-646
• Cevimeline hydrochloride hemihydrate >=95% (HPLC, NMR)
• rac,cis-Cevimeline Hydrochloride Hemihydrate DISCONTINUED, offer C283500
• Cevimeline Hydrochloride (100 mg)
• 153504-70-2
• 2C10H17NOS2HClH2O
• C20H38Cl2N2O3S2
• CHNOSHClHO
• Inhibitors