Home >> Research Area >>Neuroscience>>Muscarinic Receptor>> Cevimeline hydrochloride hemihydrate

Cevimeline hydrochloride hemihydrate

Agonist of muscarinic receptor (M1/M3) CAS# 153504-70-2

Cevimeline hydrochloride hemihydrate

Catalog No. BCC1471----Order now to get a substantial discount!

Product Name & Size Price Stock
Cevimeline hydrochloride hemihydrate: 5mg $69 In Stock
Cevimeline hydrochloride hemihydrate: 10mg Please Inquire In Stock
Cevimeline hydrochloride hemihydrate: 20mg Please Inquire Please Inquire
Cevimeline hydrochloride hemihydrate: 50mg Please Inquire Please Inquire
Cevimeline hydrochloride hemihydrate: 100mg Please Inquire Please Inquire
Cevimeline hydrochloride hemihydrate: 200mg Please Inquire Please Inquire
Cevimeline hydrochloride hemihydrate: 500mg Please Inquire Please Inquire
Cevimeline hydrochloride hemihydrate: 1000mg Please Inquire Please Inquire
Related Products

Quality Control of Cevimeline hydrochloride hemihydrate

Number of papers citing our products

Chemical structure

Cevimeline hydrochloride hemihydrate

3D structure

Chemical Properties of Cevimeline hydrochloride hemihydrate

Cas No. 153504-70-2 SDF Download SDF
PubChem ID 66577068 Appearance Powder
Formula C10H20ClNO2S M.Wt 253.79
Type of Compound N/A Storage Desiccate at -20°C
Solubility H2O : ≥ 50 mg/mL (204.27 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name 2-methylspiro[1,3-oxathiolane-5,3'-1-azabicyclo[2.2.2]octane];hydrate;hydrochloride
SMILES CC1OC2(CN3CCC2CC3)CS1.O.Cl
Standard InChIKey JKJRNPOQQPBPOV-UHFFFAOYSA-N
Standard InChI InChI=1S/C10H17NOS.ClH.H2O/c1-8-12-10(7-13-8)6-11-4-2-9(10)3-5-11;;/h8-9H,2-7H2,1H3;1H;1H2
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Cevimeline hydrochloride hemihydrate

DescriptionCevimeline hydrochloride hemihydrate, a novel muscarinic receptor agonist, is a candidate therapeutic drug for xerostomia in Sjogren's syndrome. IC50 value: Target: mAChR The general pharmacol. properties of this drug on the gastrointestinal, urinary, and reproductive systems and other tissues were investigated in mice, rats, guinea pigs, rabbits, and dogs. The in vitro metab. of SNI-2011 was also evaluated with rat and dog liver microsomes. After oral administration, plasma concns. of SNI-2011 reached to Cmax within 1 h in both species, suggesting that SNI-2011 was quickly absorbed, and then decreased with a t1/2 of 0.4-1.1 h. The bioavailability was 50% and 30% in rats and dogs, resp. Major metabolites in plasma were both S- and N-oxidized metabolites in rats and only N-oxidized metabolite in dogs, indicating that a large species difference was obsd. in the metab. of SNI-2011. Sex difference was also obsd. in the pharmacokinetics of SNI-2011 in rats, but not in dogs. In the in vitro study, chem. inhibition and pH-dependent studies revealed that the sulfoxidn. and N-oxidn. of SNI-2011 were mediated by cytochrome P 450 (CYP) and flavin-contg. monooxygenase (FMO), resp., in both species. In addn., CYP2D and CYP3A were mainly responsible for the sulfoxidn. in rat liver microsomes.

References:
[1]. Iga Y, Arisawa H, Ogane N, Saito Y, Tomizuka T, Nakagawa-Yagi Y, Masunaga H, Yasuda H, Miyata N. (+/-)-cis-2-methylspiro[1,3-oxathiolane-5,3'-quinuclidine] hydrochloride, hemihydrate (SNI-2011, cevimeline hydrochloride) induces saliva and tear secretions [2]. Omori Y, Asari T, Maruyama K, Kusama H, Kojima M, Shibata N. Effects of pilocarpine hydrochloride and cevimeline on submandibular/sublingual salivation in rat xerostomia model produced by X-ray irradiation. Arzneimittelforschung. 2003;53(5):342-50. [3]. Washio, Takuo; Kohsaka, Kazuhiro; Arisawa, Hirohiko; et al.Pharmacokinetics and metabolism of radiolabeled SNI-2011, a novel muscarinic receptor agonist, in healthy volunteers: Comprehensive understanding of absorption, metabolism and excretion using radi [4]. Washio, Takuo; Kohsaka, Kazuhiro; Arisawa, Hirohiko; et al.Pharmacokinetics and metabolism of the novel muscarinic receptor agonist SNI-2011 in rats and dogs.Arzneimittel-Forschung (2003), 53(1), 26-33. [5]. Arisawa, Hirohiko; Fukui, Kenji; Imai, Eiichi; et al.General pharmacological profile of the novel muscarinic receptor agonist SNI-2011, a drug for xerostomia in Sjogren's syndrome. Arzneimittel-Forschung (2002), 52(4), 225-232.

Cevimeline hydrochloride hemihydrate Dilution Calculator

Concentration (start)
x
Volume (start)
=
Concentration (final)
x
Volume (final)
 
 
 
C1
V1
C2
V2

calculate

Cevimeline hydrochloride hemihydrate Molarity Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
g/mol

calculate

Preparing Stock Solutions of Cevimeline hydrochloride hemihydrate

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 3.9403 mL 19.7013 mL 39.4027 mL 78.8053 mL 98.5066 mL
5 mM 0.7881 mL 3.9403 mL 7.8805 mL 15.7611 mL 19.7013 mL
10 mM 0.394 mL 1.9701 mL 3.9403 mL 7.8805 mL 9.8507 mL
50 mM 0.0788 mL 0.394 mL 0.7881 mL 1.5761 mL 1.9701 mL
100 mM 0.0394 mL 0.197 mL 0.394 mL 0.7881 mL 0.9851 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

Organizitions Citing Our Products recently

 
 
 

Calcutta University

University of Minnesota

University of Maryland School of Medicine

University of Illinois at Chicago

The Ohio State University

University of Zurich

Harvard University

Colorado State University

Auburn University

Yale University

Worcester Polytechnic Institute

Washington State University

Stanford University

University of Leipzig

Universidade da Beira Interior

The Institute of Cancer Research

Heidelberg University

University of Amsterdam

University of Auckland
TsingHua University
TsingHua University
The University of Michigan
The University of Michigan
Miami University
Miami University
DRURY University
DRURY University
Jilin University
Jilin University
Fudan University
Fudan University
Wuhan University
Wuhan University
Sun Yat-sen University
Sun Yat-sen University
Universite de Paris
Universite de Paris
Deemed University
Deemed University
Auckland University
Auckland University
The University of Tokyo
The University of Tokyo
Korea University
Korea University

Background on Cevimeline hydrochloride hemihydrate

Cevimeline hydrochloride hemihydrate is a novel and selective agonist of muscarinic acetylcholine receptor [1].

Muscarinic acetylcholine receptors (mAChRs) are acetylcholine receptors and mediate serous-saliva secretion and tear secretion. It is more sensitive to muscarine than nicotine [1].

Cevimeline hydrochloride hemihydrate induced contractions of isolated guinea pig ilea and trachea with EC50 values of 3.5 and 3 μM, respectively. Binding studies indicated that Cevimeline hydrochloride hemihydrate was a potent and highly selective M1-type muscarinic agonist. Also, it had a higher affinity for M1 receptors than other M1 agonists [2].

In normal rats and mice, X-irradiated saliva secretion defective rats and two strains of autoimmune disease mice, intraduodenal administrations of SNI-2011 (3-30 mg/kg) increased saliva and tear secretions in a dose-dependent way, which suggested that Cevimeline hydrochloride hemihydrate directly stimulated muscarinic receptors in salivary and lacrimal glands for saliva and tear secretions [1].

References:
[1].  Iga Y, Arisawa H, Ogane N, et al. (+/-)-cis-2-methylspiro[1,3-oxathiolane-5,3'-quinuclidine] hydrochloride, hemihydrate (SNI-2011, cevimeline hydrochloride) induces saliva and tear secretions in rats and mice: the role of muscarinic acetylcholine receptors. Jpn J Pharmacol, 1998, 78(3): 373-380.
[2].  Fisher A, Brandeis R, Karton I, et al. (+-)-cis-2-methyl-spiro(1,3-oxathiolane-5,3') quinuclidine, an M1 selective cholinergic agonist, attenuates cognitive dysfunctions in an animal model of Alzheimer's disease. J Pharmacol Exp Ther, 1991, 257(1): 392-403.

Featured Products
New Products
 

References on Cevimeline hydrochloride hemihydrate

(+/-)-cis-2-methylspiro[1,3-oxathiolane-5,3'-quinuclidine] hydrochloride, hemihydrate (SNI-2011, cevimeline hydrochloride) induces saliva and tear secretions in rats and mice: the role of muscarinic acetylcholine receptors.[Pubmed:9869272]

Jpn J Pharmacol. 1998 Nov;78(3):373-80.

We investigated effects of (+/-)-cis-2-methylspiro[1,3-oxathiolane-5,3'-quinuclidine] hydrochloride, hemihydrate (SNI-2011, cevimeline hydrochloride), a rigid analogue of acetylcholine, on saliva and tear secretions in rats and mice to evaluate its therapeutical efficacy for xerostomia and xerophthalmia in patients with Sjogren's syndrome and X-ray exposure in the head and neck. Intraduodenal administrations of SNI-2011 increased saliva secretion in a dose-dependent manner at doses ranging from 3 to 30 mg/kg in normal rats and mice, two strains of autoimmune disease mice and X-irradiated saliva secretion defective rats. The salivation elicited by SNI-2011 was completely inhibited by atropine. A similar atropine-sensitive response was observed in tear secretion. In rat submandibular/sublingual gland membranes, [3H]quinuclidinyl benzilate (QNB) binding was saturable, and Scatchard plot analysis revealed a single population of binding sites with a Kd of 22 pM and a maximal binding capacity of 60 fmol/mg protein. The competitive inhibition curve of the [3H]QNB binding by SNI-2011 was obtained, and its dissociation constant value calculated from IC50 was 1-2 microM. These results suggest that SNI-2011 increases saliva and tear secretions through a direct stimulation to muscarinic receptors in salivary and lacrimal glands, and they suggest that SNI-2011 should be beneficial to patients with Sjogren's syndrome and X-ray exposure in the head and neck.

Description

Cevimeline hydrochloride hemihydrate (SNI-2011) is a quinuclidine derivative of acetylcholine and a selective and orally active muscarinic M1 and M3 receptor agonist. Cevimeline hydrochloride hemihydrate stimulates secretion by the salivary glands and can be used as a sialogogue for xerostomia. Cevimeline hydrochloride hemihydrate can cross the blood-brain barrier (BBB).

Keywords:

Cevimeline hydrochloride hemihydrate,153504-70-2,Natural Products,Muscarinic Receptor, buy Cevimeline hydrochloride hemihydrate , Cevimeline hydrochloride hemihydrate supplier , purchase Cevimeline hydrochloride hemihydrate , Cevimeline hydrochloride hemihydrate cost , Cevimeline hydrochloride hemihydrate manufacturer , order Cevimeline hydrochloride hemihydrate , high purity Cevimeline hydrochloride hemihydrate

Online Inquiry for:

      Fill out the information below

      • Size:Qty: - +

      * Required Fields

                                      Result: