Zamifenacin fumarateSelective M3 antagonist CAS# 127308-98-9 |
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| Cas No. | 127308-98-9 | SDF | Download SDF |
| PubChem ID | 20056967 | Appearance | Powder |
| Formula | C31H33NO7 | M.Wt | 531.6 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | UK 76654 | ||
| Solubility | Soluble to 100 mM in DMSO and to 25 mM in ethanol | ||
| Chemical Name | (3R)-1-[2-(1-,3-Benzodioxol-5-yl)et | ||
| SMILES | C1CC(CN(C1)CCC2=CC3=C(C=C2)OCO3)OC(C4=CC=CC=C4)C5=CC=CC=C5.C(=CC(=O)O)C(=O)O | ||
| Standard InChIKey | PMHKTAIGYOVZEZ-ZHWJIHCSSA-N | ||
| Standard InChI | InChI=1S/C27H29NO3.C4H4O4/c1-3-8-22(9-4-1)27(23-10-5-2-6-11-23)31-24-12-7-16-28(19-24)17-15-21-13-14-25-26(18-21)30-20-29-25;5-3(6)1-2-4(7)8/h1-6,8-11,13-14,18,24,27H,7,12,15-17,19-20H2;1-2H,(H,5,6)(H,7,8)/b;2-1+/t24-;/m1./s1 | ||
| 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. |
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| 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. |
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| 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. | ||
| Description | Selective M3 muscarinic receptor antagonist (pKi values are 8.52, 7.93, 7.90 and 7.78 for M3, M2, M1 and M4 receptors respectively). Displays higher affinity at ileal M3 receptors (pKi = 9.3) compared to oesophageal and tracheal M3 receptors (pKi values are 8.8 and 8.2 respectively). Inhibits gastrointestinal motility in vivo in the absence of cardiovascular effects. |
Zamifenacin fumarate Dilution Calculator
Zamifenacin fumarate Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 1.8811 mL | 9.4056 mL | 18.8111 mL | 37.6223 mL | 47.0278 mL |
| 5 mM | 0.3762 mL | 1.8811 mL | 3.7622 mL | 7.5245 mL | 9.4056 mL |
| 10 mM | 0.1881 mL | 0.9406 mL | 1.8811 mL | 3.7622 mL | 4.7028 mL |
| 50 mM | 0.0376 mL | 0.1881 mL | 0.3762 mL | 0.7524 mL | 0.9406 mL |
| 100 mM | 0.0188 mL | 0.0941 mL | 0.1881 mL | 0.3762 mL | 0.4703 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. | |||||
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Muscarinic receptors in isolated urinary bladder smooth muscle from different mouse strains.[Pubmed:12359634]
Br J Pharmacol. 2002 Oct;137(4):522-8.
1. The pharmacological characteristics of muscarinic receptors in male and female mouse urinary bladder smooth muscle from different strains (C57Bl/6, 129/SvJ and hybrid backcross N1F2) were studied. 2. (+)-Cis-dioxolane, oxotremorine-M, acetylcholine, carbachol and pilocarpine induced concentration-dependent contractions of the urinary bladder smooth muscle (range for pEC(50)=6.4-6.6, 6.2-6.7, 6.2-6.4, 5.4-6.0 and 0.0-5.1, T(max)=1.9-4.7 g, 1.3-3.4 g, 1.0-3.0 g, 1.4-2.4 and 0.0-0.3 g, respectively, n=4-6 depending on the gender and the strain). In females, these contractions were competitively antagonized by a range of muscarinic receptor antagonists (pK(B) value range, depending on the strain): atropine (8.0-8.9), pirenzepine (6.1-6.4), 4-DAMP (7.6-8.4), methoctramine (5.6-6.1), p-F-HHSiD (7.5-7.7), zamifenacin (7.7-8.4) and darifenacin (8.2-8.7). 3. In recontraction studies, in which the muscarinic M(3) receptor population was decreased, and conditions optimized to study M(2) receptor activation, methoctramine exhibited an affinity estimate consistent with muscarinic M(3) receptors (pK(B)=6.26+/-0.08, pA(2)=6.31+/-0.07; pK(B)=6.09+/-0.22, pA(2)=6.08+/-0.01 for female inbred strain 129/SvJ and hybrid backcross N1F2, respectively) or intermediate between the one expected for this compound at M(2) and M(3) receptors, (pK(B)=6.66+/-0.08, pA(2)=7.00+/-0.27 for female inbred strain C57BL/6). 4. These data study suggest that muscarinic M(3) receptors are the predominant, if not the exclusive, subtype mediating contractile responses to muscarinic agonists in female mouse urinary bladder smooth muscle, with strain differences.
Pre-clinical and clinical pharmacology of selective muscarinic M3 receptor antagonists.[Pubmed:10188786]
Life Sci. 1995;56(11-12):861-8.
Muscarinic M3 receptor antagonists have therapeutic potential for the treatment of disorders associated with altered smooth muscle contractility or tone. These include irritable bowel syndrome (IBS), chronic obstructive airways disease (COAD) and urinary incontinence. Zamifenacin is a potent muscarinic receptor antagonist on the guinea pig ileum (pA2 value 9.27) with selectivity over M2 receptors in the atria (135-fold) and M1/M4 receptors in the rabbit vas deferens (78-fold). In addition, zamifenacin had lower affinity for the M3 receptor in the salivary gland (pKi 7.97). In animals, zamifenacin potently inhibited gut motility in the absence of cardiovascular effects and with selectivity over inhibition of salivary secretion. In healthy volunteers, zamifenacin inhibited small and large bowel motility and increased the rate of gastric emptying over a dose range which was associated with minimal anticholinergic side effects. These data show that zamifenacin, a selective muscarinic M3 receptor antagonist, was well tolerated in man and was efficacious as an inhibitor of gut motility. Further studies in patients are required with muscarinic M3 receptor antagonists to confirm efficacy against symptoms in diseases associated with altered smooth muscle contractility.
Characterization of the interaction of zamifenacin at muscarinic receptors in vitro.[Pubmed:8566131]
Eur J Pharmacol. 1995 Oct 16;285(2):135-42.
The interaction of zamifenacin ((3R)-(+)-diphenylmethoxy-1-(3,4)-methylenedioxyphenethyl)pi peridine) at muscarinic receptor subtypes was studied using radioligand binding and functional techniques, in vitro. In radioligand binding studies, zamifenacin acted as a competitive antagonist, with the following pKi values; rat cerebral cortex (M1) 7.90 +/- 0.08, myocardium (M2) 7.93 +/- 0.13, submaxillary gland (M3) 8.52 +/- 0.04 and rabbit lung (M4) 7.78 +/- 0.04. In functional studies zamifenacin acted as a surmountable antagonist, exhibiting the following apparent affinity values; canine saphenous vein (putative M1) 7.93 +/- 0.09, guinea-pig left atria (M2) 6.60 +/- 0.04, guinea-pig ileum (M3) 9.31 +/- 0.06, guinea-pig oesophageal muscularis mucosae (M3) 8.84 +/- 0.04, guinea-pig trachea (M3) 8.16 +/- 0.04, and guinea-pig urinary bladder (M3) 7.57 +/- 0.15. Therefore, zamifenacin is selective for muscarinic M3 receptors in guinea-pig ileum, oesophageal muscularis mucosae, trachea and bladder over muscarinic M2 receptors in atria. The degree of muscarinic M3/M2 receptor selectivity depends upon the muscarinic M3 receptor preparation studied.
