Clemastine FumarateH1 antagonist CAS# 14976-57-9 |
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Quality Control & MSDS
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| Cas No. | 14976-57-9 | SDF | Download SDF |
| PubChem ID | 5281069 | Appearance | Powder |
| Formula | C25H30ClNO5 | M.Wt | 459.96 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | Meclastine fumarate | ||
| Solubility | DMSO : 14.29 mg/mL (31.07 mM; Need ultrasonic) H2O : 0.67 mg/mL (1.46 mM; Need ultrasonic) | ||
| Chemical Name | (2R)-2-[2-[(1R)-1-(4-Chlorophenylet | ||
| SMILES | CN1CCC[C@@H]1CCO[C@](C)(c2ccccc2)c3ccc(Cl)cc3.OC(=O)C=CC(O)=O | ||
| Standard InChIKey | PMGQWSIVQFOFOQ-YKVZVUFRSA-N | ||
| Standard InChI | InChI=1S/C21H26ClNO.C4H4O4/c1-21(17-7-4-3-5-8-17,18-10-12-19(22)13-11-18)24-16-14-20-9-6-15-23(20)2;5-3(6)1-2-4(7)8/h3-5,7-8,10-13,20H,6,9,14-16H2,1-2H3;1-2H,(H,5,6)(H,7,8)/b;2-1+/t20-,21-;/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 | H1-receptor antagonist. Enhances differentiation of oligodendrocyte progenitor cells into myelin basic protein-positive oligodendrocytes in vitro and promotes remyelination in vivo. Also displays antimuscarinic properties. Clinically-used antihistamine. |
Clemastine Fumarate Dilution Calculator
Clemastine Fumarate Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.1741 mL | 10.8705 mL | 21.741 mL | 43.482 mL | 54.3526 mL |
| 5 mM | 0.4348 mL | 2.1741 mL | 4.3482 mL | 8.6964 mL | 10.8705 mL |
| 10 mM | 0.2174 mL | 1.0871 mL | 2.1741 mL | 4.3482 mL | 5.4353 mL |
| 50 mM | 0.0435 mL | 0.2174 mL | 0.4348 mL | 0.8696 mL | 1.0871 mL |
| 100 mM | 0.0217 mL | 0.1087 mL | 0.2174 mL | 0.4348 mL | 0.5435 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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Clemastine Fumarate (Clemastine) is a selective histamine H1 receptor antagonist with IC50 of 3 nM.
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Randomized controlled trial of clemastine fumarate for treatment of experimental rhinovirus colds.[Pubmed:8729205]
Clin Infect Dis. 1996 Apr;22(4):656-62.
We used a rhinovirus challenge model to test the therapeutic efficacy of Clemastine Fumarate for reducing sneezing and nasal secretion in a double-blind, randomized clinical trial. Clemastine Fumarate (1.34 mg) or placebo was administered at 8 A.M. and 8 P.M. for 4 days, beginning 24 hours, 36 hours, 48 hours, and 60 hours after viral challenge. Infected evaluable subjects who received clemastine (n = 75) had reduced sneeze-severity scores compared with those who received placebo (n = 75) on illness days 2 (0.3 vs. 0.5; P = .003), 3 (0.4 vs. 0.8; P = .0003), 4 (0.3 vs. 0.5; P = .025), and 5 (0.1 vs. 0.3; P = .03); sneeze counts for infected evaluable subjects (vs. counts for those who received placebo) were reduced on illness days 2 (1.5 vs. 3.1; P = .01), 3 (1.7 vs. 5.6; P = .0001), and 5 (0.7 vs. 1.9; P = .03). Infected evaluable subjects who received treatment had reduced rhinorrhea scores (compared with those who received placebo) on illness days 2 (0.7 vs. 1.0; P = .04) and 3 (0.6 vs. 0.9; P = .04) and had reduced nasal secretion weights on day 3 (3.6 g vs. 6.3 g; P = .03). Over 4 days of treatment, mean sneeze scores for infected evaluable subjects (vs. scores for those who received placebo) were reduced by 50%, mean sneeze counts by 57%, mean rhinorrhea scores by 27%, and mean nasal secretion weights by 35%. Other cold symptoms were unaffected by treatment. Treatment with clemastine was associated with an excess incidence of dry mouth (6%), dry nose (19%), and dry throat (17%).
Neuropsychologic and cardiovascular effects of clemastine fumarate under pressure.[Pubmed:8574128]
Undersea Hyperb Med. 1995 Dec;22(4):401-6.
Allergic rhinitis and mild respiratory infections have been widely accepted as temporary contraindications for fitness to dive. Nonetheless, several sport and professional divers use antihistamines to ease ear, nose, and throat (ENT) problems, especially for opening tubal ostium. Some divers know they are unfit to dive, but for a variety of reasons (e.g., money or short holiday) they try to clear their ears. Thus, the use of antihistaminic drugs (like Clemastine Fumarate) is common during diving. This double-blind, crossover study indicates that this special antihistamine does not increase the sedative effects of nitrogen narcosis, nor does it increase the level of cardiac arrhythmias. Liberal use of antihistamines while diving cannot be recommended because of possible complications connected with different preparations and the temporary limitations they impose on the diver.
[Biomimetic oxidation of clemastine hydrogen fumarate].[Pubmed:8767851]
Pharmazie. 1996 Jun;51(6):409-14.
The reaction of Clemastine Fumarate (1) with the biomimetic system manganese(III)-5,10,15,20-tetrakis(pentafluoro-water. The reaction of 1 in aqueous solution with manganese(III)-5,10,15,20-tetrakis (pentafluorophenyl)-beta-tetrasulfonatoporphyrin chloride (MnTPFPS4PCl) as catalyst additional generates products of aromatic hydroxylation. Products were identified by TLC, UV, and MS. Thereby we found a close conformity with rat metabolism.
Effectiveness of clemastine fumarate for treatment of rhinorrhea and sneezing associated with the common cold.[Pubmed:9356796]
Clin Infect Dis. 1997 Oct;25(4):824-30.
Limited data support the use of first-generation antihistamines for treatment of the common cold. The purpose of this study was to test the effectiveness of Clemastine Fumarate, a first-generation antihistamine, for treatment of sneezing and rhinorrhea associated with naturally occurring common colds. Four hundred three subjects (202 Clemastine Fumarate recipients and 201 placebo recipients) who reported new onset (< 24 hours) of cold symptoms that included rhinorrhea or sneezing were studied. At baseline (day 1), the mean symptom-severity scores +/- SEM for the Clemastine Fumarate and placebo groups were not significantly different. The mean rhinorrhea-severity score +/- SEM was not different on day 2; however, on day 3, the mean rhinorrhea-severity score +/- SEM was 1.02 +/- 0.07 for the Clemastine Fumarate group and 1.39 +/- 0.07 for the placebo group (P < .001). This treatment effect persisted on day 4. A significant effect on sneezing was noted on days 2-4. Sedation occurred in 14% of the Clemastine Fumarate-treated subjects and 1.5% of the placebo-treated subjects (P < .0001).
Effect of histamine and histamine antagonists on natural and antibody-dependent cellular cytotoxicity of human lymphocytes in vitro.[Pubmed:6225527]
Cell Immunol. 1983 Oct 1;81(1):45-60.
The in vitro effect of histamine and its antagonists, cimetidine and Clemastine Fumarate, on natural killer (NK) and antibody-dependent cellular cytotoxicity (ADCC) activities of human lymphocytes was investigated. The histamine 1 (H1) antagonist, Clemastine Fumarate, and the histamine 2 (H2) antagonist, cimetidine, but not histamine alone, inhibited the NK and ADCC activities of lymphocytes when added directly to the mixture of effector and target cells in a 51Cr-release assay. This inhibition was proportional to the concentration of drugs added and was observed at various effector to target ratios against several targets. H1 and H2 antagonists also inhibited NK activities of T cells as well as Percoll-separated, NK-enriched effector cells. The inhibition was significantly reversed by histamine. In target binding assays, Clemastine Fumarate and cimetidine also decreased the target binding capacity of effector lymphocytes. Further, PBL precultured with histamine (10(-3)-10(-4) M) for 24 hr showed a significant decrease in their NK and ADCC activities. In coculture experiments, PBL precultured with histamine suppressed the NK activity of normal autologous effector lymphocytes. PBL precultured with histamine showed an increased number of OKT8+ cells, as estimated using monoclonal antibodies. The suppression of cytotoxicity was not due to either direct toxicity, steric hindrance, crowding, or cell death, but by functionally viable suppressor cells. An immunoregulatory role for histamine in NK and ADCC reactions is proposed.
Histamine1--histamine2 antagonism: effect of combined clemastine and cimetidine pretreatment on allergen and histamine-induced reactions of the guinea pig lung in vivo and in vitro.[Pubmed:6177209]
Agents Actions. 1982 Apr;12(1-2):113-8.
In a preliminary study high doses of the H1-antagonist clemastine (clem) and the H2-antagonist cimetidine (cim) were used in order to detect the side effects of both drugs on allergic reactions. After pretreatment with clem or clem/cim different guinea pigs were challenged with either OA or histamine. Bronchial obstruction was measured by body plethysmography using a new parameter ('compressed air'). Pretreatment with clem/cim in high doses protected guinea pigs against OA-induced bronchial obstruction much more effectively than H1-receptor antagonism alone; lower cim doses produced insignificant effects. In histamine-challenged animals cim showed no protective effects. In vitro clem/cim caused a marked reduction of histamine release measured in perfused lungs from 16.9 +/- 4.2 ng/ml (eight control cases) to 2.8 +/- 1.7 ng/ml (n = 8). Our preliminary data suggest that high doses of clem/cim can protect sensitized guinea pigs against allergen-induced bronchial obstruction by inhibiting histamine release.
Modulation of histamine-induced bronchoconstriction with inhaled, oral, and intravenous clemastine in normal and asthmatic subjects.[Pubmed:7330790]
Thorax. 1981 Oct;36(10):737-40.
Although histamine plays an important role in the pathophysiology of asthma through stimulation of H1 receptors, H1 antagonists are of only limited use in this disease when given orally. In order to investigate the pharmacological response to a specific H1 antagonist administered by different routes, we measured the effect of inhaled clemastine on airway responsiveness to histamine aerosol and compared the results with those after oral and intravenous administration in normal and asthmatic subjects. Inhalation of 0.6 mg clemastine provided significant protection without side effects and was comparable to intravenous administration of 1.0 mg in both groups. In normal subjects 2.0 mg clemastine orally was significantly less effective than the two other routes of administration whereas in asthmatics an enhanced reaction to histamine was observed.
