Clemastine Fumarate是一种选择性组胺H1受体拮抗剂,IC50为3 nM。
            
         Clemastine Fumarate (Clemastine) is a selective histamine H1 receptor antagonist with IC50 of 3 nM.
5-20 mg/kg 腹腔注射
| 					 						 动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数  | 									 | 			
例如,已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法:将88 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到该药物用于大鼠的等效剂量44 mg/kg。
	
                      
                              [1] Seifert R, et al. Mol Pharmacol, 1992, 42(2), 227-234.
                          
                      
                              [2] Charles I Ezeamuzie et. Al. Journal of Pharmacology and Experimental Therapeutics, 350(2), 444-454 (2014)
                          
                      
                              [3] Murat Baş et. Al. New England Journal of Medicine, 372(5), 418-425 (2015)
                          
                      
                      
                      
                      
                      
                      
                      
                   
| 分子式  C25H30ClNO5  | 
                        分子量 459.96  | 
                        CAS号 14976-57-9  | 
                        储存方式 ﹣20 ℃冷藏长期储存。冰袋运输  | 
                     
| 溶剂(常温) | 
                        DMSO 34 mg/mL  | 
                        Water <1 mg/mL  | 
                        Ethanol 3 mg/mL  | 
                     
体内溶解度 
| NCT02040298 | Multiple Sclerosis, Relapsing-Remitting | Drug: Clemastine|Drug: Placebo | University of California, San Francisco | Phase 2 | 2014-01-01 | 2016-04-14 | 
| NCT02521311 | Optic Neuritis | Drug: Clemastine|Drug: Placebo | University of California, San Francisco | Phase 2 | 2016-08-01 | 2017-03-13 | 
| NCT02613091 | Healthy Subjects | Drug: Clemastine fumarate | University of California, San Francisco | Phase 1 | 2016-04-01 | 2016-11-02 | 
| NCT00913549 | Allergy | Drug: Clemastine Fumarate Tablets, 2.68 mg (Cord Laboratories)|Drug: Tavist Tablets, 2.68 mg (Sandoz Pharmaceutical Corp.) | Sandoz | Phase 1 | 1989-12-01 | 2009-06-03 | 
| NCT01239719 | Allergy|Dermatitis | Drug: Dexamethasone + clemastine|Drug: Dexamethasone | Azidus Brasil | Phase 3 | 2011-03-01 | 2011-01-27 | 
| NCT01257061 | Eczema | Drug: Group 1|Drug: Group 2 | EMS | Phase 3 | 2012-09-01 | 2013-03-01 | 
| NCT01125761 | Dermatitis | Drug: dexamethasone 0.5 mg and 1.0 mg clemastine cream|Drug: Dexamethasone 0,5 mg cream | Azidus Brasil | Phase 3 | 2010-11-01 | 2010-10-25 | 
| NCT00481676 | Chronic Urticaria | Drug: Omalizumab 75-375 mg|Drug: Placebo to omalizumab|Drug: Loratadine|Drug: Clemastine | Novartis | Phase 2 | 2007-05-01 | 2011-09-14 | 
| NCT01154361 | Angioedema | Drug: Icatibant (subcutaneous) and plazebo (intravenous)|Drug: Cortisone + Clemastin (intravenous) and plazebo (subcutaneous) | Technische Universit盲t M眉nchen | Phase 2 | null | 2011-12-22 | 
注:以上所有数据均来自公开文献,并不保证对所有实验均有效,数据仅供参考。
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