Loratadine是H1受体反向激动剂,IC50>32 μM。
Loratadine is a histamine H1 receptor antagonist, used to treat allergies. Also acts as a selective inhibitor of B(0)AT2 with IC50 of 4 μM.
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] Cuboni S, et al. J Med Chem, 2014, 57(22), 9473-9479.
分子式 C22H23ClN2O2 |
分子量 382.88 |
CAS号 79794-75-5 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 50 mg/mL |
Water <1 mg/mL |
Ethanol 77 mg/mL |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT01311336 | Pegfilgrastim-induced Back and Leg Pain | Drug: Loratadine|Drug: placebo | University of Vermont|Cancer and Leukemia Group B | Phase 2 | 2011-05-01 | 2013-01-23 |
NCT02593747 | Histamine H1 Antagonists, Non-Sedating | Drug: Loratadine oral solution|Drug: Loratadine (Claritin peach syrup) | Bayer | Phase 1 | 2015-12-01 | 2017-02-10 |
NCT02305979 | Leukemia|Lymphoma | Drug: Loratadine | Wake Forest University Health Sciences | 2014-12-01 | 2017-02-20 | |
NCT00963573 | Rhinitis | Drug: Loratadine|Drug: Betamethasone | Merck Sharp & Dohme Corp. | Phase 4 | 2003-09-01 | 2015-04-20 |
NCT00837915 | Healthy | Drug: Loratadine 10mg /Pseudoephedrine Sulfate 240 mg Extended-Release Tablets | Ranbaxy Laboratories Limited|Ranbaxy Inc. | 2002-06-01 | 2009-02-05 | |
NCT00730912 | Perennial Allergic Rhinitis | Drug: loratadine|Drug: loratadine|Drug: loratadine | Merck Sharp & Dohme Corp. | Phase 4 | 2008-06-01 | 2015-09-01 |
NCT00845546 | Healthy | Drug: 10 mg Loratadine/240 mg Pseudoephedrine Sulfate Extended-Release Tablets | Ranbaxy Laboratories Limited|Ranbaxy Inc. | 2002-06-01 | 2009-02-16 | |
NCT00762983 | Rhinitis, Allergic, Seasonal|Rhinitis, Allergic, Perennial|Urticaria|Pruritus | Drug: loratadine | Merck Sharp & Dohme Corp. | 2008-03-01 | 2015-02-12 | |
NCT00776217 | Healthy | Drug: loratadine 10 mg orally disintegrating tablets | Ranbaxy Laboratories Limited|Ranbaxy Inc. | 2006-06-01 | 2008-10-20 | |
NCT00776282 | Healthy | Drug: loratadine 10 mg orally disintegrating | Ranbaxy Laboratories Limited|Ranbaxy Inc. | 2006-07-01 | 2008-10-20 | |
NCT02513290 | Allergic Rhinitis | Drug: Bilastine|Drug: Loratadine | Universidade do Sul de Santa Catarina | Phase 4 | 2013-08-01 | 2015-07-30 |
NCT01228630 | Perennial Allergic Rhinitis | Drug: Cloratadd-D|Drug: Allegra-D | Azidus Brasil|EMS S/A | Phase 3 | 2011-08-01 | 2016-04-07 |
NCT02932774 | Allergic Rhinitis|Hay Fever|SAR|Rhinitis, Allergic, Seasonal | Drug: Cetirizine|Drug: Loratadine|Other: Placebo | Johnson & Johnson Consumer and Personal Products Worldwide|Pfizer | Phase 4 | 2001-03-01 | 2016-11-27 |
NCT01673620 | Allergic Rhinitis | Drug: Montelukast 10 mg/loratadine 10 mg|Drug: Placebo | Merck Sharp & Dohme Corp. | Phase 3 | 2012-07-01 | 2015-11-19 |
NCT02576808 | Rhinitis,Allergic | Drug: Ginger extract|Drug: Loratadine | Thai Traditional Medical Knowledge Fund|Thammasat University | Phase 2 | 2015-10-01 | 2015-10-13 |
NCT02392039 | Lymphoma | Drug: Pegfilgrastim|Drug: Loratadine|Other: Placebo|Behavioral: Questionnaires | M.D. Anderson Cancer Center|Amgen | 2015-12-01 | 2017-01-10 | |
NCT02653339 | Rhinitis, Allergic, Perennial | Drug: Qufeng Shengshi Fang and Loratadine|Drug: Loratadine | Peking Union Medical College Hospital | 2016-06-01 | 2016-04-21 | |
NCT01451996 | Healthy | Drug: Claritin | University of Chicago | Phase 4 | 2011-10-01 | 2013-12-09 |
NCT00946608 | Allergy | Drug: Loratadine 10 mg Tablets Under Fasting Conditions (Sandoz, Inc.)|Drug: Loratadine 10 mg Tablets Under Fed Conditions (Sandoz, Inc.)|Drug: Claritin (Loratadine) 10 mg Tablets Under Fed Conditions (Schering) | Sandoz | Phase 1 | 2005-06-01 | 2009-07-24 |
NCT01055756 | Allergic Rhinitis | Drug: Loratadine + Pseudoephedrine sulfate | Azidus Brasil | Phase 3 | 2010-01-01 | 2010-10-26 |
NCT01469234 | Rhinitis | Drug: loratadine|Drug: fexofenadine|Drug: placebo to loratadine|Drug: placebo to fexofenadine | Bayer | Phase 4 | 2011-10-01 | 2015-02-20 |
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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