Brimonidine Tartrate 是一种高度选择性 α-adrenergic receptor 拮抗剂,其对α2A adrenoreceptor的 EC50 为 0.45 nM ,并用于治疗开角型青光眼或高眼压症。
Brimonidine Tartrate is a highly selective α-adrenergic receptor agonist with EC50 of 0.45 nM for the α2A adrenoreceptor, and used to treat open-angle glaucoma or ocular hypertension.
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] WoldeMussie E, et al. Invest Ophthalmol Vis Sci, 2001, 42(12), 2849-2855.
分子式 C15H16BrN5O6 |
分子量 442.22 |
CAS号 70359-46-5 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 90 mg/mL |
Water 75 mg/mL |
Ethanol <1 mg/mL |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT01229410 | Vitrectomy | Drug: 400 g Brimonidine Tartrate Implant|Drug: 200 g Brimonidine Tartrate Implant | Allergan | Phase 1 | 2010-12-01 | 2013-07-02 |
NCT02003534 | Glaucoma, Open-Angle|Ocular Hypertension | Drug: 0.15% Brimonidine Tartrate | Allergan | Phase 4 | 2010-07-01 | 2014-06-24 |
NCT02039765 | Hyperemia | Drug: Brimonidine tartrate | Bausch & Lomb Incorporated|ORA, Inc. | Phase 1 | 2014-02-01 | 2014-03-28 |
NCT02856919 | Chronic Persistent Vascular Facial Erythema | Drug: brimonidine tartrate | Galderma Brasil Ltda.|Eurotrials Brasil Consultores Cientificos Ltda | Phase 4 | 2016-06-01 | 2016-08-02 |
NCT02568111 | Relapsing-Remitting Multiple Sclerosis (RRMS) | Drug: peginterferon beta-1a|Drug: brimonidine tartrate|Drug: Vehicle Gel | Biogen | Phase 4 | 2016-02-01 | 2016-04-21 |
NCT00800423 | Corneal Edema|Visual Acuity | Drug: Brimonidine Tartrate 0.2%|Drug: Timolol maleate 0.5% | Rabin Medical Center | Phase 3 | 2009-01-01 | 2008-12-01 |
NCT00658619 | Macular Degeneration | Drug: 400 g Brimonidine Tartrate Implant|Drug: 200 g Brimonidine Tartrate Implant|Other: Sham (no implant) | Allergan | Phase 2 | 2008-05-01 | 2013-03-13 |
NCT01959230 | Hyperemia | Drug: Brimonidine Tartrate|Drug: Vehicle | Bausch & Lomb Incorporated|ORA, Inc. | Phase 3 | 2013-11-01 | 2014-07-24 |
NCT02761174 | Telangiectasias | Drug: Brimonidine|Other: IPL+air-cooling | Merete Haedersdal|Skinperium, Christine Dierickx|Ellipse A/S Agern All 11, 2970 Hrsholm|Bispebjerg Hospital | Phase 4 | 2016-03-01 | 2016-05-02 |
NCT00697541 | Erythematous Rosacea | Drug: 0.18% COL-118 facial gel (1.8 mg brimonidine)|Drug: 0.2% brimonidine ophthalmic solution (0.1 mg brimonidine tartrate/drop)|Drug: Advanced Eye Relief|Drug: COL-118 facial gel vehicle | Galderma | Phase 2 | 2008-05-01 | 2014-08-06 |
NCT01959243 | Hyperemia | Drug: Brimonidine Tartrate|Drug: Vehicle | Bausch & Lomb Incorporated|ORA, Inc. | Phase 3 | 2014-02-01 | 2014-07-24 |
NCT00972374 | Rhegmatogenous Macula-off Retinal Detachment | Drug: 400 ug Brimonidine Implant|Drug: 200 ug Brimonidine Implant|Other: Sham (no implant) | Allergan | Phase 2 | 2009-11-01 | 2013-03-13 |
NCT02249065 | Rosacea | Drug: Brimonidine | Galderma Laboratories, L.P. | Phase 4 | 2014-09-01 | 2016-01-20 |
NCT02818816 | Prostate Cancer | Drug: brimonidine tartrate 0.2%|Other: Carboxymethylcellulose Eye Drops | University Health Network, Toronto | Phase 4 | 2016-07-01 | 2016-07-27 |
NCT01675609 | Ocular Redness | Drug: Placebo|Drug: Brimonidine tartrate 0.025% | Eye Therapies, LLC | Phase 2 | 2012-08-01 | 2014-07-28 |
NCT01687426 | Glaucoma and Ocular Hypertension | Drug: Brimonidine Tartrate 0.025%|Drug: Vehicle | Eye Therapies, LLC | Phase 1 | 2012-09-01 | 2012-12-21 |
NCT01250236 | Impact of Brimonidine on the Cornea | Drug: brimonidine 0.1%|Drug: placebo | Augenarztpraxis Breisach | 2010-12-01 | 2010-12-02 | |
NCT00457795 | Open-angle Glaucoma|Ocular Hypertension | Drug: brimonidine 0.1% (Alphagan P) | Allergan | Phase 4 | 2006-12-01 | 2011-10-18 |
NCT02975557 | Dry Eye|Ocular Graft vs Host Disease|Meibomian Gland Dysfunction | Drug: Brimonidine 0.15%|Drug: Brimonidine 0.075%|Drug: Placebo | University of Illinois at Chicago | Phase 1|Phase 2 | 2016-05-01 | 2016-11-23 |
NCT02659670 | Rosacea | Other: internet survey|Drug: brimonidine topical gel 0.33% | Wake Forest University Health Sciences | Phase 4 | 2016-01-01 | 2016-11-01 |
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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