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生物活性
SB705498 is a TRPV1 antagonist for hTRPV1, antagonizes capsaicin, acid, and heat activation of TRPV1 with IC50 of 3 nM, 0.1 nM and 6 nM, shows a degree of voltage dependence, exhibits >100-fold selectivity for TRPV1 over TRPM8. Phase 2.
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体外研究
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体内研究
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激酶实验
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细胞实验
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动物实验
3，10 和 30 mg/kg 口服给药
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不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）
|  动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数 |
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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。
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参考文献
[1] Gunthorpe MJ, et al. J Pharmacol Exp Ther. 2007, 321(3), 1183-1192.
[2] Chizh BA, O'Donnell MB, Napolitano A et al. The effects of the TRPV1 antagonist SB-705498 on TRPV1 receptor-mediated activity and inflammatory hyperalgesia in humans. Pain. 2007 Nov;132(1-2):132-41.
[3] Rami HK, Thompson M, Stemp G et al. Discovery of SB-705498: a potent, selective and orally bioavailable TRPV1 antagonist suitable for clinical development. Bioorg Med Chem Lett. 2006 Jun 15;16(12):3287-91.
分子式
C17H16BrF3N4O |
分子量
429.23 |
CAS号
501951-42-4 |
储存方式
﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂（常温）
|
DMSO
≥85 mg/mL |
Water
<1 mg/mL |
Ethanol
20 mg/mL |
体内溶解度
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Clinical Trial Information ( data from http://clinicaltrials.gov )
| NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
| NCT01673529 | Dermatitis, Atopic | Drug: SB705498|Drug: Placebo | GlaxoSmithKline | Phase 1 | 2012-07-01 | 2016-11-18 |
| NCT01424514 | Rhinitis | Drug: SB-705498|Drug: Placebo | GlaxoSmithKline | Phase 2 | 2010-12-01 | 2016-11-29 |
| NCT00269022 | Migraine, Acute | Drug: SB-705498 | GlaxoSmithKline | Phase 2 | 2006-01-01 | 2009-05-15 |
| NCT01476098 | Rhinitis | Drug: Placebo|Drug: SB-705498 | GlaxoSmithKline | Phase 2 | 2011-04-01 | 2016-11-30 |
| NCT01439308 | Rhinitis | Drug: Placebo|Drug: SB-705498 | GlaxoSmithKline | Phase 2 | 2009-12-01 | 2016-11-30 |
| NCT00281684 | Toothache | Drug: SB-705498 | GlaxoSmithKline | Phase 2 | 2005-12-01 | 2011-03-10 |
| NCT00461682 | Irritable Colon|Fecal Urgency|Irritable Bowel Syndrome (IBS) | Drug: SB-705498 | GlaxoSmithKline | Phase 2 | 2007-01-01 | 2012-05-31 |
| NCT00731250 | Rhinitis | Drug: SB-705498|Drug: Placebo|Other: Caspaicin | GlaxoSmithKline | Phase 1 | 2008-07-01 | 2017-03-13 |
| NCT01424397 | Rhinitis | Drug: SB-705498|Drug: FP|Drug: placebo | GlaxoSmithKline | Phase 2 | 2011-04-01 | 2016-11-18 |
| NCT00907933 | Rhinitis | Drug: SB-705498|Drug: SB-705498|Drug: SB-705498|Drug: SB-705498|Drug: SB-705498|Drug: Placebo|Drug: SB-705498|Drug: SB-705498|Drug: Placebo | GlaxoSmithKline | Phase 1 | 2008-11-01 | 2016-10-26 |
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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