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SNAP 94847 (SNAP-94847) 是一种选择性黑色素浓缩激素受体1 拮抗剂,Ki 为 2.2 nM。它具有抗焦虑和抗抑郁活性,可减少小鼠的食物摄入。
SNAP 94847 (SNAP-94847) 是一种选择性黑色素浓缩激素受体1 拮抗剂,Ki 为 2.2 nM。它具有抗焦虑和抗抑郁活性,可减少小鼠的食物摄入。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 665 | 1-2周 | |
5 mg | ¥ 2,075 | 1-2周 | |
10 mg | ¥ 2,950 | 1-2周 | |
25 mg | ¥ 4,110 | 1-2周 | |
50 mg | ¥ 5,650 | 1-2周 | |
100 mg | ¥ 8,475 | 1-2周 | |
1 mL x 10 mM (in DMSO) | ¥ 2,350 | 1-2周 |
产品描述 | SNAP 94847 (SNAP-94847) is a selective and competitive MCH1 receptor (MCH1-R) antagonist (Ki: 2.2 nM). It has anxiolytic and antidepressant activity and reduces food intake in mice. |
靶点活性 | MCH1 receptor:2.2 nM (Ki, cell free) |
体外活性 | SNAP-94847表现出了对MCH1受体的亲和力(Ki: 2.2 nM)以及对人类R1A受体(>80倍)和D2受体(>500倍)的选择性优势[1]。 |
体内活性 | SNAP-94847(10 mg/kg,口服)对2小时内测量的基础水消耗量没有影响:对照组(2.0 mL)、16g处理组(2.3 mL)。MCH诱导的饮水量被SNAP-94847在1.0、2.5和10 mg/kg的剂量下显著抑制[1]。连续21天以fluoxetine或SNAP 94847(每日20 mg/kg)处理的BALB/c小鼠显示出在quinpirole诱导的运动活动增加方面有明显提升,且在使用SNAP 94847后,超动力出现的时间点比fluoxetine早。无论哪种化合物,连续使用7天也足以增强BALB/c小鼠对quinpirole的反应[2]。黑素集中激素的脑内及脑室内注射,以及皮质醇的长期注射,增加了强迫游泳测试中的不动时间,并降低了蔗糖偏好测试中的蔗糖偏好。所有这些抑郁样行为都被SNAP-94847的蓝斑微量注射所逆转[3]。 |
动物实验 | Chronically treated Sprague–Dawley rats were administered fluoxetine (18 mg/kg/day) or SNAP 94847 (20 mg/kg/day) via oral gavage in 20% beta-cyclodextrin for 2 weeks (1 injection, 6 h into light cycle). For acute treatment, drugs were given orally in 20% betacyclodextrin 1 h before testing. On each test day, locomotor activity was recorded during a 60 min habituation to the novel locomotor cage, after which the rats were administered quinpirole (0.3 mg/kg, i.p.) and returned immediately to the cage, where locomotor activity was measured for an additional 180 min. In each case-control animals were administered the corresponding vehicle, without drug [2]. |
别名 | SNAP-94847 |
分子量 | 478.57 |
分子式 | C29H32F2N2O2 |
CAS No. | 487051-12-7 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||
溶解度信息 | DMSO: 20 mg/mL (41.79 mM) | |||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||
DMSO
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