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。
产品描述
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.
体外活性
SNAP-94847 showed a favorable combination of MCH1 receptor affinity (Ki: 2.2 nM) and human R1A receptor (>80-fold) and D2 (>500-fold) selectivity [1].
体内活性
SNAP-94847 (10 mg/kg, p.o.) had no effect on basal water consumption measured over 2 h: vehicle-treated (2.0 mL); 16g-treated (2.3 mL). MCH-evoked water intake was inhibited significantly by SNAP-94847 at doses of 1.0, 2.5, and 10 mg/kg [1]. BALB/c mice treated for 21 days with fluoxetine or SNAP 94847 (20 mg/kg/day) showed marked increases in quinpirole-induced locomotor activity, with the onset of hyper-locomotion appearing earlier in the time course after SNAP 94847 compared to fluoxetine. Administration of either compound for 7 days was also sufficient to augment the quinpirole response in BALB/c mice [2]. The intra-locus coeruleus and intracerebroventricular injections of melanin-concentrating hormone and chronic injections of corticosterone increased immobility time in the forced swim test and decreased sucrose preference in the sucrose preference test. All these depressive-like behaviors were reversed by an intra-locus coeruleus microinjection of SNAP-94847 [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].
Cas No.
487051-12-7
分子式
C29H32F2N2O2
分子量
478.57
别名
SNAP-94847
储存和溶解度
DMSO:20 mg/mL (41.79 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years