化合物SNAP-94847 T5406

Product Introduction
Bioactivity


英文名: SNAP 94847

描述: 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。

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].

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].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 20 mg/mL (41.79 mM)


关键字: inhibit | Antidepressant | MCHR1 (GPR24) | Melanin concentrating hormone receptor 1 | SNAP 94847 | Inhibitor | SNAP94847 | anxiolytic | anxiety

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