| 名稱 | A-437203 |
| 描述 | A-437203 (Lu201640) is A kind of based on 1 h - pyrimidin - 2 - one sca ? old, selective, new powerful d3 receptor antagonist, on D2, d3, and D4 receptor, Ki value 71, respectively 1.6 and 6220 nM. |
| 動物實(shí)驗(yàn) | Male Sprague-Dawley rats weighing 250-350 g are used for these experiments. Haloperidol (0.27, 1.33, and 2.66 μmol/kg=0.1, 0.5, and 1.0 mg/kg i.p.), A-437203 (LU-201640) (0.52, 1.75, 5.24, and 17.46 μmol/kg=0.3, 1.0, 3.0, and 10.0 mg/kg i.p.), and L-745,870 (0.23, 1.15, 2.3, and 5.7 μmol/kg=0.1, 0.5, 1.0, and 2.5 mg/kg i.p.) are tested initially alone in order to determine effective dose ranges. In those experiments, haloperidol, A-437203, and L-745,870 are administered i.p. 24, 5, and 0.5 h before the test swim. In the subsequent antagonism experiments, Haloperidol (0.27 μmol/kg), A-437203 (17.46 μmol/kg) or L-745,870 (1.15 μmol/kg) are injected i.p. 15 min prior to each quinpirole injection (0.4 and 1.0 μmol/kg s.c.). |
| 體外活性 | A-437203是一種具有高親和力的D3受體拮抗劑，并相對于其他多巴胺受體亞型具有較高的選擇性（與D2相比，對D3的選擇性高出44倍）[1]。 |
| 體內(nèi)活性 | A-437203在大鼠強(qiáng)迫游泳測試（FST）中單獨(dú)測試。A-437203劑量為0.52、1.75、5.24和17.46 μmol/kg，注射方式為靜脈注射。劑量的選擇基于A-437203對D3與D2多巴胺受體的選擇性。17.46 μmol/kg（10 mg/kg）或更低劑量的A-437203效果明顯由D3受體介導(dǎo)，而非D2受體。174.6 μmol/kg（100 mg/kg）等高劑量的化合物才能結(jié)合并阻斷D2受體，避免被烷化劑EEDG不可逆地失活。方差分析（ANOVA）表明，對于分析的任何行為，各處理組之間無顯著差異（對于不動行為F4, 45=1.12, p=0.359，對于攀爬行為F4, 45=0.188, p=0.943，對于游泳行為F4, 45=1.634, p=0.182）?；谶@些結(jié)果，選擇17.46 μmol/kg靜脈注射劑量的A-437203進(jìn)行進(jìn)一步實(shí)驗(yàn)[1]。 |
| 存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 60 mg/mL (131.43 mM)
|
| 關(guān)鍵字 | A-437203 | A-37203 | ABT925 | ABT 925 | A 437203 | A437203 | A 37203 |
| 相關(guān)產(chǎn)品 | Fluphenazine dihydrochloride | Octodrine | Oxolinic acid | Citicoline | Mirtazapine | Phenothiazine | Olanzapine | Mianserin hydrochloride | CLOZAPINE N-OXIDE | Doxepin hydrochloride | Octopamine hydrochloride | Promazine hydrochloride |
| 相關(guān)庫 | 抑制劑庫 | 經(jīng)典已知活性庫 | 已知活性化合物庫 | GPCR靶點(diǎn)分子庫 | 臨床期小分子藥物庫 | 膜蛋白靶向化合物庫 | 神經(jīng)退行性疾病化合物庫 | 藥物功能重定位化合物庫 | 抗癌臨床化合物庫 | 抗癌藥物庫 |