| 名称 | BMY 7378 dihydrochloride |
| 描述 | BMY 7378 dihydrochloride (BMY7378 HCl) , α1D-adrenergic receptor antagonist, is a weak partial agonist/antagonist of 5-HT1A receptor. |
| 激酶实验 | Phosphatase activities are determined on immunoprecipitates of the phosphatases. Briefly, 2×106 K562 cells are treated for 18 hr with Salubrinal (20 μM), PSI (10 nM), the combination of both drugs or okadaic acid (100 nM). After washing with PBS, cells are lysed for 15 min on ice either in PP1LB (for determination of PP1γ-activity; 20 mM Tris-HCl, pH 7.5, 1% Triton X-100, 10% glycerol, 132 mM NaCl, Roche complete protease inhibitor ) or in RIPA (for PP2A), supplemented with Roche complete protease inhibitor). Cell lysates containing 500 μg (PP1γ) or 300 μg (PP2A) protein are immunoprecipitated overnight at 4°C with 2-3 μg of the appropriate antibodies and then incubated with Protein A-Sepharose. Immunoprecipitates are washed three times in lysis buffer, followed by resuspension in phosphatase assay buffer (PP2A: 20 mM Tris-HCl, pH7.5, 0.1 mM CaCl2; PP1γ: 50 mM Tris HCl pH 7.0, 0.2 mM MnCl2, 0.1 mM CaCl2, 125 μg/mL BSA, 0.05% Tween 20), supplemented with 100 μM 6,8-difluoro-4-methyl-umbelliferyl phosphate (DiFMUP). Precipitates are allowed to react with substrate for 1 hr at 37°C on an Eppendorf Thermoshaker, centrifuged and DiFMU fluorescence is measured on a BioTek Lambda Fluoro 320 microplate reader (360 nmex/460 nmem). Phosphatase activities are given as percent change relative to the control (DMSO treated cells)[1]. |
| 体外活性 | 在大鼠体内,BMY7378（0.25-5 mg/kg,s.c.）剂量依赖性降低8-OH-DPAT（0.75 mg/kg,s.c.）诱导的前爪踩踏和头部摇晃.在麻醉大鼠的腹侧海马体中,大鼠体内微量渗析检测显示,BMY7378使5-HT释放出现剂量依赖性的显著减少.BMY7378 (pA2为8.67)与去甲肾上腺素作用可使大鼠主动脉收缩,效果比育亨宾 (pA2为6.62)高约100倍.BMY7378 (pA2：6.48)会拮抗人体隐静脉(α2C-肾上腺素受体)中去甲肾上腺素引起的收缩响应,效果比育亨宾(pA2为7.56)低10倍. |
| 体内活性 | BMY7378对α1D-肾上腺素受体亚型的作用有选择性{PKi: α1b-肾上腺素受体6.2（仓鼠）,7.2（人）；α1c-肾上腺素受体 6.1（牛）,6.6（人）；α1d-肾上腺素受体8.2（大鼠）,9.4（人）}。BMY7378对α2c-肾上腺素受体的选择性（pKi：6.54）是其他α2-肾上腺素受体的10倍。在大鼠中缝背核中,BMY7378（1-30 nM）具有剂量依赖性的抑制作用。 |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | Ethanol : 16 mg/mL (34.9 mM), Sonication is recommended.
DMSO : 85 mg/mL (185.42 mM), Sonication is recommended.
H2O : 84 mg/mL (183.24 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 5 mg/mL (10.91 mM), Sonication is recommended.
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| 关键字 | α2C-adrenoceptor | α1D-adrenoceptor | spontaneously hypertensive rats | Serotonin Receptor | selective | Inhibitor | inhibit | DopamineReceptor | Dopamine Receptor | D2 | BMY-7378 Dihydrochloride | BMY7378 Dihydrochloride | BMY-7378 | BMY7378 | BMY 7378 dihydrochloride | BMY 7378 Dihydrochloride | BMY 7378 | Beta Receptor | alpha 1-adrenoceptor | AdrenergicReceptor | Adrenergic Receptor | 5-hydroxytryptamine Receptor | 5HTReceptor | 5-HT1C | 5-HT1A receptor | 5-HT1A | 5-HT Receptor | 5HT Receptor |
| 相关产品 | Cefaclor monohydrate | Oxolinic acid | Alverine citrate | Dapoxetine hydrochloride | L-DOPA | Trazodone hydrochloride | Mianserin hydrochloride | 1,8-Cineole | D-Mannitol | Octopamine hydrochloride | Creatine | Isoprenaline hydrochloride |
| 相关库 | 抑制剂库 | 经典已知活性库 | 抗癌化合物库 | 已知活性化合物库 | 神经递质受体化合物库 | 神经信号分子库 | 5-羟色胺分子库 | 抗抑郁症化合物库 | GPCR靶点分子库 | 神经退行性疾病化合物库 | 膜蛋白靶向化合物库 | 疼痛相关化合物库 |