A-317920,360551-59-3

A-317920 产品活性：A-317920 是一种选择性强效大鼠组胺 H3 受体 (H3R) 拮抗剂，全长大鼠和全长人类 H3R 的 pKi 值分别为 9.2 和 7.0。A-317920 对大鼠的选择性亲和力比人类 H3R 高 130 倍以上。A-317920 通过 H3R 阻断增强认知能力。 产品来源： www.medchemexpress.cn/a-317920.html 研究领域：GPCR/G Protein | Neuronal Signaling | Immunology/Inflammation 作用靶点：Histamine Receptor In Vitro: A-317920 is a potent antagonist at rat H3R in reversing R-α-methylhistamine [(R)-α-MeHA] inhibition of Forskolin-stimulated cAMP formation (pKb value of 9.1) but a weak antagonist at human H3R in cyclase (pKb value of 6.3) and calcium mobilization (pKb value of 7.3) assays in cells co-expressing Galphaqi5-protein. A-317920 potently antagonizes native H3Rs by blocking histamine inhibition of potassium-evoked [3H]histamine release from rat brain cortical synaptosomes (pKb value of 9.3) and (R)-α-MeHA reversal of electric field-stimulated guinea pig ileum contractions (pA2 value of 8.3). In Vivo: A-317920 (3-10 mg/kg; s.c; 30 min prior to training; for a total of five trials) significantly improves in the avoidance test in spontaneously hypertensive rat (SHR) pups. 相关产品：Histamine | Clemastine fumarate | Cimetidine | Terfenadine | Amitriptyline hydrochloride | Astemizole | Loratadine | Mecamylamine hydrochloride | Desloratadine | Famotidine | Diphenhydramine hydrochloride | Osthole | Doxepin Hydrochloride | (S)-(+)-Dimethindene maleate | Perphenazine | Fexofenadine hydrochloride | Ketotifen fumarate | Benztropine mesylate | Promethazine hydrochloride | Mianserin hydrochloride | Ritanserin | Ebastine | Lodoxamide | JNJ-7777120 | Mepyramine maleate | Mirtazapine | Chlorpheniramine maleate | Cetirizine dihydrochloride | Meclizine dihydrochloride | Adriforant hydrochloride 品牌介绍: MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供前沿最全的高品质小分子活性化合物；10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域；设有专业的实验中心和严格的质控、验证体系；提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；产品的生物活性多经各国客户实验验证；Nature, Cell, Science 等多种TOP期刊及制药专利收录了MCE客户的科研成果；专业团队跟踪前沿的制药及生命科学研究进展，为您提供全球前沿的活性化合物；与世界各大制药公司及知名科研机构建立了长期的合作。