| Bioactivity | A-317920 is a selective and potent rat histamine H3 receptor (H3R) antagonist with pKi value of 9.2 and 7.0 for full-length rat and full-length human H3R, respectively. A-317920 exhibits over 130 fold selective affinity for the rat over the human H3R. A-317920 enhances cognition via H3R blockade[1]. |
| Invitro | A-317920 是大鼠 H3R 的强效拮抗剂，可逆转 R-α-甲基组胺 [(R)-α-MeHA] 对福斯可林刺激的 cAMP 形成 (pKb 值为 9.1) 的抑制，但在共表达 Galphaqi5-蛋白 的细胞中的环化酶 (pKb 值为 6.3) 和钙动员 (pKb 值为 7.3) 测定中，它对人类 H3R 是一种弱拮抗剂[1]。 A-317920 可有效拮抗天然 H3R，方法是阻断组胺抑制大鼠大脑皮层突触体钾诱发的 [3H] 组胺释放（pKb 值为 9.3）和 (R)-α-MeHA 逆转电场刺激的豚鼠回肠收缩（pA2 值为 8.3）[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> A-317920 相关抗体: |
| In Vivo | A-317920（3-10 mg/kg；皮下注射；训练前 30 分钟；共进行五次试验）显著提高了自发性高血压大鼠 (SHR) 幼崽的回避测试[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: |
| CAS | 360551-59-3 |
| Formula | C25H31N3O5 |
| Molar Mass | 453.53 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Timothy A Esbenshade, et al. Two novel and selective nonimidazole histamine H3 receptor antagonists A-304121 and A-317920: I. In vitro pharmacological effects. J Pharmacol Exp Ther. 2003 Jun;305(3):887-96. [2]. G B Fox, et al. Identification of novel H3 receptor (H3R) antagonists with cognition enhancing properties in rats. Inflamm Res. 2003 Apr:52 Suppl 1:S31-2. |