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别名 (R)-(-)-α-甲基组胺二氢溴酸盐
(R)-(-)-α-Methylhistamine dihydrobromide 是一种高效、选择性且可透过血脑屏障的 H3 组胺受体激动剂,具有较高受体亲和力,能够增强记忆保持并减轻大鼠模型中的认知障碍,是研究中枢组胺能信号及 H3 受体介导的学习和记忆调控的重要药理学探针。

(R)-(-)-α-Methylhistamine dihydrobromide 是一种高效、选择性且可透过血脑屏障的 H3 组胺受体激动剂,具有较高受体亲和力,能够增强记忆保持并减轻大鼠模型中的认知障碍,是研究中枢组胺能信号及 H3 受体介导的学习和记忆调控的重要药理学探针。
| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 1 mg | ¥ 389 | 现货 | |
| 5 mg | ¥ 936 | 现货 | |
| 10 mg | ¥ 1,490 | 现货 | |
| 25 mg | ¥ 2,980 | 现货 | |
| 50 mg | ¥ 4,290 | 现货 | |
| 100 mg | ¥ 5,970 | 现货 |
| 产品描述 | (R)-(-)-α-Methylhistamine dihydrobromide is a potent, selective, and brain-penetrant agonist of the H3 histamine receptor with high receptor affinity, capable of enhancing memory retention and attenuating cognitive impairment in rat models, making it a valuable pharmacological probe for elucidating central histaminergic signaling and H3 receptor-mediated modulation of learning and memory processes. |
| 靶点活性 | H3 receptor:50.3 nM (kd) |
| 体外活性 | (R)-(-)-α-Methylhistamine dihydrobromide is an H3-agonist that is > 10 times as potent as histamine (HA).(R)-(-)-α-Methylhistamine dihydrobromide has only weak affinities for H1 and H2 receptor with a pKi=4.8 and < 3.5, repectively. Its selectivity toward H3-receptors is > 1,000 times as high as that of HA. (R)-(-)-α-Methylhistamine dihydrobromide displays >200-fold selectivity over H4 receptors[1]. |
| 体内活性 | 在小鼠和大鼠模型中,腹腔注射 (i.p.) (R)-(-)-α-Methylhistamine dihydrobromide(例如 6.3 mg/kg)可降低组胺主要代谢物 tele-methylhistamine (t-MH) 的稳态水平,而不会改变总组胺水平。这表明其抑制了组胺的周转。在麻醉诱导的健忘症大鼠模型中,10 mg/kg (i.p.) 预处理可逆转由 Propofol 引起的记忆保持缺陷 [2][3][4]。 |
| 别名 | (R)-(-)-α-甲基组胺二氢溴酸盐 |
| 分子量 | 287 |
| 分子式 | C6H13Br2N3 |
| CAS No. | 868698-49-1 |
| Smiles | C[C@@H](N)CC1=CN=CN1.Br.Br |
| 密度 | no data available |
| 存储 | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
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