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Proxyfan(Proxifan)是一种高亲和力的组胺H3受体的protean拮抗剂/激动剂,具有从完全激动剂到完全逆激动剂的全谱药理活性,取决于给定组织或脑区域内组成活性和静止H3受体之间的竞争。Proxyfan在喂食相关的下丘脑腹内侧核中作为中性拮抗剂,在大鼠基底外侧杏仁核(BLA)中作为激动剂。

Proxyfan(Proxifan)是一种高亲和力的组胺H3受体的protean拮抗剂/激动剂,具有从完全激动剂到完全逆激动剂的全谱药理活性,取决于给定组织或脑区域内组成活性和静止H3受体之间的竞争。Proxyfan在喂食相关的下丘脑腹内侧核中作为中性拮抗剂,在大鼠基底外侧杏仁核(BLA)中作为激动剂。
| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 1 mg | ¥ 1,980 | In stock | |
| 5 mg | ¥ 4,920 | In stock | |
| 10 mg | ¥ 7,130 | In stock | |
| 25 mg | ¥ 10,600 | In stock | |
| 50 mg | ¥ 13,800 | In stock | |
| 100 mg | ¥ 17,500 | In stock |
Proxyfan 相关产品
| 产品描述 | Proxyfan (Proxifan) is a high-affinity protean antagonist/agonist of histamine H3 receptors with a full spectrum of pharmacological activity ranging from full agonist to full inverse agonist(antagonist), depending on the competition between constitutively active and resting H3 receptors within a given tissue or brain region.Proxyfan acts as a neutral antagonist in the feeding-associated ventral medial nucleus of the hypothalamus, and as a agonist in the basolateral amygdala of the rat (BLA). |
| 靶点活性 | Rat H3LR:2.9 nM (Ki), Human H3LR:2.7 nM (Ki) |
| 体外活性 | Proxyfan 是一种组胺 H3 受体的中性拮抗剂(neutral antagonist),其对大鼠和人类 H3 受体的结合常数(Ki 值)分别为 2.9 nM 和 2.7 nM,显示出较高的亲和力。[1] |
| 体内活性 | H3受体中性拮抗剂Proxyfan在大鼠中通过腹腔注射给药。Proxyfan(0.2–5.0 mg/kg)在光照期或黑暗期对自由进食大鼠的摄食量均无影响。在夜间,Proxyfan拮抗了H3受体激动剂Imetit(10 mg/kg)引起的促食欲作用以及反向激动剂Thioperamide(2 mg/kg)引起的抑食作用。[2] |
| 别名 | Proxifan |
| 分子量 | 216.28 |
| 分子式 | C13H16N2O |
| CAS No. | 177708-09-7 |
| Smiles | N1=CNC(=C1)CCCOCC=2C=CC=CC2 |
| 密度 | 1.115g/cm3 |
| 存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||
| 溶解度信息 | DMSO: 4 mg/mL (18.49 mM), Sonication is recommended. H2O: 4 mg/mL (18.49 mM), Sonication is recommended. | ||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||
DMSO/H2O
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