1. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  2. Histamine Receptor
  3. A-317920

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。

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A-317920 Chemical Structure

A-317920 Chemical Structure

CAS No. : 360551-59-3

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

IC50 & Target[1]

rat H3 receptor

9.2 (pKi)

human H3 receptor

7.0 (pKi)

体外研究
(In Vitro)

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.

体内研究
(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: Male spontaneously hypertensive rat (SHR) pups (postnatal day 20–24) were trained to avoid a mild footshock[1]
Dosage: 3 mg/kg,10 mg/kg
Administration: s.c; 30 min prior to training; for a total of five trials
Result: Significantly improved in the avoidance test when compared with saline controls.
分子量

453.53

Formula

C25H31N3O5

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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产品名称:
A-317920
目录号:
HY-122171
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