1. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  2. 5-HT Receptor Histamine Receptor Adrenergic Receptor
  3. AVN-101

AVN-101 是一种有效的,具有口服活性的,且可透过血脑屏障的 5-HT7 受体拮抗剂 (Ki 为 153 pM),对 5-HT65-HT2A5HT-2C 受体的效力稍弱 (Ki 值分别为 2.04 nM 、1.56   nM 和 1.17 nM)。AVN-101 还对组胺 H1 (Ki 为 0.58 nM) 和肾上腺素能 α2Aα2Bα2C (Ki= 0.41-3.6 nM) 受体表现出相当高的亲和力。AVN-101 可用于研究广泛性焦虑症、抑郁症、精神分裂症,阿尔茨海默症和多发性硬化症等疾病。

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AVN-101 Chemical Structure

AVN-101 Chemical Structure

CAS No. : 1025725-91-0

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

AVN-101 is a potent, brain-penetrant and orally active 5-HT7 receptor antagonist (Ki of 153 pM), with slightly lesser potency toward 5-HT6, 5-HT2A, and 5HT-2C receptors (Ki values of 2.04 nM, 1.56  nM, and 1.17  nM, respectively). AVN-101 also exhibits a rather high affinity toward histamine H1 (Ki of 0.58 nM) and adrenergic α2A, α2B, and α2C (Ki= 0.41-3.6 nM) receptors. AVN-101 can be studied in such diseases as general anxiety disorders, depression, schizophrenia, Alzheimer’s disease, and multiple sclerosis[1].

IC50 & Target

5-HT2A Receptor

 

5-HT2C Receptor

 

5-HT6 Receptor

 

5-HT7 Receptor

 

体外研究
(In Vitro)

AVN-101 显示出与放射性标记配体竞争组胺 H1 受体 (Ki = 0.58 nM) 和 H2 受体 (Ki = 89 nM) 的能力,同时对 H3 受体完全无活性[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

AVN-101 (0.05 mg/kg;腹腔注射;每日一次;连续 4 天) 可降低小鼠在强迫游泳测试中的不动性[1]
AVN-101 (0.02-5 mg/kg;腹腔注射;一次) 以 0.05 mg/kg 的剂量给药时,可预防小鼠在被动回避测试中由 Scopolamine (HY-N0296) 诱发的遗忘症[1]
AVN-101 (0.2、1 和 5 mg/kg) 可增加小鼠在高架十字迷宫开放臂中停留的时间[1]
AVN-101 在小鼠血浆中的稳定性较差:室温孵育 30 分钟后,原始化合物的残留量降低至 16%。同时,AVN-101 在猴和人血浆样本中表现出更好的稳定性:室温孵育 30 分钟后,原始化合物的残留量分别降至仅为 45% 和 68%[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Balb/C mice bearing porsolt forced swim and the tail suspension tests[1].
Dosage: 0.05 mg/kg
Administration: i.p.; once daily; for 4 days
Result: Reduced immobility in the forced swim test in mice.
Animal Model: Male BALB/c mice were used with amnesiac models based on either Scopolamine-induced memory impairment[1].
Dosage: 0.02 mg/kg, 0.05 mg/kg, 0.2 mg/kg, 0.5 mg/kg, 1 mg/kg, and 5 mg/kg
Administration: i.p.; once
Result: Prevented scopolamine-induced amnesia in a passive avoidance test in mice
分子量

304.43

Formula

C21H24N2

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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  • 稀释计算器

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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AVN-101
目录号:
HY-117046
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