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

AVN-101 hydrochloride 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 hydrochloride 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 hydrochloride 可用于研究广泛性焦虑症、抑郁症、精神分裂症和多发性硬化症等疾病。

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AVN-101 hydrochloride Chemical Structure

AVN-101 hydrochloride Chemical Structure

CAS No. : 1061354-48-0

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

AVN-101 hydrochloride 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 hydrochloride 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 hydrochloride can be studied in such diseases as general anxiety disorders, depression, schizophrenia, and multiple sclerosis[1].

IC50 & Target[1]

5-HT7 Receptor

0.153 nM (Ki)

5-HT2C Receptor

1.17 nM (Ki)

5-HT2A Receptor

1.56 nM (Ki)

5-HT6 Receptor

2.04 nM (Ki)

5-HT2B Receptor

10.6 nM (Ki)

5-HT1A Receptor

61 nM (Ki)

5-HT1B Receptor

720 nM (Ki)

H1 Receptor

0.58 nM (Ki)

Alpha-2B adrenergic receptor

0.41 nM (Ki)

Alpha-2A adrenergic receptor

1.77 nM (Ki)

Alpha-2C adrenergic receptor

3.55 nM (Ki)

Alpha-1B adrenergic receptor

9.4 nM (Ki)

Alpha-1A adrenergic receptor

18.9 nM (Ki)

Alpha-1D adrenergic receptor

30.2 nM (Ki)

分子量

340.89

Formula

C21H25ClN2

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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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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产品名称:
AVN-101 hydrochloride
目录号:
HY-117046A
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