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N-[2-[[(六氢-2-氧代-1H-氮杂卓-3-基)氨基]羰基]苯基]苯并[b]噻吩-2-甲酰胺

用途

ANA-12是有效,选择性的 TrkB 拮抗剂,对高亲和力和低亲和力位点的IC50 分别为45.6 nM和41.1 μM。

名称

[ CAS 号 ]:
219766-25-3

[ 中文名 ]:
N-[2-[[(六氢-2-氧代-1H-氮杂卓-3-基)氨基]羰基]苯基]苯并[b]噻吩-2-甲酰胺

[ 英文名 ]:
ANA-12

[英文别名 ]:

ANA-12

生物活性

[ 描述 ]:

ANA-12是有效,选择性的 TrkB 拮抗剂,对高亲和力和低亲和力位点的IC50 分别为45.6 nM和41.1 μM。

[ 相关类别 ]:

信号通路 >> 蛋白酪氨酸激酶 >> Trk Receptor

研究领域 >> 神经疾病

[体外研究]

ANA-12(10 nM)可阻止BDNF诱导的TrkB表达细胞中神经突向外生长,并在浓度高达10-100μM时完全消除BDNF的作用[1]。

[体内研究]

ANA-12(0.5mg/kg,ip)部分抑制小鼠全脑中的内源性TrkB活性。注射到小鼠体内的ANA-12表现出0.5mg/kg的抗焦虑和抗抑郁活性。 ANA-12(0.5,1.0和2.0 mg/kg)不影响神经元存活[1]。 ANA-12(0.5mg/kg)在脂多糖(LPS)诱导的抑郁样行为中显示出抗抑郁作用。 ANA-12(0.5mg/kg)显着减弱抑郁小鼠的不动时间增加。在TST,FST和SPT中,ANA-12(0.5mg/kg)在对照小鼠中不显示抗抑郁样作用[2]。 ANA-12(0.5 mg/kg,ip)可逆转CocSired大鼠中可卡因自我给药的减少[3]。

[动物实验]

在注射当天，氯胺酮（氯胺酮盐酸盐，10 mg / kg），7,8-二羟基黄酮（7,8-DHF; 10 mg / kg）和ANA-12，N2-（2 - {[（2-在磷酸盐缓冲盐水中的17％二甲基亚砜（DMSO）载体中制备氧代氮杂环庚烷-3-基）氨基]羰基}苯基）苯并[b]噻吩-2-甲酰胺（0.5mg / kg）。选择氯胺酮（10mg / kg），7,8-DHF（10mg / kg）和ANA-12（0.5mg / kg）的剂量。将所有化合物腹膜内（ip）给予小鼠。

[参考文献]

[1]. Cazorla M, et al. Identification of a low-molecular weight TrkB antagonist with anxiolytic and antidepressant activity in mice. J Clin Invest. 2011 May;121(5):1846-57.

[2]. Zhang JC, et al. Comparison of ketamine, 7,8-dihydroxyflavone, and ANA-12 antidepressant effects in the social defeat stress model of depression. Psychopharmacology (Berl). 2015 Dec;232(23):4325-35.

[3]. Vassoler FM, et al. Epigenetic inheritance of a cocaine-resistance phenotype. Nat Neurosci. 2013 Jan;16(1):42-7.

[4]. Fang X, et al. Brain-derived neurotrophic factor-TrkB signaling in the medial prefrontal cortex plays a role in the anhedonia-like phenotype after spared nerve injury. Eur Arch Psychiatry Clin Neurosci. 2018 Jun 7.

[相关活性小分子]

物理化学性质

[ 分子式 ]:
C₂₂H₂₁N₃O₃S

[ 分子量 ]:
407.48500

[ 精确质量 ]:
407.13000

[ PSA ]:
126.01000

[ LogP ]:
4.78680

[ 外观性状 ]:
white to beige

[ 储存条件 ]:
2-8°C

[ 水溶解性 ]:
DMSO: ≥5mg/mL at 60°C

安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302

[ 危害码 (欧洲) ]:
Xn

[ 风险声明 (欧洲) ]:
22

[ 危险品运输编码 ]:
NONH for all modes of transport

文献

Epigenetic regulation of spinal cord gene expression controls opioid-induced hyperalgesia.

Mol. Pain 10 , 59, (2014)

The long term use of opioids for the treatment of pain leads to a group of maladaptations which includes opioid-induced hyperalgesia (OIH). OIH typically resolves within few days after cessation of mo...

HBZ stimulates brain-derived neurotrophic factor/TrkB autocrine/paracrine signaling to promote survival of human T-cell leukemia virus type 1-Infected T cells.

J. Virol. 88(22) , 13482-94, (2014)

Brain-derived neurotrophic factor (BDNF) is a neurotrophin that promotes neuronal proliferation, survival, and plasticity. These effects occur through autocrine and paracrine signaling events initiate...

7, 8-Dihydroxyflavone Protects an Endothelial Cell Line from H2O2 Damage.

PLoS ONE 10 , e0135345, (2015)

7, 8-dihydroxyflavone (7, 8-DHF), a selective agonist for TrkB receptors, has been well studied for its neurotrophic functions. However, its roles outside the neural tissues have scarcely been studied...

更多文献

N-[2-[[(六氢-2-氧代-1H-氮杂卓-3-基)氨基]羰基]苯基]苯并[b]噻吩-2-甲酰胺

用途

名称

生物活性

物理化学性质

安全信息

文献

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