SML0209
ANA-12
≥98% (HPLC), TrkB antagonist, powder
别名:
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
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关于此项目
经验公式（希尔记法）:
C22H21N3O3S
化学文摘社编号:
分子量:
407.49
UNSPSC Code:
51111800
PubChem Substance ID:
NACRES:
NA.77
MDL number:
产品名称
ANA-12, ≥98% (HPLC)
SMILES string
O=C1NCCCCC1NC(=O)c2ccccc2NC(=O)c3cc4ccccc4s3
InChI key
TUSCYCAIGRVBMD-UHFFFAOYSA-N
InChI
1S/C22H21N3O3S/c26-20(25-17-10-5-6-12-23-21(17)27)15-8-2-3-9-16(15)24-22(28)19-13-14-7-1-4-11-18(14)29-19/h1-4,7-9,11,13,17H,5-6,10,12H2,(H,23,27)(H,24,28)(H,25,26)
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: ≥5 mg/mL at 60 °C
storage temp.
2-8°C
Quality Level
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相关类别
Application
ANA-12用于抑制原代小鼠皮层神经元和原代大鼠海马培养物中的TrkB。
Biochem/physiol Actions
TrkB拮抗剂在小鼠中具有有效的抗焦虑样和抗抑郁样活性
神经营养素脑源性神经营养因子（BDNF）及其受体原肌球蛋白相关激酶B（TrkB）已成为几种情绪障碍（包括焦虑症和抑郁症）的病理生理学的关键介体。ANA-12是一种TrkB配体，可有效阻止BDNF激活受体。 它选择性地与TrkB结合并抑制TrkB下游的过程，而不会改变TrkA和TrkC的功能。在成年小鼠中，ANA-12模型可降低大脑中TrkB的活性，而不会影响神经元的存活。给予 ANA-12 的小鼠在预测人类抗焦虑和抗抑郁特性的各种试验中显示焦虑和抑郁相关行为减少。ANA-12 可能是研究 BDNF/TrkB 信号的一种有价值的工具，并可能构成开发下一代治疗心境障碍药物的先导化合物。还有 N-T19，其效价较低。
signalword
Warning
hcodes
Hazard Classifications
Acute Tox. 4 Oral
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
A Montalbano et al.
Hippocampus, 23(10), 879-889 (2013-05-16)
Long-term potentiation (LTP) is accompanied by increased spine density and dimensions triggered by signaling cascades involving activation of the neurotrophin brain-derived neurotrophic factor (BDNF) and cytoskeleton remodeling. Chemically-induced long-term potentiation (c-LTP) is a widely used cellular model of plasticity, whose
Maxime Cazorla et al.
The Journal of clinical investigation, 121(5), 1846-1857 (2011-04-21)
The neurotrophin brain-derived neurotrophic factor (BDNF) and its receptor tropomyosin-related kinase B (TrkB) have emerged as key mediators in the pathophysiology of several mood disorders, including anxiety and depression. However, therapeutic compounds that interact with TrkB receptors have been difficult
Elizabeth T Barfield et al.
Frontiers in behavioral neuroscience, 11, 237-237 (2017-12-23)
Early-life trauma can increase the risk for, and severity of, several psychiatric illnesses. These include drug use disorders, and some correlations appear to be stronger in women. Understanding the long-term consequences of developmental stressor or stress hormone exposure and possible
Valerie Jeanneret et al.
Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism, 38(11), 1896-1910 (2018-03-17)
Cerebral ischemia causes the presynaptic release of tissue-type plasminogen activator (tPA). The postsynaptic density (PSD) is a postsynaptic structure that provides a matrix where signaling transduction of excitatory synapses takes place. The postsynaptic density protein-95 (PSD-95) is the most abundant
Agnieszka Pałucha-Poniewiera et al.
Behavioural pharmacology, 30(6), 471-477 (2019-02-07)
Ketamine has been shown to induce a rapid antidepressant effect on patients with depression. In many animal models, both rapid and sustained antidepressant activities were also found in response to an antagonist of group II metabotropic glutamate receptors, LY341495, and
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