| CAS |
219766-25-3 |
| Chinese Name |
N-(2-((2-氧代氮杂环庚烷-3-基)氨甲酰)苯基)苯并噻吩-2-甲酰胺 |
| English Name |
ANA-12 |
| Synonyms |
NebramycinIIsulfate |
| Molecular Formula |
C22H21N3O3S |
| Molecular Weight |
407.49 |
| Solubility |
Soluble in DMSO |
| Purity |
≥98% |
| Appearance |
White to off-white Solid |
| Storage |
Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| Delivery Time |
1-2 Days |
| EC |
EINECS 803-090-7 |
| MDL |
MFCD00117444 |
| SMILES |
O=C(C1=CC2=CC=CC=C2S1)NC3=CC=CC=C3C(NC4C(NCCCC4)=O)=O |
| InChIKey |
TUSCYCAIGRVBMD-UHFFFAOYSA-N |
| InChI |
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) |
| PubChem CID |
2799722 |
| Target Point |
Trk Receptor |
| Passage |
Protein Tyrosine Kinase/RTK;Neuronal Signaling |
| Background |
ANA-12 is a potent, selective TrkB antagonist. |
| Biological Activity |
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[1-4]。 |
| In Vitro |
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]。 |
| In Vivo |
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)显著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]。 |
| Animal Experiment |
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。 |
| Data Literature Source |
[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. |
| Unit |
Bottle |
| Specification |
2mg 5mg 10mg |
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