ANA-12

Names

[ CAS No. ]:
219766-25-3

[ Name ]:
ANA-12

[Synonym ]:
ANA-12

Biological Activity

[Description]:

ANA-12 is a potent and selective TrkB antagonist with IC50s of 45.6 nM and 41.1 μM for the high and low affinity sites, respectively.

[Related Catalog]:

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> Trk Receptor

Research Areas >> Neurological Disease

[In Vitro]

ANA-12 (10 nM) prevents BDNF-induced neurite outgrowth in the TrkB-expressing cells, and completely abolishes the effects of BDNF at concentrations up to 10-100 μM[1].

[In Vivo]

ANA-12 (0.5 mg/kg, i.p.) partially inhibits the total endogenous TrkB activity in the whole brain of mice. ANA-12, injected in mice, demonstrates anxiolytic and antidepressive activities at 0.5 mg/kg. ANA-12 (0.5, 1.0, and 2.0 mg/kg) does not affect neuron survival[1]. ANA-12 (0.5 mg/kg) shows antidepressant effects in lipopolysaccharide (LPS)-induced depression-like behavior. ANA-12 (0.5 mg/kg) significantly attenuates an increased immobility time in depressed mice. In the TST, FST, and SPT, ANA-12 (0.5 mg/kg) does not show antidepressant-like effects in the control mice[2]. ANA-12 (0.5 mg/kg, i.p.) reverses the diminished self-administration of cocaine in CocSired rats[3].

[Animal admin]

On the day of injection, ketamine (ketamine hydrochloride, 10 mg/kg), 7,8-dihydroxyflavone (7,8-DHF; 10 mg/kg), and ANA-12, N2-(2-{[(2-oxoazepan-3-yl) amino]carbonyl}phenyl)benzo[b]thiophene-2-carboxamide (0.5 mg/kg) are prepared in vehicle of 17 % dimethyl sulfoxide (DMSO) in phosphate-buffered saline. The doses of ketamine (10 mg/kg), 7,8-DHF (10 mg/kg), and ANA-12 (0.5 mg/kg) are selected. All compounds are administered intraperitoneally (i.p.) to mice.

[References]

[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.

[Related Small Molecules]

Entrectinib | LOXO-101 | LM22B 10 | GW441756 | Repotrectinib | GNF-5837 | Altiratinib | LM22A-4 | Selitrectinib (LOXO-195) | Tyrphostin AG 879 | Belizatinib | Tavilermide | AZ-23 | CH7057288 | CE-245677

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₂H₂₁N₃O₃S

[ Molecular Weight ]:
407.48500

[ Exact Mass ]:
407.13000

[ PSA ]:
126.01000

[ LogP ]:
4.78680

[ Appearance of Characters ]:
white to beige

[ Storage condition ]:
2-8°C

[ Water Solubility ]:
DMSO: ≥5mg/mL at 60°C

Safety Information

[ Symbol ]:

GHS07

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H302

[ Hazard Codes ]:
Xn

[ Risk Phrases ]:
22

[ RIDADR ]:
NONH for all modes of transport

Articles

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...

Related Compounds

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