354812-16-1 Usage
Uses
Used in Neuroscience Research:
3-amino-5-(4-methoxyphenyl)-2-Thiophenecarboxamide is used as a selective Nav1.1 activator for studying the physiology of Nav1.1 channels in HEK-293 cells expressing human Nav1.1 channels. It increases the Nav1.1-mediated current in a concentration-dependent manner (EC50=9.5 μM), making it a valuable tool for understanding the role of Nav1.1 channels in neuronal function.
Used in Neurological Disorders Research:
In rat hippocampal brain slices, AA43279 has been shown to increase the firing activity of parvalbumin-expressing, fast-spiking GABAergic interneurons and increase the spontaneous inhibitory post-synaptic currents recorded from pyramidal neurons. This suggests that it may have potential applications in the study and treatment of neurological disorders associated with altered neuronal activity.
Used in Anticonvulsant Drug Development:
3-amino-5-(4-methoxyphenyl)-2-Thiophenecarboxamide has displayed anticonvulsant activity in vivo, indicating its potential use in the development of anticonvulsant drugs for the treatment of epilepsy and other seizure disorders. Further research and development would be required to optimize its efficacy and safety as a therapeutic agent.
References
1) Frederiksen et al. (2017), A small molecule activator of Nav 1.1 channels increases fast-spiking interneuron excitability and GABAergic transmission in vitro and has anti-convulsive effects in vivo.; Eur. J. Neuroscience, 46 1887
Check Digit Verification of cas no
The CAS Registry Mumber 354812-16-1 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 3,5,4,8,1 and 2 respectively; the second part has 2 digits, 1 and 6 respectively.
Calculate Digit Verification of CAS Registry Number 354812-16:
(8*3)+(7*5)+(6*4)+(5*8)+(4*1)+(3*2)+(2*1)+(1*6)=141
141 % 10 = 1
So 354812-16-1 is a valid CAS Registry Number.
354812-16-1Relevant academic research and scientific papers
Hit-to-lead studies: The discovery of potent, orally active, thiophenecarboxamide IKK-2 inhibitors
Baxter, Andrew,Brough, Steve,Cooper, Anne,Floettmann, Eike,Foster, Steve,Harding, Christine,Kettle, Jason,McInally, Tom,Martin, Craig,Mobbs, Michelle,Needham, Maurice,Newham, Pete,Paine, Stuart,St-Gallay, Steve,Salter, Sylvia,Unitt, John,Xue, Yafeng
, p. 2817 - 2822 (2007/10/03)
A hit-to-lead optimisation programme was carried out on the thiophenecarboxamide high throughput screening hits 1 and 2 resulting in the discovery of the potent and orally bioavailable IKK-2 inhibitor 22.
