861393-28-4 Usage
Uses
Used in Pharmaceutical Industry:
A-740003 is used as a P2X7 receptor antagonist for the development of a radiotracer to image neuroinflammation in neurological disorders.
Used in Medical Imaging:
A-740003 is used as a radiotracer for positron emission tomography (PET) to visualize and monitor neuroinflammation in the brain, aiding in the diagnosis and treatment of various neurological conditions.
Biological Activity
Potent, selective and competitive P2X 7 receptor antagonist (IC 50 values are 18 and 40 nM for rat and human receptors respectively). Displays selectivity over a variety of P2X and P2Y receptors up to a concentration of 100 μ M. Reduces nociception in animal models of persistent neuropathic and inflammatory pain.
Biochem/physiol Actions
A-740003 is a selective P2X7 purinoceptor antagonist.
references
[1]. prisca honore, diana donnelly-roberts, marian t. namovic, et al. a-740003 [n-(1-{[(cyanoimino)(5-quinolinylamino)methyl]amino}-2,2-dimethylpropyl)-2-(3,4-dimethoxyphenyl)acetamide], a novel and selective p2x7 receptor antagonist, dose-dependently reduces neuropathic pain in the rat. journal of pharmacology and experimental therapeutics, 2006, 319:1376-1385.
Check Digit Verification of cas no
The CAS Registry Mumber 861393-28-4 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 8,6,1,3,9 and 3 respectively; the second part has 2 digits, 2 and 8 respectively.
Calculate Digit Verification of CAS Registry Number 861393-28:
(8*8)+(7*6)+(6*1)+(5*3)+(4*9)+(3*3)+(2*2)+(1*8)=184
184 % 10 = 4
So 861393-28-4 is a valid CAS Registry Number.
861393-28-4Relevant academic research and scientific papers
Discovery and biological evaluation of novel cyanoguanidine P2X7 antagonists with analgesic activity in a rat model of neuropathic pain
Perez-Medrano, Arturo,Donnelly-Roberts, Diana L.,Honore, Prisca,Hsieh, Gin C.,Namovic, Marian T.,Peddi, Sridhar,Shuai, Qi,Wang, Ying,Faltynek, Connie R.,Jarvis, Michael F.,Carroll, William A.
experimental part, p. 3366 - 3376 (2010/04/03)
We disclose the design of a novel series of cyanoguanidines that are potent (IC50 ? 10-100 nM) and selective (≥100-fold) P2X7 receptor antagonists against the other P2 receptor subtypes such as the P2Y2, P2X4, and P2X3. We also found that these P2X7 antagonists effectively reduced nociception in a rat model of neuropathic pain (Chung model). Particularly, analogue 53 proved to be effective in the Chung model, with an ED50 of 38 μmol/kg after intraperitoneal administration. In addition compound 53 exhibited antiallodynic effects following oral administration and maintained its efficacy following repeated administration in the Chung model. These results suggest an important role of P2X7 receptors in neuropathic pain and therefore a potential use of P2X7 antagonists as novel therapeutic tools for the treatment of this type of pain.
P2X7 antagonists for treating neuropathic pain
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Page/Page column 19, (2008/06/13)
The present invention discloses a method for treating neuropathic pain using compounds of formula I or compositions containing compounds of formula I.
