1072921-02-8
1072921-02-8
Chemical Structure
A-889425
- CAS No.: 1072921-02-8
- Formula:C19H18F3N3O3S
- Molecular Weight:425.42
IUPAC Name: 3'-methyl-N-(4-((trifluoromethyl)sulfonyl)phenyl)-3,6-dihydro-2H-[1,2'-bipyridine]-4-carboxamide
InChIKey: DYXUIRJHJRVUJH-UHFFFAOYSA-N
SMILES: O=C(C1=CCN(C2=NC=CC=C2C)CC1)NC3=CC=C(S(=O)(C(F)(F)F)=O)C=C3
Biological Activity: A-889425 is an oral active selective TRPV1 receptor antagonist with the with an IC50 of 335 nM (rat) and 34 nM (human). A-889425 has good penetration into the CNS and reduces mechanical allodynia and spinal neuron responses to mechanical stimulation of Complete Freund's adjuvant (HY-153808)-inflamed rat hind paws[1][2].
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A-889425 | A-889425 is an oral active selective TRPV1 receptor antagonist with the with an IC50 of 335 nM (rat) and 34 nM (human). A-889425 has good penetration into the CNS and reduces mechanical allodynia and spinal neuron responses to mechanical stimulation of Complete Freund's adjuvant (HY-153808)-inflamed rat hind paws. | |||||||||||||||||||||
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References
- [1]. McGaraughty S, et al. Contributions of central and peripheral TRPV1 receptors to mechanically evoked and spontaneous firing of spinal neurons in inflamed rats. J Neurophysiol. 2008;100(6):3158-3166. [Content Brief]
- [2]. Brederson JD, et al. TRPV1 antagonist, A-889425, inhibits mechanotransmission in a subclass of rat primary afferent neurons following peripheral inflammation. Synapse. 2012;66(3):187-195. [Content Brief]
