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AZD-3161 is a potent and selective blocker of NaV1.7 channel, with a pIC50 of 7.1. AZD-3161 can be used for the research of neuropathic and inflammatory pain[1][2]. | [Definition]
ChEBI: Pavinetant is a member of the class of quinolines that is the amide obtained by formal condensation of the carboxy group of 3-[(methanesulfonyl)amino]-2-phenylquinoline-4-carboxylic acid with the amino group of (1S)-1-phenylpropan-1-amine. A neurokinin-3 receptor antagonist that has been trialled as a potential drug for treatment of schizophrenia and menopausal symptoms. It has a role as a neurokinin-3 receptor antagonist and an antipsychotic agent. It is a member of quinolines, a secondary carboxamide, a sulfonamide and an aromatic amide. | [in vivo]
AZD-3161 (16-99 μmol/kg; p.o.) displays a dose dependent antinociceptive effect in the phase 1 of the formalin model of pain in rats[1].
AZD-3161 (3 μmol/kg; i.v.) exhibits long half-life (2.2 h) and Vss (4.2 L/kg)[1].
AZD-3161 (10 μmol/kg; p.o.) exhibits high oral bioavailability (44%), long half-life (4.8 h) and Cmax (0.30 μmol/L)[1]. | [References]
[1] Kers I, et, al. Structure and activity relationship in the (S)-N-chroman-3-ylcarboxamide series of voltage-gated sodium channel blockers. Bioorg Med Chem Lett. 2012 Sep 1; 22(17): 5618-24. DOI:10.1016/j.bmcl.2012.06.105
[2] Bagal SK, et, al. Recent progress in sodium channel modulators for pain. Bioorg Med Chem Lett. 2014 Aug 15; 24(16): 3690-9. DOI:10.1016/j.bmcl.2014.06.038 |
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