Publications by authors named "Azusa Nozu"
P2X receptor is an ATP-gated ion channel, mainly localized on peripheral sensory neurons. Currently, several clinical trials are being conducted with P2X receptor antagonists for the treatment of chronic pain or cough. To identify a P2X lead compound, we reexamined the HTS evaluation compounds and selected dioxotriazine derivatives from which we identified a hit compound.
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- - A new series of compounds known as (6-aminopyridin-3-yl)(4-(pyridin-2-yl)piperazin-1-yl) methanone derivatives were discovered to selectively block the TRPV4 channel and reduce pain in animal models.
- - The research focused on enhancing a previously identified compound (16d) to develop a more effective compound (26i) that showed promising results.
- - The paper details the design, synthesis, and analysis of how the structure of these compounds relates to their effectiveness (structure-activity relationship or SAR).
A series of 2',4'-dimethyl-[4,5'-bithiazol]-2-yl amino derivatives have been identified as selective TRPV4 antagonists that display inhibition potencies against 4α-phorbol 12,13-didecanoate (4αPDD), well known as a TRPV4 selective agonist and/or a hypotonicity. In particular, 9-(6-((2',4'-dimethyl-[4,5'-bithiazol]-2-yl)amino)nicotinoyl)-3-oxa-9-azabicyclo[3.3.
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