1421703-70-9Relevant articles and documents
Optimization of a novel series of TRPV4 antagonists with in vivo activity in a model of pulmonary edema
Hilfiker, Mark A.,Hoang, Tram H.,Cornil, Johan,Eidam, Hilary S.,Matasic, Daniel S.,Roethke, Theresa J.,Klein, Michael,Thorneloe, Kevin S.,Cheung, Mui
, p. 293 - 296 (2013)
High-throughput screening and subsequent hit optimization identified 1-piperidinylbenzimidazoles, exemplified by compound 1, as TRPV4 inhibitors. Lead optimization identified potent TRPV4 blocker 19, which has good target activity and pharmacokinetic properties. Inhibitor 19 was then profiled in an in vivo rat model, demonstrating its ability to inhibit TRPV4-mediated pulmonary edema.
SIGNALING-BIASED MU OPIOID RECEPTOR AGONISTS
-
Page/Page column 16; 18, (2017/10/11)
The invention provides -opioid receptor agonists that are analgesic agents and that promote diminished side effects relative to a comparably effective dose of morphine. The side effects that are absent or attenuated include one or more of the following: constipation, respiratory depression, tolerance, dependence, nausea, confusion, sedation, hypotension, and post-treatment withdrawal symptoms.