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.jpg): Failed to open stream: No such file or directory in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 117 ACS+Med+Chem+Lett
2013 ; 4
(2
): 293-6
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Optimization of a Novel Series of TRPV4 Antagonists with In Vivo Activity in a
Model of Pulmonary Edema
#MMPMID24900661
Hilfiker MA
; Hoang TH
; Cornil J
; Eidam HS
; Matasic DS
; Roethke TJ
; Klein M
; Thorneloe KS
; Cheung M
ACS Med Chem Lett
2013[Feb]; 4
(2
): 293-6
PMID24900661
show ga
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.