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Beschreibung

A pyrrolocarboxamide compound that potently antagonizes TRP (transient receptor potential) family cation channel TRPV4 activity (IC50 = 17, 48, and 133 nM, respectively, against mouse, human, or rat TRPV4 in whole cell voltage-gated current measurement) in a reversible manner, displaying much reduced potency against human ERG and TRPM8 (IC50 = 368 and 780 nM, respectively) and little or no activity toward hKv1.3, hTRPA1, hTRPC5, hTRPV1/2/3/6, mTRPM7, mTRPV2, or rKv1.2. HC-067047 is efficacious (10 mg/kg via i.p.) in reducing micturition (urination) frequency and increasing voided urine volume of mice and rats suffering from CPA- (Cat. No. 239785) induced cystitis in vivo.