Introduction of 105431-72-9 :
Linopirdine (DuP 996) is an orally active, selective M-type K+ current (IM; Kv7; KCNQ Channels) inhibitor with an IC50 of 2.4 μM. Linopirdine is a TRPV1 agonist. Linopirdine, a putative cognition enhancing drug, increases acetylcholine release in rat brain tissue[1][2][3]. IC50 & Target: IC50: 2.4 μM (M-type K+ current)[1] In Vitro: Linopirdine (DuP 996) inhibits IC (measured as a medium afterhyperpolarization tail current, ImAHP) with an IC50 of 16.3 μM. Linopirdine (100 μM) weakly inhibits the K+ leak current, IL, the transient outward current, IA, the delayed rectifier, IK, and the slow component of IAHP, by 28, 37, 36 and 52 percent, respectively. The mixed Na+/K+ inward rectifying current, IQ, is essentially unaffected by Linopirdine (IC50>300 μM)[1].
Linopirdine acts as an agonist of TRPV1 (transient receptor potential vanilloid type 1)[3].
In Vivo: Linopirdine (DuP 996; i.v.; 0.1-6 mg/kg; increasing doses) transiently (10-15 min) and dose-dependently increases MAP by up to 15%[2].
