105431-72-9
105431-72-9 結(jié)構(gòu)式
基本信息
1,3-二氫-1-苯基-3,3-雙(4-吡啶基甲基)-2H-吲哚-2-酮
Linopirdine2HCl
LINOPIRDINE (DUP996)
LINOPIRDINE DIHYDROCHLORIDE
1-Phenyl-3,3-bis(pyridin-4-ylmethyl)indol-2-one
1-phenyl-3,3-bis(pyridin-4-ylmethyl)indolin-2-one
1-Phenyl-3,3-bis(4-pyridinylmethyl)-2,3-dihydro-1H-indole-2-one
2H-Indol-2-one, 1,3-dihydro-1-phenyl-3,3-bis(4-pyridinylmethyl)-
1-Phenyl-3,3-bis(pyridin-4-ylmethyl)indolin-2-one dihydrochloride
1,3-Dihydro-1-Phenyl-3,3-Bis(4-Pyridinylmethyl)-2H-Indol-2-One(WXC03502)
物理化學性質(zhì)
常見問題列表
IC50: 2.4 μM (M-type K + current)
Linopirdine (DuP 996) inhibits IC (measured as a medium afterhyperpolarization tail current, ImAHP) with an IC
50
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 (IC
50
>300 μM).
Linopirdine acts as an agonist of TRPV1 (transient receptor potential vanilloid type 1).
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%.
| Animal Model: | Male Sprague-Dawley rats (300-350 g) |
| Dosage: | 0.1, 0.5, 1, 3, 6 mg/kg |
| Administration: | 5 intravenous bolus injections of increasing doses |
| Result: | Transiently and dose-dependently increases MAP by up to 15%. |