5-Aminoisoquinolin-1(2H)-one

5-AIQ (5-Aminoisoquinolin-1-one) is a water-soluble PARP-1 inhibitor. 5-AIQ is an important functional group in various drugs. 5-AIQ reduces the tissue injury associated with ischemia-reperfusion of the liver, it can be used for the research of the therapy conditions associated with ischemia-reperfusion of the liver[1][2].

Research Areas >> Cancer

Signaling Pathways >> Epigenetics >> PARP

Signaling Pathways >> Cell Cycle/DNA Damage >> PARP

PARP-1

5-AIQ (5000 μg) significantly reduces the number of colonies of TA 98 without metabolic activation, and TA 98 and TA 1537 with metabolic activation[1].

5-AIQ (150 and 250 mg/kg; p.o.; once) possess no significantly genotoxic in vivo system by micronucleus test[1]. 5-AIQ (3 mg/kg; p.o.; 5 min prior to onset of liver ischemia) reduces the tissue injury associated with ischemia-reperfusion of the liver[2]. Animal Model: Male mice[1] Dosage: 150 and 250 mg/kg Administration: Oral gavage; 150 and 250 mg/kg; once Result: Showed no increase of micronucleated polychromatic erythrocytes (MNPCE) in both 24 h and 48 h after both 125 and 250 mg/kg duration exposure as compared to the corresponding control. Animal Model: Anesthetised male Wistar rats with liver ischemia (for 30 minutes) and reperfusion (for 2 hours) [2] Dosage: 3 mg/kg Administration: Intravenous injection; 3 mg/kg; 5 min prior to onset of liver ischemia Result: Reduced PARP activation and showed less staining for ICAM-1.

[1]. Vinod KR, Chandra S, Sharma SK. Evaluation of 5-aminoisoquinoline (5-AIQ), a novel PARP-1 inhibitor for genotoxicity potential in vitro and in vivo. Toxicol Mech Methods. 2010 Feb;20(2):90-5.

[2]. Mota-Filipe H, et al. The novel PARP inhibitor 5-aminoisoquinolinone reduces the liver injury caused by ischemia and reperfusion in the rat. Med Sci Monit. 2002 Nov;8(11):BR444-53.