AR-C 102222

AR-C102222 hydrochloride is a potent, competitive, orally active and highly selective inducible nitric oxide synthase (iNOS) inhibitor, with an IC50 of 37 nM[1]. AR-C102222 hydrochloride has antinociception and anti-inflammatory activities[2].

Signaling Pathways >> Immunology/Inflammation >> NO Synthase

Research Areas >> Inflammation/Immunology

Research Areas >> Neurological Disease

AR-C102222 (3, 10, 30, 100 mg/kg, P.O.) attenuates arachidonic acid-induced ear inflammation and possesses anti-inflammatory activity[2]. AR-C102222 shows good efficacy in a rat adjuvant-induced arthritis model[3]. Animal Model: Male Balb/c mice (20-25 g)[2]. Dosage: 3, 10, 30, 100 mg/kg. Administration: P.O. 55 min before the administration of 0.6% acetic acid (i.p., 1 mL/100 g volume). Result: Significantly inhibited arachidonic acid-induced ear inflammation following a dose of 100 mg/kg of has a maximal inhibition of approximately 79%.

[1]. Tinker AC, et al. 1,2-Dihydro-4-quinazolinamines: potent, highly selective inhibitors of inducible nitric oxide synthase which show antiinflammatory activity in vivo. J Med Chem. 2003 Mar 13;46(6):913-6.

[2]. LaBuda CJ, et al. Antinociceptive activity of the selective iNOS inhibitor AR-C102222 in rodent models of inflammatory, neuropathic and post-operative pain. Eur J Pain. 2006 Aug;10(6):505-12. Epub 2005 Aug 24.

[3]. Yoon J, et al. Syntheses of 1,2,3-triazolyl salicylamides with inhibitory activity on lipopolysaccharide-induced nitric oxide production. Bioorg Med Chem Lett. 2011 Apr 1;21(7):1953-7.