InvivoChem Cat #:V3653CAS #:883093-10-5 Purity >=98%Description: RO 4938581 (also known as Ro 4882224) is a novel, potent and selective GABAA alpha5 inverse agonist, with a Ki of 4.6 nM for GABAA alpha5beta3gamma2a, and shows a lower affinity at alpha1beta3gamma2a, alpha2beta3gamma2a, alpha3beta3gamma2a (Ki, 174, 185, 80 nM, respectively); RO 4938581 is used in the research of cognitive dysfunction. RO4938581 displays strong CYP1A2 autoinduction properties in rats. RO4938581 acts as a subtype-selective inverse agonist at the alpha5 subtype of the benzodiazepine binding site on the GABAA receptor. It has good selectivity for the alpha5 subtype and did not produce convulsant or anxiogenic effects in animal studies, making it a promising potential nootropic. Ro4938581 and a related derivative basmisanil (RG-1662, RO5186582) have subsequently been investigated for the alleviation of cognitive dysfunction in Down syndrome.
References: Bioorg Med Chem Lett. 2009 Oct 15; 19(20):5940-4.