Ro 10-5824 dihydrochloride

Ro 10-5824 dihydrochloride is a selective agonist of dopamine D4 receptor partial, (Ki of 5.2 nM) . (In Vitro) :RO-10-5824 shows high affinity binding (Ki=5.2±0.9 nM (n=3) ), 250-fold selectivity vs human D3R, and >1000 fold selectivity for D4 vs human D2, D1, and D5 receptors. RO-10-5824 stimulates 35S-GTPγS binding (EC50 : 205±67 nM) (n=7) and maximal induction at 36±4% above basal level. (In Vivo) :The success rate in the ORD task increased by Ro 10-5824 (3 mg/kg) . At doses of 1 and 3 mg/kg, in the frontal cortex, Ro 10-5824 increases baseline gamma band activity. RO-10-5824 (10.0 mg/kg) does not increase center entries in the open field in a single 60-min session without the novel object present, nor does it increase overall transitions in the initial experiment with C57 mice.