Ro 10-5824 (dihydrochloride)

Ro 10-5824 dihydrochloride is a selective dopamine D4 receptor partial agonist, with K_i of 5.2 nM. IC50 & Target: Ki: 5.2 nM (dopamine D4 receptor)^[2] In Vitro: RO-10-5824 shows high affinity binding with a K_i=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 with an EC₅₀ value of 205±67 nM (n=7) and maximal induction at 36±4% above basal level^[2]. In Vivo: Ro 10-5824 (3 mg/kg) increases the success rate in the ORD task. At doses of 1 and 3 mg/kg, Ro 10-5824 increases baseline gamma band activity in the frontal cortex. Ro 10-5824 has no effect on spontaneous locomotion^[1]. 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^[2].