Ro 10-5824 dihydrochloride 是选择性的多巴胺D4 受体部分激动剂,Ki=5.2 nM。
半岛bd体育手机客户端 描述
Ro 10-5824 dihydrochloride is a selective agonist of dopamine D4 receptor partial, (Ki of 5.2 nM).
体外活性
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[2].
体内活性
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[2].
Cas No.
189744-94-3
分子式
C17H22Cl2N4
分子量
353.29
储存和溶解度
H2O:60 mg/mL (169.83 mM)
DMSO:8.33 mg/mL (23.58 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years