Ro 10-5824 dihydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Ro 10-5824 diHClide 是多巴胺 D4 受体部分的选择性激动剂（Ki 为 5.2 nM）。

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.

RO-10-5824 shows high affinity binding with a 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 with an EC50 value of 205±67 nM (n=7) and maximal induction at 36±4% above basal level.

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. 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.

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GPCR/G Protein

Dopamine Receptor

Human Endogenous Metabolite

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189744-94-3

353.29

C17H22Cl2N4

>98% (HPLC)

In Vitro:?H2O : 100 mg/mL (283.05 mM)

Cl.Cl.Cc1ncc(CN2CCC(=CC2)c2ccccc2)c(N)n1

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(-20℃)

With Ice Pack

≥ 2 years