Ro 10-5824 dihydrochloride |
カタログ番号GC12428 |
Ro 10-5824 二塩酸塩は、Ki が 5.2 nM の選択的ドーパミン D4 受容体部分アゴニストです。
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Cas No.: 189744-94-3
Sample solution is provided at 25 µL, 10mM.
Ro 10-5824 dihydrochloride is a selective dopamine D4 receptor partial agonist, with Ki of 5.2 nM.
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[2].
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].
References:
[1]. Nakazawa S, et al. Behavioral and neurophysiological effects of Ro 10-5824, a dopamine D4 receptor partial agonist, in common marmosets. Psychopharmacology (Berl). 2015 Sep;232(17):3287-95.
[2]. Powell SB, et al. RO-10-5824 is a selective dopamine D4 receptor agonist that increases novel object exploration in C57 mice. Neuropharmacology. 2003 Mar;44(4):473-81.
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