Shanghai Nianxing Industrial Co., Ltd
China
Product Name: Ro 10-5824 dihydrochloride
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Purity: 99.0%
Stocking Period: 10 Day
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189744-94-3

189744-94-3 structure

189744-94-3 structure

Name: Ro 10-5824 dihydrochloride
Chemical Name: Ro 10-5824 dihydrochloride
CAS Number: 189744-94-3
Molecular Formula: C₁₇H₂₂Cl₂N₄
Molecular Weight: 353.289
Catalog: Signaling Pathways GPCR/G Protein Dopamine Receptor
Create Date: 2018-01-26 14:28:03
Modify Date: 2024-01-05 10:31:43
Ro 10-5824 dihydrochloride is a selective dopamine D4 receptor partial agonist, with Ki of 5.2 nM.

Name	Ro 10-5824 dihydrochloride
Synonyms	2-Methyl-5-[(4-phenyl-3,6-dihydro-1(2H)-pyridinyl)methyl]-4-pyrimidinamine dihydrochloride 2-Methyl-5-[(4-phenyl-3,6-dihydropyridin-1(2H)-yl)methyl]pyrimidin-4-amine dihydrochloride 4-Pyrimidinamine, 5-[(3,6-dihydro-4-phenyl-1(2H)-pyridinyl)methyl]-2-methyl-, hydrochloride (1:2) Ro 10-5824 (dihydrochloride)

Description	Ro 10-5824 dihydrochloride is a selective dopamine D4 receptor partial agonist, with Ki of 5.2 nM.
Related Catalog	Signaling Pathways >> GPCR/G Protein >> Dopamine Receptor Signaling Pathways >> Neuronal Signaling >> Dopamine Receptor Research Areas >> Others
Target	Ki: 5.2 nM (dopamine D4 receptor)[2]
In Vitro	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].
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].
Animal Admin	In the experiment, 39 C57 and 40 DBA mice are tested over a three-day period. On days 1 and 2, mice are placed into the VT for 60 min and locomotor behavior is recorded. On the third day, mice are placed into the VT chamber for 60 min. Following the 60-min period, mice are removed from the chambers and administered 0, 1.0, 3.0, or 10.0 mg/kg of RO-10-5824 (n=9-11 per group). Mice are assigned to drug group pseudo-randomly, with each dose being represented in a cage of four mice. A novel paper cup measuring 9.5 cm in height and 7.5 cm in diameter at the rim is placed upside down in the center of each open field and secured to the floor with tape. Mice are returned to the VT 10 min following injection and tested for an additional 30 min.
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.

Molecular Formula	C₁₇H₂₂Cl₂N₄
Molecular Weight	353.289
Exact Mass	352.122162
Storage condition	2-8℃