Dopamine D4 receptor antagonist-1

• 常用名: Dopamine D4 receptor antagonist-1
• 英文名: Dopamine D4 receptor antagonist-1
• CAS号: 444724-92-9
• 分子量: 326.82
• 密度: N/A
• 沸点: N/A
• 分子式: C₁₈H₁₉ClN₄
• 熔点: N/A
• 闪点: N/A

Dopamine D4 receptor antagonist-1用途

多巴胺D4受体拮抗剂-1是一种选择性DRD4拮抗剂,Hd4.2的Ki为9.0nM。多巴胺D4R拮抗剂-1可用于精神分裂症的研究[1]。

Dopamine D4 receptor antagonist-1名称

• 英文名: Dopamine D4 receptor antagonist-1

Dopamine D4 receptor antagonist-1生物活性

• 描述: 多巴胺D4受体拮抗剂-1是一种选择性DRD4拮抗剂,Hd4.2的Ki为9.0nM。多巴胺D4R拮抗剂-1可用于精神分裂症的研究[1]。
• 相关类别:
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> 多巴胺受体
  信号通路 >> 神经信号通路 >> 多巴胺受体
  研究领域 >> 神经疾病
• 体内研究: 多巴胺D4受体拮抗剂-1(10 mg/kg；i.p.；单一)对儿茶酚胺能系统(海马中多巴胺累积)具有抑制作用[1]。动物模型：雄性Long Evans大鼠(180-250 g)；敲除DA D4受体基因座小鼠(D4 KO)；野生型大鼠(WT)[1]。剂量：10 mg/kg给药：腹腔内注射,单次。结果：多巴胺(DOPA)在海马的蓄积增加,纹状体无明显影响。
• 参考文献:

  [1]. Pugsley TA, et al. The discovery of PD 89211 and related compounds: selective dopamine D4 receptor antagonists. Prog Neuropsychopharmacol Biol Psychiatry. 2002 Feb;26(2):219-26.

Dopamine D4 receptor antagonist-1物理化学性质

• 分子式: C₁₈H₁₉ClN₄
• 分子量: 326.82
• InChIKey: BRLVOVGBNYPHBQ-UHFFFAOYSA-N
• SMILES: Clc1cccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)c1

Dopamine D4 receptor antagonist-1靶点实验

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实验名称：Binding affinity against human Dopamine receptor D2 using [3H]spiperone as radioligan... 来源：ChEMBL 靶标：D(2) dopamine receptor External Id：CHEMBL672347

实验名称：Effective concentration against human D4 receptor; NA = Not applicable 来源：ChEMBL 靶标：D(4) dopamine receptor External Id：CHEMBL673644

实验名称：Selectivity ratio of D2 receptor to that of D4 receptor 来源：ChEMBL 靶标：Dopamine receptors; D2 & D4 External Id：CHEMBL848004

实验名称：Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement. 来源：ChEMBL 靶标：D(4) dopamine receptor External Id：CHEMBL674046

实验名称：D4 efficacy was measured using recombinant human D4 receptor expressed in HEK293 cell... 来源：ChEMBL 靶标：D(4) dopamine receptor External Id：CHEMBL673650

实验名称：Cell-based high throughput primary assay to identify activators of GPR151 来源：The Scripps Research Institute Molecular Screening Center 靶标：RecName: Full=G-protein coupled receptor 151; AltName: Full=G-protein coupled receptor PGR7; AltName: Full=GPCR-2037; AltName: Full=Galanin receptor 4; AltName: Full=Galanin-receptor-like protein; Short=GalRL External Id：GPR151_PHUNTER_AG_LUMI_1536_1X%ACT

实验名称：AlphaScreen-based biochemical high throughput primary assay to identify activators of... 来源：The Scripps Research Institute Molecular Screening Center 靶标：N/A External Id：FBW7_ACT_ALPHA_1536_1X%ACT PRUN

实验名称：AlphaScreen-based biochemical high throughput primary assay to identify inhibitors of... 来源：The Scripps Research Institute Molecular Screening Center External Id：MITF_INH_Alpha_1536_1X%INH PRUN

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