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Dopamine D3 受体激动剂13a是一种Dopamine D3 受体激动剂。该化合物选择性地与Dopamine D3 受体结合,相较于Dopamine D1、D2和D4受体(Kis = 0.14、4,600、2.85和756 nM,分别)具有更高的亲和力,并且还能与血清素(5-HT)受体亚型5-HT1A、5-HT2A、5-HT2B和5-HT2C(Kis = 6、54、1.47和252 nM,分别)结合;然而,它是Dopamine D2受体的部分激动剂(EC50 = 2.26 nM,在G蛋白招募分析中)并且作为Dopamine D3受体的拮抗剂(IC50 = 4.62 nM)。在大鼠身上,当剂量为3 mg/kg时,Dopamine D3 受体激动剂13a能减少可卡因自我给药。
Dopamine D3 受体激动剂13a是一种Dopamine D3 受体激动剂。该化合物选择性地与Dopamine D3 受体结合,相较于Dopamine D1、D2和D4受体(Kis = 0.14、4,600、2.85和756 nM,分别)具有更高的亲和力,并且还能与血清素(5-HT)受体亚型5-HT1A、5-HT2A、5-HT2B和5-HT2C(Kis = 6、54、1.47和252 nM,分别)结合;然而,它是Dopamine D2受体的部分激动剂(EC50 = 2.26 nM,在G蛋白招募分析中)并且作为Dopamine D3受体的拮抗剂(IC50 = 4.62 nM)。在大鼠身上,当剂量为3 mg/kg时,Dopamine D3 受体激动剂13a能减少可卡因自我给药。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 630 | 35日内发货 | |
5 mg | ¥ 2,970 | 35日内发货 | |
10 mg | ¥ 5,630 | 35日内发货 |
产品描述 | Dopamine D3 receptor agonist 13a selectively targets the dopamine D3 receptor over dopamine D1, D2, and D4 receptors, with affinities (Ki values) of 0.14, 4,600, 2.85, and 756 nM, respectively. It also interacts with serotonin (5-HT) receptor subtypes 5-HT1A, 5-HT2A, 5-HT2B, and 5-HT2C, with Ki values of 6, 54, 1.47, and 252 nM, respectively. While acting as a partial agonist at dopamine D2 receptors (EC50 = 2.26 nM in a G protein recruitment assay), it serves as an antagonist at dopamine D3 receptors (IC50 = 4.62 nM). Additionally, Dopamine D3 receptor agonist 13a, at a dose of 3 mg/kg, has been shown to reduce cocaine self-administration in rats. |
分子量 | 442.42 |
分子式 | C22H33Cl2N3O2 |
CAS No. | 2899250-94-1 |
存储 | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度信息 | Ethanol: 3 mg/ml DMF: Soluble |
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