GR 103691 | Dopamine D3 Receptor Antagonist | AmBeed-信号通路专用抑制剂

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GR 103691 {[allProObj[0].p_purity_real_show]}

货号：A819643

GR 103691 is an effective and selective receptor antagonist of the dopamine D3 receptor (D3DR).

GR 103691 化学结构
CAS号：162408-66-4

GR 103691 3D分子结构
CAS号：162408-66-4

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GR 103691 纯度/质量文件产品仅供科研

货号：A819643 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Cell, 2024, 101755. Ambeed. [ A399663 ]; • EMBO J., 2024. Ambeed. [ A295334 ]; • JMC, 2024, 67(20): 18265-18289. Ambeed. [ A538667 , A341145 , A117430 , A172297 ]; • JMC, 2024. Ambeed. [ A210558 , A1518164 ]; • Cell Death Discov., 2024, 10, 436. Ambeed. [ A384235 ]; 更多 >

多巴胺受体亚型比较

产品名称	D1 receptor ↓ ↑	D2 receptor ↓ ↑	D3 receptor ↓ ↑	D4 receptor ↓ ↑	D5 receptor ↓ ↑	DAT ↓ ↑	Dopamine receptor ↓ ↑	其他靶点	纯度
Penfluridol	+ Dopamine receptor, Ki: 1.6 μM								98%
Ansofaxine HCl	++ Dopamine receptor, IC50: 491 nM								98%
Tetrahydroberberine,THB		+ D2 receptor, pKi: 6.08							98+%
Prochlorperazine Maleate		✔							95%
Olanzapine		✔							99+%
Trifluoperazine		++++ Dopamine D2 receptor, IC50: 1.1 nM							98%
Ropinirole hydrochloride		++ D2 receptor, Ki: 29 nM							99%
Lurasidone		++++ D2 receptor, Ki: 1 nM							98%
Levosulpiride		✔							99+%
Pridopidine		✔							95%
Metoclopramide		✔					✔		99+%
Molindone HCl		✔							98%
Sulpiride		✔							99+%
Perospirone		++++ D2 receptor, Ki: 1.4 nM							99%
Perospirone HCl		++++ D2 receptor, Ki: 1.4 nM							98+%
Phenothiazine		✔							98%
Pimozide	+ Dopamine D1 receptor, Ki: 6600 nM	+++ Dopamine D2 receptor, Ki: 3.0 nM	++++ Dopamine D3 receptor, Ki: 0.83 nM						98%
Rotundine	++ D1 receptor, IC50: 166 nM	+ D2 receptor, IC50: 1.47 μM	+ D3 receptor, IC50: 3.25 μM						98%
Domperidone		✔							99+%
ONC206		✔							97%
Pimethixene maleate	++ Dopamine D1 Receptor, pKi: 6.37	+++ Dopamine D2 Receptor, pKi: 8.19		++ Dopamine D4.4 Receptor, pKi: 7.54					97%
Loxapine succinate	++ D2 receptor (Human), Ki: 62 nM D1 receptor (human), Ki: 26 nM	++ D2 receptor (bovine), Ki: 26 nM D2 receptor (human), Ki: 24 nM		+++ D4 receptor (human), Ki: 7.5 nM					99%
Chlorprothixene	+++ D1 receptor, Ki: 18 nM	+++ D2 receptor, Ki: 2.96 nM	+++ D3 receptor, Ki: 4.56 nM		+++ D5 receptor, Ki: 9 nM				98%
SCH-23390 HCl	++++ D1 dopamine receptor, Ki: 0.2 nM				++++ D5 dopamine receptor, Ki: 0.3 nM				98%
MPP+ iodide						✔			97%
σ1 Receptor antagonist-1						+ DAT, pKi: 5.8			97%
Benztropine mesylate						++ DAT, IC50: 118 nM			98%
Azaperone							✔		98%
Ziprasidone HCl							✔		98+%
Paliperidone							✔		98%
Alizapride HCl							✔		99+%
Amisulpride							✔		98%
Quetiapine hemifumarate							✔	Adrenergic Receptor	98%
Clozapine N-oxide							✔		99%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

GR 103691 生物活性

描述

GR 103691 is a potent, selective dopamine D3 receptor antagonist with a Ki value of 0.4 nM. GR 103691 shows more than 100-fold selectivity for human dopamine human (h)D3 over hD4 and hD1 sites. GR 103691 shows marked affinity for serotonin1A (5-HT1A) receptors (Ki of 5.8 nM) and α-1 adrenoceptors (Ki of 12.6 nM)^[1]. The D(3) antagonist GR 103691 (10 nM) significantly decreased dopamine uptake. D(3) receptor activation increases dopamine uptake in the nucleus accumbens and suggest that this receptor subtype can regulate extracellular dopamine by modulating the DA transporter activity^[2]. Low dopamine levels (1 mM) decreased the monosynaptic "stretch" reflex (MSR) amplitude in WT animals and increased it in D3KO animals. Higher dopamine concentrations (10-100 mM) decreased MSR amplitudes in both groups, but always more strongly in WT. GR 103691 and nafadotride increased the MSR (monosynaptic "stretch" reflex) in WT but not in D3KO (D3-receptor knock-out) mice^[3].

GR 103691 参考文献

[1]Audinot V, Newman-Tancredi A, Gobert A, Rivet JM, Brocco M, Lejeune F, Gluck L, Desposte I, Bervoets K, Dekeyne A, Millan MJ. A comparative in vitro and in vivo pharmacological characterization of the novel dopamine D3 receptor antagonists (+)-S 14297, nafadotride, GR 103,691 and U 99194. J Pharmacol Exp Ther. 1998 Oct;287(1):187-97

[2]Zapata A, Shippenberg TS. D(3) receptor ligands modulate extracellular dopamine clearance in the nucleus accumbens. J Neurochem. 2002 Jun;81(5):1035-42

[3]Clemens S, Hochman S. Conversion of the modulatory actions of dopamine on spinal reflexes from depression to facilitation in D3 receptor knock-out mice. J Neurosci. 2004 Dec 15;24(50):11337-45

[4]Zapata A, Shippenberg TS. D(3) receptor ligands modulate extracellular dopamine clearance in the nucleus accumbens. J Neurochem. 2002 Jun;81(5):1035-42

[5]Clemens S, Hochman S. Conversion of the modulatory actions of dopamine on spinal reflexes from depression to facilitation in D3 receptor knock-out mice. J Neurosci. 2004 Dec 15;24(50):11337-45

GR 103691 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.06mL

0.41mL

0.21mL

10.30mL

2.06mL

1.03mL

20.59mL

4.12mL

2.06mL

GR 103691 技术信息

CAS号	162408-66-4
分子式	C₃₀H₃₅N₃O₃
分子量	485.617

别名
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C

溶解度

DMSO: 4 mg/mL(8.24 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验配方

GR 103691 {[allProObj[0].p_purity_real_show]}

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GR 103691 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

GR 103691 质控信息

GR 103691 生物活性

GR 103691 参考文献

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GR 103691 技术信息

最近浏览的产品

大规格询价

摩尔计算器

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总药量计算器

工作液计算器

细胞研究

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