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GR 103691

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Chemical Structure| 162408-66-4 同义名 : -
CAS号 : 162408-66-4
货号 : A819643
分子式 : C30H35N3O3
纯度 : 98+%
分子量 : 485.617
MDL号 : MFCD00936840
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
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：
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].
实验方案
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
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