质量水平
检测方案
≥98% (HPLC)
形式
powder
颜色
white to beige
溶解性
DMSO: 10 mg/mL, clear
储存温度
−20°C
SMILES字符串
C[C@]12[C@H](NC(C3=NN(CC4=CC=C(C)C=C4)C(C5=CC=C(Cl)C(C)=C5)=C3)=O)C(C)(C)[C@@H](C2)CC1
InChI
1S/C29H34ClN3O/c1-18-6-8-20(9-7-18)17-33-25(21-10-11-23(30)19(2)14-21)15-24(32-33)26(34)31-27-28(3,4)22-12-13-29(27,5)16-22/h6-11,14-15,22,27H,12-13,16-17H2,1-5H3,(H,31,34)/t22-,27-,29+/m1/s1
InChI key
SUGVYNSRNKFXQM-XRHWURSXSA-N
应用
SR144528 has been used as a cannabinoid CB2 receptor antagonist:
- to study its blocking effect on the anti-dyskinetic functionality of HU-308
- to study its effects on spontaneous excitatory postsynaptic currents (sEPSCs) from the globus pallidus neurons
- to analyze its effect on the gastric emptying in rats
生化/生理作用
SR144528 is a potent and highly selective cannabinoid CB2 receptor inverse agonist. SR144528 exhibited a Ki of 0.6 nM at CB2 compared to 400 nM at the related CB1 receptor.
WGK
WGK 3
I Freiman et al.
Neuroscience, 133(1), 305-313 (2005-05-17)
The globus pallidus receives its major glutamatergic input from the subthalamic nucleus and subthalamic nucleus neurons synthesize CB1 cannabinoid receptors. The hypothesis of the present work was that CB1 receptors are localized in terminals of subthalamo-pallidal glutamatergic axons and that
Qiang Tan et al.
Brain research, 1654(Pt A), 24-33 (2016-10-23)
Fibrosis in ventricular system has a role in hydrocephalus following intraventricular hemorrhage (IVH). The cannabinoid receptor 2 (CB2) has been reported to participate in alleviating the fibrosis process of many diseases. However, its role in fibrosis after IVH was unclear
M Rinaldi-Carmona et al.
The Journal of pharmacology and experimental therapeutics, 284(2), 644-650 (1998-03-07)
Based on both binding and functional data, this study introduces SR 144528 as the first, highly potent, selective and orally active antagonist for the CB2 receptor. This compound which displays subnanomolar affinity (Ki = 0.6 nM) for both the rat
A A Izzo et al.
Naunyn-Schmiedeberg's archives of pharmacology, 360(2), 221-223 (1999-09-24)
We have studied the effect of WIN 55,212-2 (a psychoactive cannabinoid agonist), cannabinol (a nonpsychoactive cannabinoid agonist), SR141716A, a cannabinoid CB1 antagonist, and SR144528, a cannabinoid CB2 antagonist, on gastric emptying in the rat. WIN 55,212-2 (0.1-5 mg/kg, i.p.) and
Peggy Rentsch et al.
Neurobiology of disease, 134, 104646-104646 (2019-11-02)
L-dopa induced dyskinesia (LID) is a debilitating side-effect of the primary treatment used in Parkinson's disease (PD), l-dopa. Here we investigate the effect of HU-308, a cannabinoid CB2 receptor agonist, on LIDs. Utilizing a mouse model of PD and LIDs
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