CGP 55845 hydrochloride
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
IC50: 5 nM
CGP 55845是一种强效的和选择性的GABAB受体拮抗剂,消除激动剂结合(pKi = 8.35)并阻断GABA和谷氨酸释放(pEC50值分别为8.08和7.85)。CGP 55845防止GABAB应答巴氯芬(在异丙肾上腺素测定中,IC50 = 130 nM),并增加体外对葡萄糖的低血糖反应。 [1,2]
突触前GABAB受体似乎调节若干神经递质的释放。GABAB受体激动剂巴氯芬,通过自身受体防止GABA本身的释放,拮抗(-)巴氯芬对GABA释放的抑制作用和生长抑素样免疫反应(SRIF-LI)比对谷氨酸的拮抗作用强效10倍以上。然而,CGP 35348在预防巴氯芬对谷氨酸和SRIF-LI的作用比对GABA释放作用强效约70倍。
体外:存在CNQX和d(2)-2-amino-5-phosphonovaleric acid时,GABAB受体的拮抗剂CGP 55845 A阻止抑制性突触后电位-B和双脉冲抑郁。[3]。
这种分泌对镉敏感,通过CGP 55845增效,并被酮色林阻断。汇总这些数据表明,CB受体作为直接葡萄糖传感器,低血糖的处理利用与缺氧类似的神经递质和神经调节机制[4]。惊厥4-氨基吡啶(4-AP)和GABAB受体拮抗剂CGP 55845都应用于成年豚鼠海马切片,导致引发巨大的GABA介导的突触后电位(GPSPs)和痫样放电。[5]。
体内:目前尚未进行体内研究。
临床试验:目前尚未进行临床研究。
参考文献:
[1] Waldmeier PC, Wicki P, Feldtrauer JJ, Mickel SJ, Bittiger H, Baumann PA. GABA and glutamate release affected by GABAB receptor antagonists with similar potency: no evidence for pharmacologically different presynaptic receptors. Br J Pharmacol. 1994 Dec;113(4):1515-21.
[2] Cunningham MD, Enna SJ. Evidence for pharmacologically distinct GABAB receptors associated with cAMP production in rat brain. Brain Res. 1996 May 13;720(1-2):220-4.
[3] Deisz RA. The GABA(B) receptor antagonist CGP 55845A reduces presynaptic GABA(B) actions in neocortical neurons of the rat in vitro. Neuroscience. 1999;93(4):1241-9.
[4] Zhang M, Buttigieg J, Nurse CA. Neurotransmitter mechanisms mediating low-glucose signalling in cocultures and fresh tissue slices of rat carotid body. J Physiol. 2007 Feb 1;578(Pt 3):735-50. Epub 2006 Nov 23.
[5] Salah A, Perkins KL. Effects of subtype-selective group I mGluR antagonists on synchronous activity induced by 4-aminopyridine/CGP 55845 in adult guinea pig hippocampal slices. Neuropharmacology. 2008 Jul;55(1):47-54. doi: 10.1016/j.neuropharm.2008.04.010. Epub 2008 Apr 23.
Physical Appearance | White solid |
Storage | Store at RT |
M.Wt | 438.71 |
Cas No. | 149184-22-5 |
Formula | C18H22Cl2NO3P·HCl |
Solubility | <43.87mg/ml in DMSO |
Chemical Name | benzyl((S)-3-(((S)-1-(3,4-dichlorophenyl)ethyl)amino)-2-hydroxypropyl)phosphinic acid hydrochloride |
SDF | Download SDF |
Canonical SMILES | C[C@@](NC[C@@](O)([H])CP(CC1=CC=CC=C1)(O)=O)([H])C2=CC(Cl)=C(Cl)C=C2.Cl |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |