CGP 55845 hydrochloride

Pricing Availability   Qty
说明: Potent and selective GABAB antagonist
化学名: (2S)-3-[[(1S)-1-(3,4-Dichlorophenyl)ethyl]amino-2-hydroxypropyl](phenylmethyl)phosphinic acid hydrochloride
纯度: ≥98% (HPLC)
说明书
引用文献 (105)
评论 (2)
文献 (2)

生物活性 for CGP 55845 hydrochloride

CGP 55845 hydrochloride is a potent, selective GABAB receptor antagonist (IC50 = 5 nM) that prevents agonist binding (pKi = 8.35) and inhibits GABA and glutamate release (pEC50 values are 8.08 and 7.85 respectively). Inhibits GABAB responses to baclofen (IC50 = 130 nM in an isoproterenol assay) and potentiates the hypoglycemic response to glucose in vitro.

许可信息

Sold with the permission of Novartis Pharma AG

化合物库 for CGP 55845 hydrochloride

CGP 55845 hydrochloride is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。

技术数据 for CGP 55845 hydrochloride

分子量 438.71
公式 C18H22Cl2NO3P.HCl
储存 Store at RT
纯度 ≥98% (HPLC)
CAS Number 149184-22-5
PubChem ID 5311042
InChI Key ZODSPDOOCZZEIM-BBRMVZONSA-N
Smiles Cl.C[C@H](NC[C@H](O)CP(O)(=O)CC1=CC=CC=C1)C1=CC=C(Cl)C(Cl)=C1

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for CGP 55845 hydrochloride

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 43.87 100 温和加热

制备储备液 for CGP 55845 hydrochloride

以下数据基于产品分子量 438.71。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

选择批次从而根据批次分子量重新计算:
浓度/溶剂体积/质量 1 mg 5 mg 10 mg
1 mM 2.28 mL 11.4 mL 22.79 mL
5 mM 0.46 mL 2.28 mL 4.56 mL
10 mM 0.23 mL 1.14 mL 2.28 mL
50 mM 0.05 mL 0.23 mL 0.46 mL

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产品说明书 for CGP 55845 hydrochloride

分析证书/产品说明书
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参考文献 for CGP 55845 hydrochloride

参考文献是支持产品生物活性的出版物。

Cunninghan and Enna (1996) Evidence for pharmacologically distinct GABAB receptors associated with cAMP production in rat brain. Brain Res. 720 220 PMID: 8782915

Deisz (1999) The GABAB antagonist CGP 55845A reduces presynaptic GABA1 actions in neurons of the rat in vitro. Neuroscience 93 1241 PMID: 10501448

Salah and Perkins (2008) Effects of subtype-selective group I mGluR antagonists on synchronous activity induced by 4-aminopyridine/CGP 55845 in adult guinea pig hippocampal slices. Neuropharmacology 55 47 PMID: 18538357

Waldmeier et al (1994) GABA and glutamate release affected by GABAB receptor antagonists with similar potency: no evidence for pharmacologically different presynaptic receptors. Br.J.Pharmacol. 113 1515 PMID: 7889310

Zhang et al (2007) Neurotransmitter mechanisms mediating low-glucose signalling in cocultures and fresh tissue slices of rat carotid body. J.Physiol. 578 735 PMID: 17124268

Froestl et al (1996) Potent, orally active GABAB receptor antagonists. Pharmacol.Rev.Comm. 8 127


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关键词: CGP 55845 hydrochloride, CGP 55845 hydrochloride supplier, Potent, selective, GABAB, antagonists, Receptors, CGP55845, hydrochloride, 1248, Tocris Bioscience

105 篇 CGP 55845 hydrochloride 的引用文献

引用文献是使用了 Tocris 产品的出版物。 CGP 55845 hydrochloride 的部分引用包括:

Wu et al (2013) Ovarian hormone loss impairs excitatory synaptic transmission at hippocampal CA3-CA1 synapses. J Neurosci 33 16158 PMID: 24107948

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Zhu et al (2012) Persistent inflammation increases GABA-induced depolarization of rat cutaneous dorsal root ganglion neurons in vitro. Neurobiol Dis 220 330 PMID: 22728089

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Darbin and Wichmann (2008) Effects of striatal GABA A-receptor blockade on striatal and cortical activity in monkeys. J Neurophysiol 99 1294 PMID: 18216224

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Muralidhar et al (2014) Synaptic and cellular organization of layer 1 of the developing rat somatosensory cortex. Front Neuroanat 7 52 PMID: 24474905

Kramer et al (2014) Inhibitory glycinergic neurotransmission in the mammalian auditory brainstem upon prolonged stimulation: short-term plasticity and synaptic reliability. Front Neural Circuits 8 14 PMID: 24653676

Toader et al (2013) Dentate gyrus network dysfunctions precede the symptomatic phase in a genetic mouse model of seizures. Nat Commun 7 138 PMID: 24009558

Medrihan et al (2013) Synapsin II desynchronizes neurotransmitter release at inhibitory synapses by interacting with presynaptic calcium channels. Proc Natl Acad Sci U S A 4 1512 PMID: 23443540

Zhu et al (2011) Suppression of PKR promotes network excitability and enhanced cognition by IF.-γ-mediated disinhibition. Cell 147 1384 PMID: 22153080

Zschenderlein et al (2011) Capsaicin-induced changes in LTP in the lateral amygdala are mediated by TRPV1. PLoS One 6 e16116 PMID: 21249195

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Wei et al (2011) Diffuse and specific tectopulvinar terminals in the tree shrew: synapses, synapsins, and synaptic potentials. PLoS One 6 e23781 PMID: 21858222

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Shen et al (2008) Dichotomous DArgic control of striatal synaptic plasticity. Science 321 848 PMID: 18687967

Jüngling et al (2008) Neuropeptide S-mediated control of fear expression and extinction: role of intercalated GABAergic neurons in the amygdala. Neuron 59 298 PMID: 18667157

Atherton et al (2008) Autonomous initiation and propagation of action potentials in neurons of the subthalamic nucleus. J Physiol 586 5679 PMID: 18832425

Namikawa et al (2018) Salicylate-Induced Suppression of Electrically Driven Activity in Brain Slices from the Auditory Cortex of Aging Mice. Front Aging Neurosci 9 395 PMID: 29311894

Morel et al (2018) JIP1-Mediated JNK Activation Negatively Regulates Synaptic Plasticity and Spatial Memory. J Neurosci 38 3708 PMID: 29540552

Wang et al (2014) GABAB receptors expressed in human aortic endothelial cells mediate intracellular calcium concentration regulation and endothelial nitric oxide synthase translocation. J Cereb Blood Flow Metab 2014 871735 PMID: 25114926

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CGP-55845 increases field potential amplitudes in cortex tissue.
By Anonymous on 06/07/2019
分析类型: Ex Vivo
种属: Rat
细胞系/组织: Anterior cingulate cortex

CGP-55845 was used to study input of GABA-B receptors into field potential generation in anterior cingulate cortex. Application of 10 nM CGP-55845 increased significantly amplitudes of field potentials and reduced their paired-pulse ratio.

Should be sonicated when dissolved.

PMID: 15936838
review image

CGP55845 reverses Baclofen effects on dopamine release..
By Anonymous on 03/28/2018
分析类型: Ex Vivo
种属: Mouse

Effects of GABAB activation on electrically stimulated dopamine release in the striatum was measured using fast scan cyclic votlammetry. CGP55845 (200nM) nicely reverse Baclofen (30uM) effects on dopamine release.

We typically make a 10mM stock solution in DMSO. Drug seems pretty stable.

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