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Submit ReviewCGP 46381 is a brain penetrant, selective GABAB receptor antagonist (IC50 = 4.9 μM).
Sold with the permission of Novartis Pharma AG
分子量 | 219.26 |
公式 | C10H22NO2P |
储存 | Store at RT |
CAS Number | 123691-14-5 |
PubChem ID | 130022 |
InChI Key | XOESDNIUAWGCLU-UHFFFAOYSA-N |
Smiles | NCCCP(CC1CCCCC1)(O)=O |
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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
water | 21.93 | 100 |
以下数据基于产品分子量 219.26。 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.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 4.56 mL | 22.8 mL | 45.61 mL |
5 mM | 0.91 mL | 4.56 mL | 9.12 mL |
10 mM | 0.46 mL | 2.28 mL | 4.56 mL |
50 mM | 0.09 mL | 0.46 mL | 0.91 mL |
参考文献是支持产品生物活性的出版物。
Curtis and Lacey (1998) Prolonged GABAB receptor-mediated synaptic inhibition in the cat spinal cord: an in vivo study. Exp.Brain Res. 121 319 PMID: 9746138
Staubli et al (1999) GABAB receptor antagonism: facilitatory effects on memory parallel those on LTP induced by TBS but not HFS. J.Neurosci. 19 4609 PMID: 10341258
Lingenhoehl and Olpe (1993) Blockade of the late inhibitory postsynaptic potential in vivo by the GABAB antagonist CGP 46381. Pharmacol.Comm. 3 49
Froestl et al (1996) Potent, orally active GABAB receptor antagonists. Pharmacol.Rev.Comm. 8 127
If you know of a relevant reference for CGP 46381, please let us know.
关键词: CGP 46381, CGP 46381 supplier, Brain, penetrant, selective, GABAB, antagonist, Receptors, CGP46381, 1247, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 CGP 46381 的部分引用包括:
Lee and Sherman (2012) Intrinsic modulators of auditory thalamocortical transmission. Hear Res 287 43 PMID: 22726616
Cheng et al (2015) GABAB receptor antagonist CGP46381 inhibits form-deprivation myopia development in guinea pigs. Front Cell Neurosci 2015 207312 PMID: 25649745
Pacey et al (2011) Subchronic administration and combination metabotropic glutamate and GABAB receptor drug therapy in fragile X syndrome. Biomed Res Int 338 897 PMID: 21636656
Oberlander (2016) 17β-OE Acutely Potentiates Glutamatergic Synaptic Transmission in the Hippocampus through Distinct Mechanisms in Males and Females. J Neurosci 36 2677 PMID: 26937008
Costa et al (2008) Electrophysiology and pharmacology of striatal neuronal dysfunction induced by mitochondrial complex I inhibition. J Neurosci 28 8040 PMID: 18685029
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意,Tocris 仅会向正规科研企业/机构地址发送文献。
Written by Ian Martin, Norman Bowery and Susan Dunn, this review provides a history of the GABA receptor, as well as discussing the structure and function of the various subtypes and the clinical potential of receptor modulators; compounds available from Tocris are listed.
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