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Submit ReviewSKF 97541
说明： Highly potent GABAB agonist; also GABAA-ρ antagonist
别名： CGP 35024
化学名： 3-Aminopropyl(methyl)phosphinic acid
生物活性 for SKF 97541
SKF 97541 is a potent GABAB agonist (EC50 = 50 nM). SKF 97541 depresses striatal synaptic potentials and hyperpolarizes nigral neurons (EC50 values = 92 nM and 150 nM, respectively). SKF 97541 shows antidepressant effects in animal models and is also a GABAA-ρ antagonist.
技术数据 for SKF 97541
| 分子量 | 137.12 |
| 公式 | C4H12NO2P |
| 储存 | Desiccate at RT |
| CAS Number | 127729-35-5 |
| PubChem ID | 5230 |
| InChI Key | NHVRIDDXGZPJTJ-UHFFFAOYSA-N |
| Smiles | NCCCP(O)(C)=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.
溶解性数据 for SKF 97541
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| water | 13.71 | 100 |
制备储备液 for SKF 97541
以下数据基于产品分子量 137.12。 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 | 7.29 mL | 36.46 mL | 72.93 mL |
| 5 mM | 1.46 mL | 7.29 mL | 14.59 mL |
| 10 mM | 0.73 mL | 3.65 mL | 7.29 mL |
| 50 mM | 0.15 mL | 0.73 mL | 1.46 mL |
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产品说明书 for SKF 97541
参考文献 for SKF 97541
参考文献是支持产品生物活性的出版物。
Bon and Galvan (1996) Electrophysiological characterization of GABAB agonists and antagonists in dorso-lateral septal neurones in vitro. Br.J.Pharmacol. 118 961 PMID: 8799569
Froestl et al (1995) Phosphinic acid analogues of GABA. 1. New potent and selective GABAB agonists. J.Med.Chem. 38 3297 PMID: 7650684
Johnston (1996) GABAC receptors: relatively simple transmitter-gated ion channels? TiPS 17 319 PMID: 8885697
Seabrook et al (1990) Electrophysiological characterization of potent agonists and antagonists on pre- and postsynaptic GABAB receptors on neurones in brain slices. Br.J.Pharmacol. 101 949 PMID: 1964824
If you know of a relevant reference for SKF 97541, please let us know.
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关键词: SKF 97541, SKF 97541 supplier, potent, GABAB, agonists, GABAC, antagonists, Receptors, SKF97541, CGP35024, CGP, 35024, GABAA-rho, 0379, Tocris Bioscience
8 篇 SKF 97541 的引用文献
引用文献是使用了 Tocris 产品的出版物。 SKF 97541 的部分引用包括：
Ignell et al (2009) Presynaptic peptidergic modulation of olfactory receptor neurons in Drosophila. Br J Pharmacol 106 13070 PMID: 19625621
Root et al (2008) A presynaptic gain control mechanism fine-tunes olfactory behavior. Neuron 59 311 PMID: 18667158
Chen et al (2008) Differential regulation of mor. antinociceptive effects by endogenous enkephalinergic system in the forebrain of mice. Mol Pain 4 41 PMID: 18826595
Ki and Lim (2019) Sleep-promoting effects of threonine link amino acid metabolism in Drosophila neuron to GABAergic control of sleep drive. Elife 8 PMID: 31313987
Lecat-Guillet (2017) FRET-based sensors unravel activation and allosteric modulation of the GABAB receptor. Cell Chem Biol 24 360 PMID: 28286129
Martelli and Fiala (2019) Slow presynaptic mechanisms that mediate adaptation in the olfactory pathway of Drosophila. Elife 8 PMID: 31169499
Wood et al (2000) The human GABA(B1b) and GABA(B2) heterodimeric recombinant receptor shows low sensitivity to phaclofen and saclofen. Mol Pain 131 1050 PMID: 11082110
Piqueras and Martínez (2004) Peripheral GABAB agonists stimulate gastric acid secretion in mice. Br J Pharmacol 142 1038 PMID: 15210585
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SKF 97541 的评论
平均评分: 4 (Based on 1 Review.)
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Test of potential modulation of 5HT-1B receptor effects.
By
Sergiy Sylantyev on 12/10/2023
分析类型： In Vitro
种属： Mouse
细胞系/组织： Arcuate nucleus
SKF 97541 was used to test a (potential) impact of GABA-B receptors on the effect of 5HT-1B receptors on neurotransmitter vesicle release in interneuronal synapse. Picture: membrane capacitance fluctuation of living neuron after series of electrical stimuli delivered to acute neural tissue. Left: control. Right: activation of GABA-B receptors (with 1 microM SKF 97541), mGlu receptors and ACh receptors do not show a significant effect. Grey traces: individual recordings; red: averaged trace.
该领域的文献
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。
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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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The key feature of drug addiction is the inability to stop using a drug despite clear evidence of harm. This poster describes the brain circuits associated with addiction, and provides an overview of the main classes of addictive drugs and the neurotransmitter systems that they target.