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说明： Selective GABAA-ρ antagonist
化学名： (1,2,5,6-Tetrahydropyridin-4-yl)methylphosphinic acid
纯度： ≥97% (HPLC)
生物活性 for TPMPA
TPMPA is a selective, competitive GABAA-ρ antagonist with only minimal effects on GABAA and GABAB receptors (Kb values are 2.1 μM (antagonist), 320 μM (antagonist) and EC50 ~ 500 μM (weak agonist) respectively). Displays 8-fold selectivity for human recombinant ρ1 receptors over ρ2 receptors.
技术数据 for TPMPA
| 分子量 | 161.14 |
| 公式 | C6H12NO2P |
| 储存 | Store at RT |
| 纯度 | ≥97% (HPLC) |
| CAS Number | 182485-36-5 |
| PubChem ID | 5520 |
| InChI Key | MFUKVPOVVKKLRQ-UHFFFAOYSA-N |
| Smiles | OP(C1=CCNCC1)(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 TPMPA
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| water | 100 |
制备储备液 for TPMPA
以下数据基于产品分子量 161.14。 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 | 6.21 mL | 31.03 mL | 62.06 mL |
| 5 mM | 1.24 mL | 6.21 mL | 12.41 mL |
| 10 mM | 0.62 mL | 3.1 mL | 6.21 mL |
| 50 mM | 0.12 mL | 0.62 mL | 1.24 mL |
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产品说明书 for TPMPA
参考文献 for TPMPA
参考文献是支持产品生物活性的出版物。
Chebib et al (1998) GABAC receptor antagonists differentiate between human r1 and r2 receptors expressed in Xenopus oocytes. Eur.J.Pharmacol. 357 227 PMID: 9797041
Ragozzino et al (1996) Design and in vitro pharmacology of a selective γ-aminobutyric acidc receptor antagonist. Mol.Pharmacol. 50 1024 PMID: 8863850
Xu et al (2009) The involvement of GABA-C receptors in paired pulse depression of inhibitory postsynaptic currents in rat hippocampal CA1 pyramidal neurons. Exp.Neurol. 216 243 PMID: 19100735
Murata et al (1996) The first selective antagonist for a GABAc receptor. Bioorg.Med.Chem.Lett. 6 2073
If you know of a relevant reference for TPMPA, please let us know.
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关键词: TPMPA, TPMPA supplier, Selective, GABAC, antagonists, Receptors, GABAA-rho, GABAA-ρ, GABA-A, 1040, Tocris Bioscience
12 篇 TPMPA 的引用文献
引用文献是使用了 Tocris 产品的出版物。 TPMPA 的部分引用包括：
Manookin et al (2018) Neural Mechanisms Mediating Motion Sensitivity in Parasol Ganglion Cells of the Primate Retina. Neuron 97 1327 PMID: 29503188
Vielma et al (2014) Nitric oxide modulates the temporal properties of the glutamate response in type 4 OFF bipolar cells. PLoS One 9 e114330 PMID: 25463389
Jensen (2013) Effects of a metabotropic glutamate 1 receptor antagonist on light responses of retinal ganglion cells in a rat model of retinitis pigmentosa. PLoS One 8 e79126 PMID: 24205371
Lindstrom et al (2010) Retinal input to efferent target amacrine cells in the avian retina. J Neurosci 27 103 PMID: 20650017
Olmos-Serrano et al (2010) Defective GABAergic neurotransmission and pharmacological rescue of neuronal hyperexcitability in the amygdala in a mouse model of fragile X syndrome. Br J Pharmacol 30 9929 PMID: 20660275
Hellmer et al (2018) A group I metabotropic glutamate receptor controls synaptic gain between rods and rod bipolar cells in the mouse retina. Physiol Rep 6 e13885 PMID: 30338673
Antonelli et al (2014) Pin1-dependent signalling negatively affects GABAergic transmission by modulating neuroligin2/gephyrin interaction. Nat Commun 5 5066 PMID: 25297980
Chaffiol et al (2017) DA Regulation of GABAA Receptors Contributes to Light/Dark Modulation of the ON-Cone Bipolar Cell Receptive Field Surround in the Retina. Curr Biol 27 2600 PMID: 28844643
Murphy-Baum and Taylor (2015) The Synaptic and Morphological Basis of Orientation Selectivity in a Polyaxonal Amacrine Cell of the Rabbit Retina. Vis Neurosci 35 13336 PMID: 26424882
Elgueta et al (2015) Acetylcholine induces GABA release onto rod bipolar cells through heteromeric nicotinic receptors expressed in A17 amacrine cells. J Neurosci 9 6 PMID: 25709566
Wood et al (2000) The human GABA(B1b) and GABA(B2) heterodimeric recombinant receptor shows low sensitivity to phaclofen and saclofen. Front Cell Neurosci 131 1050 PMID: 11082110
Gascon et al (2006) GABA regulates dendritic growth by stabilizing lamellipodia in newly generated interneurons of the olfactory bulb. J Neurosci 26 12956 PMID: 17167085
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TPMPA 的评论
平均评分: 5 (Based on 1 Review.)
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Used in inhibitor cocktail.
By
Anonymous on 12/03/2019
分析类型： In Vitro
种属： Rat
细胞系/组织： Retinal rod bipolar cells
Retinal dissections were performed in HEPES-buffered extracellular solution containing inhibitor cocktail50 umol/L
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。
GABA Receptors Scientific Review
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.