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Submit ReviewDihydro-β-erythroidine hydrobromide
说明： α4β2, muscle type and Torpedo nAChR antagonist
别名： DHβE
化学名： (2S,13bS)-2-Methoxy-2,3,5,6,8,9,10,13-octahydro-1H,12H-benzo[i]pyrano[3,4-g]indolizin-12-one hydrobromide
纯度： ≥98% (HPLC)
生物活性 for Dihydro-β-erythroidine hydrobromide
Dihydro-β-erythroidine hydrobromide is a member of the Erythrina alkaloids, it is a competitive nicotinic acetylcholine receptor antagonist with moderate selectivity for the neuronal α4 receptor subunit (IC50 values are 0.19 and 0.37 μM for α4β4 and α4β2 receptors, respectively). Antagonizes behavioral effects of nicotine in vivo. Dihydro-β-erythroidine blocks excitation of striatal GABAergic neurons, which completely suppress polysynaptic inhibition between striatal cholinergic interneurons. Dihydro-β-erythroidine hydrobromide has antidepressive-like effects in mice (forced swim and mouse suspension). Orally bioavailable.
化合物库 for Dihydro-β-erythroidine hydrobromide
Dihydro-b-erythroidine hydrobromide 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 Dihydro-β-erythroidine hydrobromide
| 分子量 | 356.26 |
| 公式 | C16H21NO3.HBr |
| 储存 | Desiccate at RT |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 29734-68-7 |
| PubChem ID | 11957537 |
| InChI Key | GFIGWAJEIMHJJB-LINSIKMZSA-N |
| Smiles | Br.CO[C@H]1CC=C2CCN3CCC4=C(CC(=O)OC4)[C@]23C1 |
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 Dihydro-β-erythroidine hydrobromide
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| water | 35.63 | 100 | |
| DMSO | 8.91 | 25 |
制备储备液 for Dihydro-β-erythroidine hydrobromide
以下数据基于产品分子量 356.26。 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 | 2.81 mL | 14.03 mL | 28.07 mL |
| 5 mM | 0.56 mL | 2.81 mL | 5.61 mL |
| 10 mM | 0.28 mL | 1.4 mL | 2.81 mL |
| 50 mM | 0.06 mL | 0.28 mL | 0.56 mL |
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产品说明书 for Dihydro-β-erythroidine hydrobromide
参考文献 for Dihydro-β-erythroidine hydrobromide
参考文献是支持产品生物活性的出版物。
Williams and Robinson (1984) Binding of the nicotinic cholinergic antagonist, dihydro-β-erythroidine, to rat brain tissue. J.Neurosci. 4 2906 PMID: 6502210
Damaj et al (1995) In vivo pharmacological effects of dihydro-β-erythroidine, a nicotinic antagonist, in mice. Psychopharmacology 117 67 PMID: 7724704
Harvey et al (1996) Multiple determinants of dihydro-β-erythroidine sensitivity on rat neuronal nicotinic receptor α subunits. J.Neurochem. 67 1953 PMID: 8863500
Sullivan et al (2008) Recurrent Inhibitory Network among Striatal Cholinergic Interneurons. J.Neurosci. 28 8682 PMID: 18753369
Dorst et al (2020) Polysynaptic inhibition between striatal cholinergic interneurons shapes their network activity patterns in a dopamine-dependent manner. Nat.Commun 11 5133 PMID: 33037215
Andreasen et al (2009) Antidepressant-like effects of nicotinic acetylcholine receptor antagonists, but not agonists, in the mouse forced swim and mouse tail suspension tests. J.Psychopharmacol. 23 797 PMID: 18583432
If you know of a relevant reference for Dihydro-β-erythroidine hydrobromide, please let us know.
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关键词: Dihydro-b-erythroidine hydrobromide, Dihydro-b-erythroidine hydrobromide supplier, antagonists, neuronal, alpha4-containing, nicotinic, receptors, α4β2, a4b2, Nicotinic, Receptors, Acetylcholine, nAChR, Non-Selective, Subtypes, Other, Dihydro-beta-erythroidine, hydrobromide, Dihydro-β-erythroidine, DHβE, DHbE, (Other, Subtypes), (a4b2), 2349, Tocris Bioscience
30 篇 Dihydro-β-erythroidine hydrobromide 的引用文献
引用文献是使用了 Tocris 产品的出版物。 Dihydro-β-erythroidine hydrobromide 的部分引用包括：
Platt et al (2012) Striatal DA transmission is subtly modified in human A53Tα-synuclein overexpressing mice. PLoS One 7 e36397 PMID: 22570709
Caiati et al (2012) Developmental regulation of CB1-mediated spike-time dependent depression at immature mossy fiber-CA3 synapses. Sci Rep 2 285 PMID: 22368777
Goddard et al (2012) Gamma oscillations are generated locally in an attention-related midbrain network. Neuron 73 567 PMID: 22325207
Li et al (2010) Cytisine induces autonomic cardiovascular responses via activations of different nicotinic receptors. Auton Neurosci 154 14 PMID: 19887306
Herman et al (2016) A cholinergic basal forebrain feeding circuit modulates appetite suppression Nature 538 253 PMID: 27698417
Mamaligas et al (2016) Nicotinic and opioid receptor regulation of striatal DA D2-receptor mediated transmission Scientific Reports 6 37834 PMID: 27886263
Kunisawa et al (2016) Nicotine evokes kinetic tremor by activating the inferior olive via α7 nicotinic acetylcholine receptors. Behav.Brain Res. 314 173 PMID: 27506652
Huang et al (2019) Neural mechanisms of contextual modulation in the retinal direction selective circuit. Nat Commun 10 2431 PMID: 31160566
Saunders et al (2015) Corelease of acetylcholine and GABA from cholinergic forebrain neurons. J Neurosci 4 PMID: 25723967
Ngolab et al (2015) Functional Upregulation of α4* Nicotinic Acetylcholine Receptors in VTA GABAergic Neurons Increases Sensitivity to Nicotine Reward. J Neurosci 35 8570 PMID: 26041923
Yorgason et al (2015) Greater ethanol inhibition of presynaptic DA release in C57BL/6J than DBA/2J mice: Role of nicotinic acetylcholine receptors. Front Cell Neurosci 284 854 PMID: 25451295
Elgueta et al (2015) Acetylcholine induces GABA release onto rod bipolar cells through heteromeric nicotinic receptors expressed in A17 amacrine cells. PLoS One 9 6 PMID: 25709566
Miguel Angel Garcia-Bereguiain et al (2016) Spontaneous Release Regulates Synaptic Scaling in the Embryonic Spinal Network In Vivo The Journal of Neuroscience 6 7268 PMID: 27383600
Kiss et al (2014) Nicotinic acetylcholine receptors containing the α7-like subunit mediate contractions of muscles responsible for space positioning of the snail, Helix pomatia L. tentacle. PLoS One 9 e109538 PMID: 25303328
Dilger et al (2015) Absence of plateau potentials in dLGN cells leads to a breakdown in retinogeniculate refinement. J Neurosci 35 3652 PMID: 25716863
Stouffer et al (2015) Ins enhances striatal DA release by activating cholinergic interneurons and thereby signals reward. Nat Commun 6 8543 PMID: 26503322
Zhong et al (2013) Nicotine elicits prolonged calcium signaling along ventral hippocampal axons. Pharmacol Res Perspect 8 e82719 PMID: 24349346
Bader and Diener (2015) Novel aspects of cholinergic regulation of colonic ion transport. Elife 3 e00139 PMID: 26236483
Morrie and Feller (2015) An Asymmetric Increase in Inhibitory Synapse Number Underlies the Development of a Direction Selective Circuit in the Retina. Neuroscience 35 9281 PMID: 26109653
Lozovaya et al (2349) GABAergic inhibition in dual-transmission cholinergic and GABAergic striatal interneurons is abolished in Parkinson disease. Nat Commun 9 1422 PMID: 29651049
Zhang et al (2018) Pauses in Cholinergic Interneuron Activity Are Driven by Excitatory Input and Delayed Rectification, with DA Modulation. Neuron 98 918 PMID: 29754751
Li et al (2009) Specific subtypes of nicotinic cholinergic receptors involved in sympathetic and parasympathetic cardiovascular responses. Neurosci Lett 462 20 PMID: 19573576
Dorst et al (2020) Polysynaptic inhibition between striatal cholinergic interneurons shapes their network activity patterns in a dopamine-dependent manner. Nat Commun 11 5113 PMID: 33037215
Assous (2017) Differential processing of thalamic information via distinct striatal interneuron circuits. Nat Commun 8 15860 PMID: 28604688
Kiguchi (2018) Inhibition of peripheral macrophages by nicotinic acetylcholine receptor agonists suppresses spinal microglial activation and neuropathic pain in mice with peripheral nerve injury. J Neuroinflammation 15 96 PMID: 29587798
Kutlu et al (2018) Differential effects of α4β2 nicotinic receptor antagonists and partial-agonists on contextual fear extinction in male C57BL/6 mice. Psychopharmacology (Berl) 235 1211 PMID: 29383396
Brodnik et al (2018) Local GABAA receptor mediated suppression of DA release within the nucleus accumbens. ACS Chem Neurosci 17 1978 PMID: 30253088
Govind et al (2017) Selective and regulated trapping of nicotinic receptor weak base ligands and relevance to smoking cessation. Elife 6 PMID: 28718768
Sternfeld et al (2017) Speed and segmentation control mechanisms characterized in rhythmically-active circuits created from spinal neurons produced from genetically-tagged embryonic stem cells. Elife 6 PMID: 28195039
Jareczek et al (2017) Plasticity in Brainstem Mechanisms of Pain Modulation by Nicotinic Acetylcholine Receptors in the Rat. Eneuro 4 PMID: 28197544
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该领域的文献
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Nicotinic ACh Receptors Scientific Review
Updated in 2014, this review by Sue Wonnacott summarizes the diverse structure and function of nicotinic acetylcholine receptors and gives an in-depth review of the ligands available for nAChR research. Compounds available from Tocris are listed.