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Submit ReviewRX 821002 hydrochloride is a potent, selective α2-adrenoceptor antagonist with very low affinity for imidazoline sites. Displays selectivity for the α2D over the α2A subtypes (pKd values are 9.7 and 8.2 respectively).
RX 821002 hydrochloride is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 270.72 |
公式 | C12H14N2O3.HCl |
储存 | Desiccate at RT |
纯度 | ≥99% (HPLC) |
CAS Number | 109544-45-8 |
PubChem ID | 11957683 |
InChI Key | IMPOOMVZVWKSAP-UHFFFAOYSA-N |
Smiles | Cl.COC1(COC2=CC=CC=C2O1)C1=NCCN1 |
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 | 100 | ||
DMSO | 27.07 | 100 |
以下数据基于产品分子量 270.72。 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 | 3.69 mL | 18.47 mL | 36.94 mL |
5 mM | 0.74 mL | 3.69 mL | 7.39 mL |
10 mM | 0.37 mL | 1.85 mL | 3.69 mL |
50 mM | 0.07 mL | 0.37 mL | 0.74 mL |
参考文献是支持产品生物活性的出版物。
Erdbrugger et al (1995) Does [3H]2-methoxy-idazoxan (RX 821002) detect more alpha-2-adrenoceptor agonist high-affinity sites than [3H]rauwolscine? A comparison of nine tissues and cell lines. J.Pharmacol.Exp.Ther. 273 1287 PMID: 7791100
O'Rourke et al (1994) Characterisation of [3H]RX 821002 binding to alpha-2 adrenergic receptor subtypes. J.Pharmacol.Exp.Ther. 268 1362 PMID: 7908054
Trendelenburg et al (1996) Antagonists that differentiate between α2A- and α2D-adrenoceptors. Naunyn Schmiedebergs Arch.Pharmacol. 353 245 PMID: 8692278
If you know of a relevant reference for RX 821002 hydrochloride, please let us know.
关键词: RX 821002 hydrochloride, RX 821002 hydrochloride supplier, Potent, selective, α2D-adrenoceptor, alpha2D-adrenoceptor, a2d-adrenoceptor, α2d-adrenergic, alpha2d-adrenergic, a2d-adrenergic, antagonists, Receptors, RX821002, hydrochloride, Adrenergic, Alpha-2, 1324, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 RX 821002 hydrochloride 的部分引用包括:
Hott et al (2012) Both α1- and β1-adrenoceptors in the bed nucleus of the stria terminalis are involved in the expression of conditioned contextual fear. Br J Pharmacol 167 207 PMID: 22506532
Deupree et al (2008) Alpha-2 adrenergic-induced changes in rectal temperature in adult and 13-day old rats following acute and repeated desipr. administration. BMC Pharmacol 8 17 PMID: 18831759
Crestani et al (2008) Both alpha1 and alpha2-adrenoceptors mediate the cardiovascular responses to noradrenaline microinjected into the bed nucleus of the stria terminal of rats. Br J Pharmacol 153 583 PMID: 18037912
Alves et al (2014) Both α1- and α2-adrenoceptors in the insular cortex are involved in the cardiovascular responses to acute restraint stress in rats. J Chem Biol 9 e83900 PMID: 24404141
Uchański et al (2019) An improved yeast surface display platform for the screening of nanobody immune libraries. Sci Rep 9 382 PMID: 30674983
Li et al (2017) Pericytes impair capillary blood flow and motor function after chronic spinal cord injury. Nat Med 23 733 PMID: 28459438
Staedtke et al (2018) Disruption of a self-amplifying catecholamine loop reduces cytokine release syndrome. Nature 564 273 PMID: 30542164
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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。
Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.
Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.