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Submit ReviewA 61603 hydrobromide
说明： α1A agonist
化学名： N-[5-(4,5-Dihydro-1H-imidazol-2-yl)-2-hydroxy-5,6,7,8-tetrahydronaphthalen-1-yl]methanesulfonamide hydrobromide
生物活性 for A 61603 hydrobromide
A 61603 hydrobromide is a potent α-adrenoceptor agonist that is at least 35-fold more potent at α1A than at α1B or α1D sites. Induces dose response increases in spontaneous Ca2+ transients in rat ventricular myocytes in vitro (EC50 = 6.9 nmol/L).
技术数据 for A 61603 hydrobromide
| 分子量 | 390.29 |
| 公式 | C14H19N3O3S.HBr |
| 储存 | Desiccate at +4°C |
| CAS Number | 107756-30-9 |
| PubChem ID | 9865178 |
| InChI Key | LRFLWCZMTGTUEP-UHFFFAOYSA-N |
| Smiles | Br.CS(=O)(=O)NC1=C(O)C=CC2=C1CCCC2C1=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.
溶解性数据 for A 61603 hydrobromide
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| water | 50 |
制备储备液 for A 61603 hydrobromide
以下数据基于产品分子量 390.29。 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 |
|---|---|---|---|
| 0.5 mM | 5.12 mL | 25.62 mL | 51.24 mL |
| 2.5 mM | 1.02 mL | 5.12 mL | 10.25 mL |
| 5 mM | 0.51 mL | 2.56 mL | 5.12 mL |
| 25 mM | 0.1 mL | 0.51 mL | 1.02 mL |
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产品说明书 for A 61603 hydrobromide
参考文献 for A 61603 hydrobromide
参考文献是支持产品生物活性的出版物。
Knepper et al (1995) A-61603, a potent α1-adrenergic receptor agonist, selective for the α1A receptor subtype. J.Pharmacol.Exp.Ther. 274 97 PMID: 7616455
Luo et al (2007) Receptor subtype involved in α1A-adrenergic receptor-mediated Ca2+ signaling in cardiomyocytes. Acta.Pharmacol.Sin. 28 968 PMID: 17588332
Meyer et al (1996) Synthesis and in vitro characterisation of N-[5-(4,5-dihydro-1H-imidazol-2-yl)-2-hydroxy-5,6,7,8-tetrahydronaphthalen-1-yl]methanesulfonamide and its enantiomers: a novel selective α1A receptor agonist. J.Med.Chem. 39 4116 PMID: 8831777
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关键词: A 61603 hydrobromide, A 61603 hydrobromide supplier, α1A-adrenoceptor, alpha1A-adrenoceptor, agonists, α1a-adrenergic, alpha1a-adrenergic, a1a-adrenergic, a1a-adrenoceptor, Receptors, A61603, hydrobromide, α1a, Adrenergic, Alpha-1, 1052, Tocris Bioscience
12 篇 A 61603 hydrobromide 的引用文献
引用文献是使用了 Tocris 产品的出版物。 A 61603 hydrobromide 的部分引用包括：
Thomas et al (2016) The α-1A Adrenergic Receptor in the Rabbit Heart. Nephrol Dial Transplant 11 e0155238 PMID: 27258143
Desir and Peixoto (2014) Renalase in hypertension and kidney disease. Circ Res 29 42604 PMID: 24137013
Treen et al (2016) Divergent regulation of ER and kiss genes by 17 beta -OE in hypothalamic ARC versus AVPV models. Mol.Endocrinol. 30 217 PMID: 26726951
Dash et al (2011) A molecular MRI probe to detect treatment of cardiac apoptosis in vivo. Magn Reson Med 66 1152 PMID: 21360750
O-Uchi et al (2008) Interaction of α1-adrenoceptor subtypes with different G proteins induces opposite effects on cardiac L-type Ca2+ channel. PLoS One 102 1378 PMID: 18467629
Jensen et al (2009) The α-1D Is the predominant α-1-adrenergic receptor subtype in human epicardial coronary arteries. PLoS One 54 1137 PMID: 19761933
Montgomery (2017) An Alpha-1A Adrenergic Receptor Agonist Prevents Acute dox. Cardiomyopathy in Male Mice. Plos One 12 e0168409 PMID: 28081170
Copik et al (2015) Isoproterenol acts as a biased agonist of the α-1A-adrenoceptor that selectively activates the MAPK/ERK pathway. PLoS One 10 e0115701 PMID: 25606852
Amirak et al (2013) p90 ribosomal S6 kinases play a significant role in early gene regulation in the cardiomyocyte response to G(q)-protein-coupled receptor stimuli, endothelin-1 and α(1)-adrenergic receptor agonists. Biochem J 450 351 PMID: 23215897
Thomas et al (2016) A Myocardial Slice Culture Model Reveals Alpha-1A-Adrenergic Receptor Signaling in the Human Heart. JACC Basic Transl Sci 1 155 PMID: 27453955
Jensen et al (2010) Functional alpha-1B adrenergic receptors on human epicardial coronary artery endothelial cells. Naunyn Schmiedebergs Arch Pharmacol 382 475 PMID: 20857090
Rokosh and Simpson (2002) Knockout of the alpha 1A/C-adrenergic receptor subtype: the alpha 1A/C is expressed in resistance arteries and is required to maintain arterial blood pressure. Proc Natl Acad Sci U S A 99 9474 PMID: 12093905
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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.