A 61603 hydrobromide
Cat. No. 1052
Chemical Name: N-[5-(4,5-Dihydro-1H-imidazol-2-yl)
Biological ActivityPotent 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). Also available as part of the α1-Adrenoceptor Tocriset™.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Datasheet
References are publications that support the products' biological activity.
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.
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.
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Citations are publications that use Tocris products. Selected citations for A 61603 hydrobromide include:
Thomas et al (2016) The α-1A Adrenergic Receptor in the Rabbit Heart. Nephrol Dial Transplant 11 e0155238. PMID: 27258143.
Treen et al (2016) Divergent regulation of ER and kiss genes by 17ß-estradiol in hypothalamic ARC versus AVPV models. Mol.Endocrinol. 30 217. PMID: 26726951.
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.
Desir and Peixoto (2014) Renalase in hypertension and kidney disease. Circ Res 29 42604. PMID: 24137013.
Dash et al (2011) A molecular MRI probe to detect treatment of cardiac apoptosis in vivo. Magn Reson Med 66 1152. PMID: 21360750.
Jensen et al (2010) Functional alpha-1B adrenergic receptors on human epicardial coronary artery endothelial cells. Naunyn Schmiedebergs Arch Pharmacol 382 475. PMID: 20857090.
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.
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.
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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