An α1A-adrenoceptor agonist
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A-61603

Item No. 17358

Technical Information
Formal Name
N-[5-(4,5-dihydro-1H-imidazol-2-yl)-5,6,7,8-tetrahydro-2-hydroxy-1-naphthalenyl]-methanesulfonamide, monohydrobromide
CAS Number
107756-30-9
Molecular Formula
C14H19N3O3S • HBr
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
DMF: 20 mg/mlDMSO: 20 mg/mlEthanol: 1 mg/mlPBS (pH 7.2): 10 mg/ml
SMILES
OC1=C(NS(C)(=O)=O)C2=C(C(C3=NCCN3)CCC2)C=C1.Br
InChi Code
InChI=1S/C14H19N3O3S.BrH/c1-21(19,20)17-13-10-3-2-4-11(14-15-7-8-16-14)9(10)5-6-12(13)18;/h5-6,11,17-18H,2-4,7-8H2,1H3,(H,15,16);1H
InChi Key
LRFLWCZMTGTUEP-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    The α1-adrenergic receptors are Gq protein-coupled receptors that play a key role in the modulation of sympathetic nervous system activity and are the site of action for therapeutic agents, such as antihypertensive drugs. A-61603 is a selective α1A-adrenergic receptor agonist that is at least 35-fold more potent at α1A receptor sites than at α1B or α1D.1 Activation of the α1A-adrenergic receptor by A-61603 has been reported to increase the frequency of spontaneous Ca2+ transients in rat ventricular myocytes in vitro (EC50 = 6.9 nM) much more potently than activation by phenylephrine (Item No. 17205; EC50 = 2.3 µM).2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Meyer, M.D., Altenbach, R.J., Hancock, A.A., et alSynthesis and in vitro characterization 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(20), 4116-4119 (1996).

    2. Luo, D.l., Gao, J., Fan, L.l., et alReceptor subtype involved in α1-adrenergic receptor-mediated Ca2+ signaling in cardiomyocytes. Acta Pharmacol. Sin. 28(7), 968-974 (2007).