A reversible α-adrenergic receptor antagonist
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Labeled Version(s)
29417Phentolamine-d4 (hydrochloride)
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Phentolamine (mesylate)

Item No. 16135

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-[[(4,5-dihydro-1H-imidazol-2-yl)methyl](4-methylphenyl)amino]-phenol, monomethanesulfonate
CAS Number
65-28-1
Molecular Formula
C17H19N3O • CH3SO3H
Formula Weight
377.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 50 mg/mlDMSO: 30 mg/mlEthanol: 15 mg/mlPBS (pH 7.2): 10 mg/ml
λmax
209, 277 nm
SMILES
CC(C=C1)=CC=C1N(C2=CC(O)=CC=C2)CC3=NCCN3.CS(O)(=O)=O
InChi Code
InChI=1S/C17H19N3O.CH4O3S/c1-13-5-7-14(8-6-13)20(12-17-18-9-10-19-17)15-3-2-4-16(21)11-15;1-5(2,3)4/h2-8,11,21H,9-10,12H2,1H3,(H,18,19);1H3,(H,2,3,4)
InChi Key
OGIYDFVHFQEFKQ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    50 mg

    $49

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    100 mg

    $86

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    500 mg

    $306

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    1 g

    $469

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    Product Description

    Phentolamine is a reversible antagonist of α-adrenergic receptors, non-specifically binding all α1- and α2-adrenoceptors with nanomolar affinities.1,2,3,4 Formulations containing phentolamine have been used in the treatment of hypertensive emergencies, as well as chronic and emergent pain.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Lomasney, J.W., Cotecchia, S., Lorenz, W., et al. Molecular cloning and expression of the cDNA for the α1A-adrenergic receptor. The gene for which is located on human chromosome 5. The Journal of Biological Chemisty 266(10), 6365-6369 (1991).

    2. Millan, M.J., Newman-Tancredi, A., Audinot, V., et al. Agonist and antagonist actions of yohimbine as compared to fluparoxan at α2-adrenergic receptors (AR)s, serotonin (5-HT)1A, 5-HT1B, 5-HT1D and dopamine D2 and D3 receptors. Significance for the modulation of frontocortical monoaminergic transmission and depressive states. Synapse 35(2), 79-95 (2000).

    3. O'Rourke, M.F., Iversen, L.J., Lomasney, J.W., et al. Species orthologs of the Alpha-2A adrenergic receptor: The pharmacological properties of the bovine and rat receptors differ from the human and porcine receptors. J. Pharmacol. Exp. Ther. 271(2), 735-740 (1994).

    4. Richelson, E., and Nelson, A. Antagonism by antidepressants of neurotransmitter receptors of normal human brain in vitro. J. Pharmacol. Exp. Ther. 230(1), 94-102 (1984).