Phentolamine-d4 is intended for use as an internal standard for the quantification of phentolamine by GC- or LC-MS. 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.
|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. J. Biol. Chem. 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).