Phentolamine Mesylate

Catalog No.S2038 Synonyms: Phentolamine methanesulfonate

For research use only.

Phentolamine Mesylate(Phentolamine methanesulfonate) is a reversible and nonselective alpha-adrenergic receptor antagonist, used for the prevention or control of hypertensive episodes.

Phentolamine Mesylate Chemical Structure

CAS No. 65-28-1

Selleck's Phentolamine Mesylate has been cited by 1 Publication

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Biological Activity

Description Phentolamine Mesylate(Phentolamine methanesulfonate) is a reversible and nonselective alpha-adrenergic receptor antagonist, used for the prevention or control of hypertensive episodes.
Targets
α-adrenergic receptor [1]
In vitro

Phentolamine mesylate displaces binding of the selective alpha 1 receptor antagonists [125I]HEAT and [3H]prazosin and the alpha 2 receptor antagonists [3H]rauwolscine and [3H]RX 821002 with relatively high affinity in corpus cavernosum membranes. Phentolamine mesylate causes concentration dependent relaxation in erectile tissue strips pre-contracted with adrenergic agonists phenylephrine, norepinephrine, oxymetazoline and UK 14,304, as well as with non-adrenergic contractile agents Endothelin and KCl. Phentolamine mesylate induces relaxation of corpus cavernosum erectile tissue by direct antagonism of alpha 1 and 2 adrenergic receptors and by indirect functional antagonism via a non-adrenergic, endothelium-mediated mechanism suggesting nitric oxide synthase activation. [1] Phentolamine, an alpha-adrenergic antagonist, blocks the vasoconstriction associated with the epinephrine used in dental anesthetic formulations, thus enhancing the systemic absorption of the local anesthetic from the injection site. [2]

In vivo

Phentolamine is a reversible competitive alpha-adrenergic antagonist with similar affinities for alphal and alpha2 receptors. Phentolamine mesylate causes vasodilatation and thus hypotension by decreasing peripheral vascular resistance. [4] Phentolamine mesylate (30 and 100 nM) dose-dependently enhances electrical field stimulation-induced relaxation of the rabbit corpus cavernosum. Phentolamine relaxes rabbit corpus cavernosum independent of alpha-adrenergic receptor blockade. Phentolamine mesylate relaxes nonadrenergic noncholinergic neurons of the rabbit corpus cavernosum by activating NO synthase and is independent of alpha-adrenergic receptor blockade. [5]

Protocol (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 377.46
Formula

C17H19N3O.CH4O3S

CAS No. 65-28-1
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=CC=C(C=C1)N(CC2=NCCN2)C3=CC(=CC=C3)O.CS(=O)(=O)O

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04955236 Completed Drug: Partial scalp block|Drug: Fentanyl Posterior Fossa Tumor Kasr El Aini Hospital July 14 2021 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-11-29)

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