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Phentolamine Mesylate

Name: Phentolamine Mesylate
Brand: Selleck Chemicals
SKU: S2038
Rating: 5 (2 reviews)

Synonyms: Phentolamine methanesulfonate

Catalog No.S2038 Purity: 99.96%

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: 65-28-1

Selleck's Phentolamine Mesylate has been cited by 2 publications

Purity & Quality Control

Batch: Purity: 99.96%

99.96

Phentolamine Mesylate Related Products

Related Targets	α-adrenergic receptor β-adrenergic receptor Beta-Adrenergic Receptor	Click to Expand
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Signaling Pathway

Adrenergic Receptor Signaling Pathway

Choose Selective Adrenergic Receptor Inhibitors

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
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
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]

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT04955236	Completed	Posterior Fossa Tumor	Kasr El Aini Hospital	July 14 2021	Phase 1

References

[4] Vemulapalli S, et al. Fundam Clin Pharmacol,?001, 15(1), 1-7.

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Chemical Information & Solubility

Molecular Weight	377.46	Formula	C₁₇H₁₉N₃O.CH₄O₃S
CAS No.	65-28-1	SDF	Download Phentolamine Mesylate SDF
Smiles	CC1=CC=C(C=C1)N(CC2=NCCN2)C3=CC(=CC=C3)O.CS(=O)(=O)O
Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 76 mg/mL ( (201.34 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 76 mg/mL

Ethanol : 76 mg/mL

Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.

In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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