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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

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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
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 lnformation & 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

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In vivo
Batch:

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In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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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.

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