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Phentolamine Mesylate

Cat. No. M3752
Phentolamine Mesylate Structure
Size Price Availability Quantity
100mg USD 80 In stock
500mg USD 160 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

Phentolamine mesylate is safe and effective in the long-term treatment of men with mild to moderate ED. Phentolamine increased catecholamine release by presynaptic alpha 2-blockade, thereby suppressing the autoinhibition of transmitter release. Phentolamine leads to an increase in FBM by preferentially antagonizing presynaptic alpha 2-adrenoreceptors over postsynaptic alpha 1-adrenoreceptors. This influence of phentolamine on FBM may be secondary to its effect on ECoG. Promotion of LV-ECoG by catecholamines is mediated via an alpha 1-independent mechanism.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 377.46
Formula C18H23N3O4S
CAS Number 65-28-1
Purity >99%
Solubility DMSO 75 mg/mL
Water 75 mg/mL
Storage at -20°C
References

Long-term safety and efficacy of oral phentolamine mesylate (Vasomax) in men with mild to moderate erectile dysfunction.
Padma-Nathan H, et al. Int J Impot Res. 2002 Aug;14(4):266-70. PMID: 12152116.

Alpha 1- and alpha 2-adrenoreceptor actions of phentolamine and prazosin on breathing movements in fetal sheep in utero.
Giussani DA, et al. J Physiol. 1995 Jul 1;486 ( Pt 1):249-55. PMID: 7562640.

Alpha-adrenoceptor blockade by phentolamine causes beta-adrenergic vasodilation by increased catecholamine release due to presynaptic alpha-blockade.
Saeed M, et al. J Cardiovasc Pharmacol. 1982 Jan-Feb;4(1):44-52. PMID: 6176798.

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Abmole Inhibitor Catalog 2017




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