Phentolamine hydrochloride
Based on 8 publication(s) in Google Scholar
Phentolamine hydrochloride is an orally active, selective α1 and α2 Adrenergic receptor antagonist. Phentolamine hydrochloride antagonizes the vasodilatory effect of Cromakalim (HY-110011) on isolated circumflex coronary artery segments in dogs. Phentolamine hydrochloride reduces systemic vascular resistance and increases cardiac output. Phentolamine hydrochloride improves erectile dysfunction. Phentolamine hydrochloride can be used for the research of erectile dysfunction.
For research use only. We do not sell to patients.
- Purity: 99.91%
- CAS No.: 73-05-2
- Formula: C17H20ClN3O
- Molecular Weight:317.82
-
Storage:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
-
Bioactive Compound Library Max
HY-L181
-
Bioactive Compound Library
HY-L001
-
GPCR/G Protein Compound Library
HY-L006
-
Neuronal Signaling Compound Library
HY-L013
-
FDA-Approved Drug Library
HY-L022
-
Drug Repurposing Compound Library
HY-L035
-
Anti-Cardiovascular Disease Compound Library
HY-L046
-
Endocrinology Compound Library
HY-L047
-
Orally Active Compound Library
HY-L061
-
Neurotransmitter Receptor Compound Library
HY-L062
-
FDA Approved & Pharmacopeial Drug Library
HY-L066
-
Anti-Alzheimer's Disease Compound Library
HY-L069
-
Neurodegenerative Disease-related Compound Library
HY-L086
-
Antidepressant Compound Library
HY-L108
-
Human Metabolite Library
HY-L123
-
Off-patent Drug Library
HY-L141
-
Antihypertensive Compound Library
HY-L145
-
Membrane Protein-targeted Compound Library
HY-L149
-
Membrane Receptor-targeted Compound Library
HY-L150
-
Highly Selective Inhibitors Library
HY-L158
-
Anti-Drug-Resistant Compound Library
HY-L169
-
Multi-Target Compound Library
HY-L176
-
MCE Bioactive Compound Library
HY-L001V
-
Drug Repurposing Compound Library Plus
HY-L035P
-
FDA-Approved Drug Library Plus
HY-L022P
-
FDA-Approved Drug Library Mini
HY-L022M
-
High-Throughput Bioactive Compound Library
HY-L205
-
Mass Spectrometry Human Metabolite Library
HY-L215
-
Lactylation Compound Library
HY-L249
Publications Citing Use of MedChemExpress (MCE) Phentolamine hydrochloride
More- Acta Pharmacol Sin. 2026 May 29. [Abstract]
- Neurosci Bull. 2023 Dec;39(12):1789-1806. [Abstract]
- J Endocrinol. 2020 Mar;244(3):459-471. [Abstract]
- Comput Struct Biotechnol J. 2025 Dec 31;31:192-201.
- Insect Biochem Mol Biol. 2025 May:180:104312. [Abstract]
- J Cancer. 2024 Sep 9;15(17):5691-5709. [Abstract]
- SSRN. 2026 Apr 30.
- bioRxiv. 2023 Oct 13.
Customer Validation & Images
-
Cell Migration/Invasion Assay
-
Cell Migration/Invasion Assay
-
IHC
-
WB
-
In Vivo Efficacy Study
All Adrenergic Receptor Isoforms
More
Biological Activity
|
α1-adrenergic receptor |
α2-adrenergic receptor |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
1.1 nM
Compound: Phentolamine
|
Displacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysis
Displacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysis
|
[PMID: 26005522] |
| CHO | IC50 |
10.8 nM
Compound: Phentolamine
|
Displacement of [3H]-Prazosin from human alpha-1B adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysis
Displacement of [3H]-Prazosin from human alpha-1B adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysis
|
[PMID: 26005522] |
| CHO | IC50 |
12.5 nM
Compound: Phentolamine
|
Displacement of [3H]-Prazosin from human alpha-1D adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysis
Displacement of [3H]-Prazosin from human alpha-1D adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysis
|
[PMID: 26005522] |
Phentolamine hydrochloride (1-100 μM) concentration-dependently antagonizes the vasodilatory effect of Cromakalim on isolated circumflex coronary artery segments of dogs; at a concentration of 100 μM, it reduces the pD2 value of Cromakalim from 6.62 to 5.08[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS No. 73-05-2
-
Appearance Solid
-
Molecular Weight 317.82
-
Formula C17H20ClN3O
-
Color Off-white to light yellow
-
SMILES
OC1=CC=CC(N(CC2=NCCN2)C3=CC=C(C)C=C3)=C1.[H]Cl
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Publications (8)
-
Journal Impact Factor
-
Most Recent
-
Acta Pharmacol Sin
Activation of peripheral muscarinic receptors rescues depressive-like behaviors via gut-brain-axis, involving parasympathetic excitation. [Abstract]2026 May 29. PMID: 42215618 -
Neurosci Bull
Peripheral BDNF Regulates Somatosensory-Sympathetic Coupling in Brachial Plexus Avulsion-Induced Neuropathic Pain. [Abstract]2023 Dec;39(12):1789-1806. PMID: 37335428
Phentolamine hydrochloride purchased from MedChemExpress. Usage Cited in: Neurosci Bull. 2023 Dec;39(12):1789-1806. [Abstract]
Phentolamine (0.5, 1 mg/kg; IP; once a day for 5 consecutive days) decreased the expression of BDNF, TrκB, and α2-AR after BPA.
Phentolamine hydrochloride purchased from MedChemExpress. Usage Cited in: Neurosci Bull. 2023 Dec;39(12):1789-1806. [Abstract]
Phentolamine (0.5, 1 mg/kg; IP; once a day for 5 consecutive days) increased the mechanical allodynia threshold of the affected ipsilateral forepaw and relieved the hypothermia in the ipsilateral forepaw and the edema in the ipsilateral forepaw of mice after BPA.
-
J Endocrinol
miR-7 mediates the signaling pathway of NE affecting FSH and LH synthesis in pig pituitary. [Abstract]2020 Mar;244(3):459-471. PMID: 31905166 -
-
Insect Biochem Mol Biol
Molecular and pharmacological characterization of the dopamine receptors in the oriental fruit fly, Bactrocera dorsalis. [Abstract]2025 May:180:104312. PMID: 40245998 -
J Cancer
Pan-cancer analysis of the role of α2C-adrenergic receptor (ADRA2C) in human tumors and validation in glioblastoma multiforme models. [Abstract]2024 Sep 9;15(17):5691-5709. PMID: 39308687
Phentolamine hydrochloride purchased from MedChemExpress. Usage Cited in: J Cancer. 2024 Sep 9;15(17):5691-5709. [Abstract]
Phentolamine (10 μM; 24, 48 h) increased the migration speed in GL261 cells.
Phentolamine hydrochloride purchased from MedChemExpress. Usage Cited in: J Cancer. 2024 Sep 9;15(17):5691-5709. [Abstract]
Phentolamine (0.005 μM; 12, 24 h) increased the migration speed in U87 cells.
Phentolamine hydrochloride purchased from MedChemExpress. Usage Cited in: J Cancer. 2024 Sep 9;15(17):5691-5709. [Abstract]
Phentolamine (1 mg/kg; IP; every other day for 14 days) elevated the Bcl2/Bax ratio and MMP2 expression level in tumor tissues of mouse glioma models.
-
-
Solvent & Solubility
DMSO : 116.67 mg/mL (367.09 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (6.54 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.08 mg/mL (6.54 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.08 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
-
Data Sheet (277 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
-
Handling Instructions (2659 KB)
References
[1]. Goldstein I, et al. Oral phentolamine: an alpha-1, alpha-2 adrenergic antagonist for the treatment of erectile dysfunction. Int J Impot Res. 2000;12 Suppl 1:S75-S80. [Content Brief]
[2]. Majid PA, et al. Phentolamine for vasodilator treatment of severe heart-failure. Lancet. 1971 Oct 2;2(7727):719-24. [Content Brief]
[3]. McPherson GA, et al. Phentolamine and structurally related compounds selectively antagonize the vascular actions of the K+ channel opener, cromromakalim. Br J Pharmacol. 1989;97(3):941-949. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.1464 mL | 15.7322 mL | 31.4644 mL | 78.6609 mL |
| 5 mM | 0.6293 mL | 3.1464 mL | 6.2929 mL | 15.7322 mL | |
| 10 mM | 0.3146 mL | 1.5732 mL | 3.1464 mL | 7.8661 mL | |
| 15 mM | 0.2098 mL | 1.0488 mL | 2.0976 mL | 5.2441 mL | |
| 20 mM | 0.1573 mL | 0.7866 mL | 1.5732 mL | 3.9330 mL | |
| 25 mM | 0.1259 mL | 0.6293 mL | 1.2586 mL | 3.1464 mL | |
| 30 mM | 0.1049 mL | 0.5244 mL | 1.0488 mL | 2.6220 mL | |
| 40 mM | 0.0787 mL | 0.3933 mL | 0.7866 mL | 1.9665 mL | |
| 50 mM | 0.0629 mL | 0.3146 mL | 0.6293 mL | 1.5732 mL | |
| 60 mM | 0.0524 mL | 0.2622 mL | 0.5244 mL | 1.3110 mL | |
| 80 mM | 0.0393 mL | 0.1967 mL | 0.3933 mL | 0.9833 mL | |
| 100 mM | 0.0315 mL | 0.1573 mL | 0.3146 mL | 0.7866 mL |
Phentolamine hydrochloride Related Classifications
HY-12717A Related Classifications
Powered by Bioz
- Phentolamine
- 73-05-2
- Adrenergic Receptor
- ischaemic heart-disease
- alpha-1 receptor
- cromakalim-sensitive K+ channels
- dog isolated circumflex coronary artery segments
- human corpus cavernosum tissue
- erectile dysfunction
- cardiac beta-receptors
- alpha-2 receptor
- alpha-adrenergic receptor
- rat isolated femoral artery segments
- Inhibitor
- inhibitor
- inhibit