Phentolamine hydrochloride

Manufactured by Merck Group

Sourced in United States

Phentolamine hydrochloride is a chemical compound used in laboratory settings. It functions as an alpha-adrenergic antagonist, which means it blocks the action of certain neurotransmitters in the body. This compound is commonly utilized in research applications, but its specific intended uses should not be extrapolated upon.

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Phentolamine (38 citations) Hydrochlorides (2 citations)

12 protocols using phentolamine hydrochloride

Molecular Mechanisms of Vascular Remodeling

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Norepinephrine bitartrate monohydrate was obtained from MedChem Express (Monmouth Junction, NJ, USA). Propranolol hydrochloride and losartan were bought from Tocris Bioscience (Bristol, Avon, UK). Phentolamine hydrochloride and GW4869 were purchased from Sigma (St. Louis, MO, USA). GW4869 was dissolved in 1% dimethyl sulfoxide (DMSO). PBS containing 1% DMSO was used as the control. Other chemicals were dissolved in PBS.
Antibodies against α-SMA (1:5000), CD9 (1:1000), TSG101 (1:2000), calnexin (1:2000) and ACE (1:1000) were purchased from Abcam (Cambridge, MA, USA). Antibodies against PCNA (1:5000) and PECAM-1 (1:2000) were obtained from Protein Tech Group Inc. Antibody against CD63 (1:1000) was acquired from Wanleibio. (Shengyang, China). Antibody against vimentin (1:2000) was purchased from Abways Technology, Inc. (Shanghai, China). Antibodies against β-actin (1:10000) and GAPDH (1:10000) were bought from Cell Signaling Technology (Beverly, MA, USA). These antibodies were used for Western blot analyses. GAPDH and β-actin were used as loading control.

Ye C., Zheng F., Xu T., Wu N., Tong Y., Xiong X.Q., Zhou Y.B., Wang J.J., Chen Q., Li Y.H., Zhu G.Q, & Han Y. (2022). Norepinephrine acting on adventitial fibroblasts stimulates vascular smooth muscle cell proliferation via promoting small extracellular vesicle release. Theranostics, 12(10), 4718-4733.

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Antidepressant Activity of Apigenin

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“Beijing Mesochem Technology Co., Ltd. (Beijing, China)” provided apigenin (purity: 98.20 percent by HPLC). The rest of the chemicals required for this investigation were obtained from well-known suppliers, and the labels were recorded for future use. Ondansetron hydrochloride, p-chlorophenylalanine methyl ester, α-methyl-para-tyrosine methyl ester (AMPT), R(+)-SCH-23390 hydrochloride, sulpiride, phentolamine hydrochloride, and propranolol were procured from Sigma-Aldrich. Sodium chloride (0.9 percent) was used for dissolving all compounds except AMPT, whereas, the solution of AMPT was made in 10% Tween 80. Apigenin (25 and 50 mg/kg was given orally (Redrobe et al., 1998 (link)) three times before the test sessions, at 24, 5, and 1 h (Shoubaky et al., 2016 (link)). The standard antidepressant fluoxetine (30 mg/kg, oral) (Castagné et al., 2011 ) was used to compare antidepressant activities. Except for SCH23390, which was given subcutaneously, all other compounds were given by intraperitoneal route (10 ml/kg).

Al-Yamani M.J., Mohammed Basheeruddin Asdaq S., Alamri A.S., Alsanie W.F., Alhomrani M., Alsalman A.J., Al mohaini M., Al Hawaj M.A., Alanazi A.A., Alanzi K.D, & Imran M. (2021). The role of serotonergic and catecholaminergic systems for possible antidepressant activity of apigenin. Saudi Journal of Biological Sciences, 29(1), 11-17.

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Cardiovascular Pharmacology Reagents Protocol

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Sodium pentobarbital (Dorminal 20%) was bought as an injectable solution (200 mg/ml, w/v) from Alfasan Woerden-Holland. Dimethyl sulfoxide (DMSO), sodium chloride (NaCl), potassium chloride (KCl), calcium chloride dihydrate (CaCl₂.2H₂O), magnesium sulfate heptahydrate (MgSO₄.7H₂O), potassium dihydrogen phosphate (KH₂PO₄), D (+)-glucose, and sodium hydrogen carbonate (NaHCO₃) were purchased from Merck, Germany. Carbogen (a mixture of 95% O₂ and 5% CO₂) was purchased from Linde (M) Sdn. Bhd. Serotonin hydrochloride, phenylephrine hydrochloride, atropine sulfate, N_ω-nitro-l-arginine methyl ester (L-NAME), propranolol hydrochloride, and phentolamine hydrochloride were purchased from Sigma®, USA.

Ismail A, & Wan Ahmad W.A. (2017). Autonomic Receptors and Nitric-Oxide Involvements in Mediating Vasorelaxation Effect Induced by Syzygium polyanthum Leaves Extract. Pharmacognosy Research, 9(Suppl 1), S9-S14.

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Investigating Adrenergic Modulation of Tumor Growth

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Phentolamine hydrochloride (Sigma, #P7547) in PBS vehicle, or an equivalent volume of vehicle alone for placebo in control mice and restraint-only mice, was injected subcutaneously at 5mg/kg daily, commencing 5 days before tumor cell inoculation and continuing to the end of the experiment on Day 28. Two experiments with phentolamine were conducted and included the following groups: (1) Control; (2) Restraint + Placebo; (3) No Restraint + Phentolamine; (4) Restraint + Phentolamine. For each experiment, n = 3 to 5 mice per group. An additional experiment was conducted with phentolamine and the non-selective β-blocker, s-propranolol (#P8688) at 2mg/kg, to determine whether the promoting effects of phentolamine were mediated through β-adrenergic receptors and included the following groups: (1) Control; (2) Phentolamine; (3) Propranolol; (4) Phentolamine + Propranolol (n = 5 mice per group). To examine the effect of selective α-adrenergic receptor blockade under non-stress conditions, an experiment was conducted with the α₁-blocker, prazosin hydrochloride (#P7791) at 2mg/kg, and the α₂-blocker, efaroxan hydrochloride (#E3263) at 5mg/kg, and included the following groups: (1) Control; (2) Prazosin; (3) Efaroxan (n = 4 to 6 mice per group).

Lamkin D.M., Sung H.Y., Yang G.S., David J.M., Ma J.C., Cole S.W, & Sloan E.K. (2014). α2-adrenergic blockade mimics the enhancing effect of chronic stress on breast cancer progression. Psychoneuroendocrinology, 51, 262-270.

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Adrenergic and Cholinergic Receptor Modulation

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Phentolamine hydrochloride (Sigma, P7547), nadolol (Sigma, N1892), atenolol (Sigma, A7655), and ICI-118,551 hydrochloride (SelleckChem, 0821), were used in this study as antagonists for different adrenergic receptors and were dissolved in milliQ water and filter-sterilized. Three different ADRB2 agonists were used. Norepinephrine bitartrate (Sigma, A0937) was dissolved in complete IMDM supplemented with 10% FBS. Albuterol (Salbutamol sulfate, SelleckChem, S2507) was dissolved in either DMSO (Fig. 2C) or complete IMDM supplemented with 10% FBS (all others). Salmeterol (Tocris, 1660) was dissolved in DMSO. The α7 nicotinic acetylcholine receptor antagonist, methyllycaconitine, was dissolved in milliQ water. Forskolin was dissolved in DMSO and used to stimulate cAMP production. The corresponding vehicle control was used for each experiment.

Estrada L.D., Ağaç D, & Farrar J.D. (2016). Sympathetic neural signaling via the β2-adrenergic receptor suppresses T-cell receptor-mediated human and mouse CD8+ T-cell effector function. European journal of immunology, 46(8), 1948-1958.

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Pharmacological Treatments for Neurological Research

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Dopamine hydrochloride (H8502, Sigma-Aldrich, Saint Louis, MO, USA), eticlopride hydrochloride (E101, Sigma-Aldrich), quinpirole hydrochloride (1061, Tocris Bioscience, Bristol, UK), and phentolamine hydrochloride (P7547, Sigma Aldrich) were all prepared fresh prior to each injection by dissolving in 0.9% NaCl. Domperidone (J63681, Alfa Aesar, Haverhill, MA, USA) was mixed in a solution of 0.02% acetic acid and gently heated until fully dissolved. Heparin sodium (American Pharmaceutical Partners, Incorporated, Schaumberg, IL, USA) was diluted to 10 units per milliliter in 0.9% NaCl. Gentamicin sulfate (510209, VetOne, Boise, ID, USA) was diluted to 5 mg/ml in 0.9% NaCl. The injection volume for each of these drugs was 1 ml/kg. Each of these drugs was administered IV. Urethane (44804-30, Alfa Aesar) was dissolved at a concentration of 150 mg/ml in 0.9% NaCl and administered at 8 ml/kg intraperitoneal (IP). All procedures using urethane anesthesia were terminal.

Obray J.D., Small C.A., Baldwin E.K., Jang E.Y., Lee J.G., Yang C.H., Yorgason J.T, & Steffensen S.C. (2022). Dopamine D2-Subtype Receptors Outside the Blood-Brain Barrier Mediate Enhancement of Mesolimbic Dopamine Release and Conditioned Place Preference by Intravenous Dopamine. Frontiers in Cellular Neuroscience, 16, 944243.

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Isolation and Characterization of Ganoderic Acid A

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Ganoderic acid A (purity > 90%) was isolated in the Department of Natural Medicinal Chemistry, Institute of Materia Medica, Chinese Academy of Medical Sciences, and the structure is shown in Fig. 1.Fig. 1

The structure of ganoderic acid A.

Metoprolol was purchased from Shanghai Dingkang Biomedical Materials Technology Co., Ltd. (China). dl-Adrenalin was purchased from Shanghai Yuanye Biotechnology Co., Ltd. (China). Phentolamine hydrochloride, ICI 118551, SNP, and 3-(4,5-dimethylthia-zol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) were purchased from Sigma-Aldrich Chemical Co. (St. Louis, MO, USA). Dulbecco’s modified Eagle’s medium (DMEM) and horse serum (HS) were obtained from Gibco Life Technologies Inc. (Grand Island, NY, USA). Fetal bovine serum (FBS) was purchased from PAN Seratech Co. (Aidenbach, Germany).

Yu Z.R., Jia W.H., Liu C., Wang H.Q., Yang H.G., He G.R., Chen R.Y, & Du G.H. (2020). Ganoderic acid A protects neural cells against NO stress injury in vitro via stimulating β adrenergic receptors. Acta Pharmacologica Sinica, 41(4), 516-522.

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Ligand Binding Assay Reagents

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Tyramine hydrochloride, (±)-octopamine hydrochloride, dopamine hydrochloride, naphazoline hydrochloride, forskolin, chlorpromazine hydrochloride, phentolamine hydrochloride, and mianserin hydrochloride were all purchased from Sigma-Aldrich (St. Louis, MO, USA). To culture HEK-293 cells, DMEM/F12 medium, fetal bovine serum (FBS), fungizone, penicillin, and streptomycin were purchased from Gibco Cell Culture at Life Technologies (Grand Island, NY, USA). TransIT-LT1 Transfection Reagent was obtained from Mirus Bio LLC (Madison, WI, USA).

Li H.M., Jiang H.B., Gui S.H., Liu X.Q., Liu H., Lu X.P., Smagghe G, & Wang J.J. (2016). Characterization of a β-Adrenergic-Like Octopamine Receptor in the Oriental Fruit Fly, Bactrocera dorsalis (Hendel). International Journal of Molecular Sciences, 17(10), 1577.

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Neurochemical Analysis Protocol

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6-OHDA hydrobromide, DL-propranolol hydrochloride, phentolamine hydrochloride, guanidine hydrochloride, DL alanine, α-ketoglutaric acid, sodium pyruvate, 2,4-dinitrophenilhydrazine, metaphosphoric acid, 2-propanol and 1-bromo-3-chloropropane (Sigma Chemical, St. Louis, MO, USA).

Aldaba-Muruato L.R., Muñoz-Ortega M.H., Macías-Pérez J.R., Pulido-Ortega J., Martínez-Hernández S.L, & Ventura-Juárez J. (2017). Adrenergic regulation during acute hepatic infection with Entamoeba histolytica in the hamster: involvement of oxidative stress, Nrf2 and NF-KappaB. Parasite, 24, 46.

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Evaluating Stress Response Modulation

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Non-stressed C57BL/6J mice were intraperitoneally injected with either vehicle (saline) or propranolol (30 mg kg⁻¹, propranolol hydrochloride, Sigma-Aldrich) and phentolamine (30 mg kg⁻¹, phentolamine hydrochloride, Sigma-Aldrich) under short isoflurane anaesthesia. Then, 75 min after injection, baseline blood was withdrawn under short isoflurane anaesthesia. After a short recovery from the isoflurane, the mice were restraint-stressed for 20 min and then allowed to recover for 40 min before blood was withdrawn again.

Poller W.C., Downey J., Mooslechner A.A., Khan N., Li L., Chan C.T., McAlpine C.S., Xu C., Kahles F., He S., Janssen H., Mindur J.E., Singh S., Kiss M.G., Alonso-Herranz L., Iwamoto Y., Kohler R.H., Wong L.P., Chetal K., Russo S.J., Sadreyev R.I., Weissleder R., Nahrendorf M., Frenette P.S., Divangahi M, & Swirski F.K. (2022). Brain motor and fear circuits regulate leukocytes during acute stress. Nature, 607(7919), 578-584.

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