Structure of 65-28-1
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
Phentolamine mesylate is a reversible and nonselective alpha-adrenergic receptor antagonist, used for the prevention or control of hypertensive episodes.
Synonyms: Phentolamine methanesulfonate; Phentolamine mesylate; Phentolamine (mesylate)
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Batch number can be found on the product's label following the word 'Batch'.
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Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
Batch number can be found on the product's label following the word 'Batch'.
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CAS No. : | 65-28-1 |
Formula : | C18H23N3O4S |
M.W : | 377.46 |
SMILES Code : | CS(O)(=O)=O.CC1=CC=C(N(C2=CC(O)=CC=C2)CC3=NCCN3)C=C1 |
Synonyms : |
Phentolamine methanesulfonate; Phentolamine mesylate; Phentolamine (mesylate)
|
MDL No. : | MFCD00134201 |
InChI Key : | OGIYDFVHFQEFKQ-UHFFFAOYSA-N |
Pubchem ID : | 91430 |
GHS Pictogram: |
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Signal Word: | Warning |
Hazard Statements: | H302+H312+H332-H315-H319-H335 |
Precautionary Statements: | P261-P280-P301+P312+P330-P305+P351+P338 |
Target |
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In Vitro:
Concentration | Treated Time | Description | References |
Rabbit aortic spiral strips | 0.1 μM | 2 hours | To investigate the inhibitory effect of phentolamine on ergonovine-induced contractions in normal and atherosclerotic rabbit aortic spiral strips. Results showed that 0.1 μM phentolamine inhibited 1 μM ergonovine-induced contractions by 71% in normal arteries, while the same concentration of phentolamine only inhibited 54% in atherosclerotic arteries. | PMC371712 |
Human periodontal ligament fibroblasts (HPDLFs) | 25 μM | 24 h or 48 h | To investigate the effect of phentolamine on LPS-inhibited HPDLF proliferation, results showed that phentolamine significantly ameliorated LPS-inhibited cell proliferation. | PMC4221694 |
Rabbit right atrium | 0.1-10 μM | 30 minutes | Phentolamine inhibited the tachycardia induced by field stimulation in a concentration-dependent manner. This effect was prevented by benextramine treatment and antagonized 10-fold by yohimbine (1 μM) but not by prazosin (0.1 μM). | PMC1986863 |
Mouse pancreatic β-cells | 20-100 μM | To study the inhibitory effects of phentolamine on ATP-sensitive K+ channels, results showed phentolamine significantly inhibited 86Rb efflux and ATP-sensitive K+ currents. | PMC1917617 | |
Mouse pancreatic β-cells | 10 μM | To investigate the inhibitory effect of Phentolamine on ATP-sensitive K+ channels and its impact on insulin release. Results showed that Phentolamine inhibited 86Rb efflux, indicating blockade of ATP-sensitive K+ channels, thereby increasing insulin release. | PMC1907631 | |
Guinea-pig detrusor smooth muscle cells | 3 μM - 100 μM | To investigate the effect of phentolamine on rhythmic contractions of detrusor muscle, results showed phentolamine induced concentration-dependent rhythmic contractions without affecting basal tone | PMC1986976 |
In Vivo:
Administration | Dosage | Frequency | Description | References |
Rabbit | Ganglion-blocked conscious or anaesthetized rabbits | Intravenous injection | 3-1000 μg/kg | Single injection | Phentolamine caused a dose-related rise in blood pressure in ganglion-blocked rabbits, which was antagonized by yohimbine (1 mg kg-1). In rabbits without ganglion blockade, phentolamine did not evoke a pressor response. | PMC1986863 |
Mice | Pancreatic β-cells | Perifusion | 20-100 μM | To study the inhibitory effects of phentolamine on ATP-sensitive K+ channels, results showed phentolamine significantly inhibited 86Rb efflux and ATP-sensitive K+ currents. | PMC1917617 | |
Sprague-Dawley rats | Hippocampal slices | Perfusion | 50 μM | 30 minutes | To study the long-term effects of NE and phentolamine on synaptic responses in the hippocampal dentate gyrus. Results showed that NE and phentolamine selectively potentiated responses to medial PP stimulation while depressing responses to lateral PP stimulation. | PMC287356 |
Guinea-pig | Detrusor smooth muscle strips | Tissue bath | 3 μM -100 μM | Single administration | To investigate the effect of phentolamine on rhythmic contractions of detrusor muscle, results showed phentolamine induced concentration-dependent rhythmic contractions without affecting basal tone | PMC1986976 |
Rats | Wistar WI/Ico, Wistar WAG/Rij, Fischer 344 | Perfusion and superfusion | 1μM | 10 minutes | To evaluate the efficiency of α2-adrenoceptor-mediated inhibition of noradrenaline release, results showed an increase in noradrenaline release in all ages and strains. | PMC1510134 |
Clinical Trial:
NCT Number | Conditions | Phases | Recruitment | Completion Date | Locations |
NCT03240822 | Urologic Injuries ... More >> Genital Diseases, Male Amputation Less << | Phase 1 | Recruiting | December 2025 | United States, North Carolina ... More >> Wake Forest School of Medicine Recruiting Winston-Salem, North Carolina, United States, 27104 Contact: Mary-Clare Day, RN BSN 336-713-1343 Mday@wakehealth.edu Less << |
NCT01422616 | Ischemic Stroke ... More >> High Blood Pressure Less << | Phase 3 | Recruiting | February 2019 | Australia, New South Wales ... More >> Royal Prince Alfred Hospital Recruiting Sydney, New South Wales, Australia, 2050 Contact: Craig S Anderson, MD +61 2 933 4500 canderson@georgeinstitute.org.au Less << |
NCT00226096 | CVA (Cerebrovascular Accident)... More >> Cerebral Hemorrhage Intracranial Hemorrhages Less << | Not Applicable | Completed | - | Australia, New South Wales ... More >> Concord Hospital Concord, New South Wales, Australia, 2138 Gosford Hospital Gosford, New South Wales, Australia, 2250 St George Hospital Kogarah, New South Wales, Australia, 2217 John Hunter Hospital Newcastle, New South Wales, Australia, 2310 St Vincent's Hospital Sydney, New South Wales, Australia, 2010 Royal Prince Alfred Hospital Sydney, New South Wales, Australia, 2050 Westmead Hospital Westmead, New South Wales, Australia, 2145 Australia, South Australia Royal Adelaide Hospital Adelaide, South Australia, Australia, 5000 Australia, Victoria Royal Melbourne Hospital Melbourne, Victoria, Australia, 3050 St Vincent's Hospital Melbourne, Victoria, Australia, 3065 Box Hill Hospital Melbourne, Victoria, Australia, 3128 Alfred Hospital Melbourne, Victoria, Australia, 3181 Austin Health Melbourne, Victoria, Australia Monash Medical Centre Melbourne, Victoria, Australia Australia, Western Australia Sir Charles Gairdner Hospital Perth, Western Australia, Australia, 6009 China Regional Coordinating Centre: Peking University First Hospital Beijing, China, 100034 Hospitals in China, c/o The George Institute China Beijing, China Regional Coordinating Centre: Centre for Epidemiological Studies and Clinical Trials, Ruijin Hospital, Shanghai Institute of Hypertension, Shanghai Second Medical University Shanghai, China, 200025 New Zealand North Shore Hospital Auckland, New Zealand Christchurch Hospital Christchurch, New Zealand Less << |
NCT01032694 | - | Terminated(This study was term... More >>inated January 11, 2011 due to low enrollment. This study is not being terminated because of safety or efficacy concerns.) Less << | - | - | |
NCT01032694 | - | Terminated(This study was term... More >>inated January 11, 2011 due to low enrollment. This study is not being terminated because of safety or efficacy concerns.) Less << | - | - | |
NCT03752957 | - | Not yet recruiting | October 2019 | - | |
NCT00577876 | Prostate Cancer | Not Applicable | Completed | - | United States, New York ... More >> Memorial Sloan-Kettering Cancer Center New York, New York, United States, 10021 Less << |
NCT00104104 | Multiple Myeloma | Phase 4 | Completed | - | - |
NCT02966665 | Chronic Obstructive Pulmonary ... More >>Disease Pulmonary Artery Hypertension Heart Failure Hypertension Less << | Phase 1 | Recruiting | August 2020 | United States, Utah ... More >> George E Wahlen VA Medical Center Recruiting Salt Lake City, Utah, United States, 84132 Contact: Russell Richardson, Ph.D. 801-582-1565 r.richardson@hsc.utah.edu Contact: Ashley Nelson, MD 801-582-1565 ext 4127 ash.nelson@hsc.utah.edu Less << |
NCT00716079 | Intracerebral Hemorrhage ... More >> Stroke Hypertension Less << | Not Applicable | Completed | - | - |
NCT00104104 | - | Completed | - | - | |
NCT00080808 | Prostate Cancer | Phase 2 | Completed | - | United States, Texas ... More >> M.D. Anderson Cancer Center at University of Texas Houston, Texas, United States, 77030-4009 Less << |
NCT00716079 | - | Completed | - | - | |
NCT00154167 | Soft Tissue Anesthesia (Numbne... More >>ss) Less << | Phase 2 | Completed | - | United States, Washington ... More >> Northwest Kinetics Tacoma, Washington, United States, 98403 Less << |
NCT00132106 | Heart Failure, Congestive | Not Applicable | Unknown | - | Netherlands ... More >> Radboud University Nijmegen Medical Centre Recruiting Nijmegen, Netherlands, 6500 HB Contact: Marc ER Gomes, MD 31-24-3614533/3616550 m.gomes@cardio.umcn.nl Sub-Investigator: Marc ER Gomes, MD Sub-Investigator: Alexandra H Mulder, MD Sub-Investigator: Freek WA Verheugt, MD, PhD Sub-Investigator: Paul Smits, MD, PhD Principal Investigator: Cees J Tack, MD, PhD Sub-Investigator: Louise Bellersen, MD Less << |
NCT02584686 | Vasculogenic Erectile Dysfunct... More >>ion Less << | Phase 1 | Completed | - | Egypt ... More >> Cairo University Hospitals Cairo, Egypt, 11321 Less << |
NCT02584686 | - | Completed | - | - | |
NCT00309322 | Anesthesia, Dental | Phase 2 | Completed | - | United States, Massachusetts ... More >> The Forsyth Institute Boston, Massachusetts, United States, 02115 Less << |
NCT00309335 | Anesthesia, Dental | Phase 3 | Completed | - | United States, Massachusetts ... More >> Tufts University School of Dental Medicine Boston, Massachusetts, United States, 02111 Less << |
NCT00309361 | Anesthesia, Dental | Phase 3 | Completed | - | United States, Massachusetts ... More >> Tufts School of Dental Medicine Boston, Massachusetts, United States, 02111 Less << |
NCT03079921 | Type1diabetes ... More >> Hypoglycemia Hypoglycemia Unawareness Less << | Early Phase 1 | Recruiting | December 2020 | United States, Pennsylvania ... More >> University of Pennsylvania - Institute for Diabetes, Obesity and Metabolism Recruiting Philadelphia, Pennsylvania, United States, 19104 Contact: Eileen Markmann 215-350-0364 eileen.markmann@uphs.upenn.edu Contact: Cornelia Dalton Bakes 2155274490 ext Dalton Bakes cornelia.dalton-bakes@uphs.upenn.edu Principal Investigator: Michael R Rickels, MD., MS Less << |
NCT03098680 | Drug-Related Side Effects and ... More >>Adverse Reactions Cardiovascular System Disease Less << | Phase 1 | Recruiting | February 29, 2020 | United Kingdom ... More >> Addenbrooke's Hospital Recruiting Cambridge, Cambridgeshire, United Kingdom, CB2 0QQ Contact: Joseph Cheriyan, MBChB, MA, FRCP jc403@medschl.cam.ac.uk Less << |
NCT03318094 | Insulin Resistance ... More >> Healthy Obesity Less << | Phase 1 | Recruiting | November 30, 2025 | United States, Tennessee ... More >> Autonomic Dysfunction Center Recruiting Nashville, Tennessee, United States, 37232 Contact: Misty D Hale, CCRP 615-343-8649 autonomics@vanderbilt.edu Contact: Jorge E Celedonio 6153223304 autonomics@vanderbilt.edu Less << |
NCT03033537 | - | Completed | - | - | |
NCT02995291 | Anesthesia, Local | Phase 4 | Recruiting | February 2019 | Canada, Nova Scotia ... More >> Dalhousie University Faculty of Dentistry Recruiting Halifax, Nova Scotia, Canada, B3H 4R2 Contact: Pierre-Luc Michaud, MSc 902-494-4264 PL.Michaud@Dal.ca Principal Investigator: Pierre-Luc Michaud, MSc Less << |
NCT02861378 | Soft Tissue Anaesthesia | Not Applicable | Completed | - | Canada, Nova Scotia ... More >> Dalhousie University Faculty of Dentistry Halifax, Nova Scotia, Canada, B3H 4R2 Less << |
NCT01703559 | Night Vision Complaints | Phase 2 | Completed | - | United States, Arizona ... More >> Celerion Phoenix, Arizona, United States, 67230 Less << |
NCT01474382 | Dental Anesthesia ... More >> Anesthesia, Local Anesthesia, Reversal Less << | Phase 4 | Completed | - | United States, California ... More >> University of California, San Francisco San Francisco, California, United States, 94143 United States, Indiana Indiana University School of Dentistry Indianapolis, Indiana, United States, 46202 United States, Ohio Nationwide Children's Hospital Columbus, Ohio, United States, 43205 United States, Pennsylvania University of Pennsylvania School of Dental Philadelphia, Pennsylvania, United States, 19104-6030 University of Pittsburgh School of Dental Medicine Pittsburgh, Pennsylvania, United States, 15261 United States, Utah Jean Brown Research Salt Lake City, Utah, United States, 84124 United States, Washington Center for Pediatric Dentistry Seattle`, Washington, United States, 98115 Less << |
NCT03740386 | Anesthesia, Local | Not Applicable | Completed | - | - |
Bio Calculators | ||||
Preparing Stock Solutions | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.65mL 0.53mL 0.26mL |
13.25mL 2.65mL 1.32mL |
26.49mL 5.30mL 2.65mL |
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Dissolving Methods |
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:
in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day; The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
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