Phentolamine mesylate (OraVerse), a nonselective a-adrenergic blocking drug, is the first therapeutic agent marketed for the reversal of soft-tissue anaesthesia and the associated functional deficits resulting from an intraoral submucosal injection of a local anaesthetic containing a vasoconstrictor[3]. Phentolamine mesylate (PM) is widely used to reverse local anesthesia after dental procedures. PM substantially reduced the time to recovery of normal sensation and function after local anesthesia in routine dental treatment[4]. Phentolamine leads to an increase in FBM (fetal breathing movements) 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 (electrocortical activity). Promotion of LV-ECoG by catecholamines is mediated via an alpha 1-independent mechanism[5]. Phentolamine mesylate, at dosages from 0.4 to 0.8 mg in adults and adolescents and at dosages from 0.2 to 0.4 mg in children aged 4 to 11 years, has been proven to be safe. Its ability to block a-adrenergic receptors on blood vessels induces vasodilation and enhances the redistribution of the local anesthetic away from the injection site[6].
Phentolamine methanesulfonate salt/甲磺酸酚妥拉明 细胞实验
Cell Line
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.
Mediation by a serotonergic mechanism. J Clin Invest.
Human periodontal ligament fibroblasts (HPDLFs)
25 µM
24 hours or 48 hours
To investigate the effect of phentolamine on LPS-inhibited HPDLF proliferation, results showed that phentolamine significantly ameliorated LPS-inhibited cell proliferation.
Exp Mol Med. 2014 Oct 17;46(10):e118.
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).
Br J Pharmacol. 1984 Mar;81(3):423-5.
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.
Br J Pharmacol. 1990 Sep;101(1):115-20.
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.
Br J Pharmacol. 1992 Sep;107(1):8-14.
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
Br J Pharmacol. 1984 Dec;83(4):965-71.
Phentolamine methanesulfonate salt/甲磺酸酚妥拉明 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Rats
Wistar WI/Ico, Wistar WAG/Rij, Fischer 344
Perfusion and superfusion
1 µM
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.
Br J Pharmacol. 1994 Oct;113(2):363-8
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.
Br J Pharmacol. 1990 Sep;101(1):115-20.
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
Br J Pharmacol. 1984 Dec;83(4):965-71.
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.
Br J Pharmacol. 1984 Mar;81(3):423-5.
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.
United States, North Carolina
... 展开 >>
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 收起 <<
Ischemic Stroke
... 展开 >> High Blood Pressure 收起 <<
Phase 3
Recruiting
February 2019
Australia, New South Wales
... 展开 >>
Royal Prince Alfred Hospital
Recruiting
Sydney, New South Wales, Australia, 2050
Contact: Craig S Anderson, MD +61 2 933 4500 canderson@georgeinstitute.org.au 收起 <<
Australia, New South Wales
... 展开 >>
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 收起 <<
United States, North Carolina
... 展开 >>
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 收起 <<
Ischemic Stroke
... 展开 >> High Blood Pressure 收起 <<
Phase 3
Recruiting
February 2019
Australia, New South Wales
... 展开 >>
Royal Prince Alfred Hospital
Recruiting
Sydney, New South Wales, Australia, 2050
Contact: Craig S Anderson, MD +61 2 933 4500 canderson@georgeinstitute.org.au 收起 <<
Australia, New South Wales
... 展开 >>
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 收起 <<
Terminated(This study was term... 展开 >>inated January 11, 2011 due to low enrollment. This study is not being terminated because of safety or efficacy concerns.) 收起 <<
Terminated(This study was term... 展开 >>inated January 11, 2011 due to low enrollment. This study is not being terminated because of safety or efficacy concerns.) 收起 <<
United States, Utah
... 展开 >>
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 收起 <<
Netherlands
... 展开 >> 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 收起 <<
United States, Pennsylvania
... 展开 >>
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 收起 <<
United States, California
... 展开 >>
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 收起 <<
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