Mianserin Hydrochloride is an potent antagonist of H1 histamine receptor and 5-HT serotonin receptors, used for the treatment of depression. Mianserin (2 mg/kg s.c.) causes a modest increase of DOPAC (Dihydroxyphenylacetic acid) levels up to about 30% above base-line, which is statistically significant when compared to saline. Mianserin increases extracellular norepinephnne, but a comparison with desipramine and idazoxan showed that both NE reuptake inhibition and alpha-2 autoreceptor blockade contributed to the mianserin-induced increase in extracellular norepinephnne[3]. Mianserin (1, 5 and 10 mg/kg, SC) dose-dependently increases up to about 6 times extracellular dopamine in the medial prefrontal cortex of the rat. Mianserin also dose-dependently increases extracellular noradrenaline in the prefrontal cortex. Mianserin also dose-dependently increased extracellular noradrenaline in the prefrontal cortex[4]. Rats were chronically treated with mianserin (10 mg/kg i.p.) or eltoprazine (1 mg/kg i.p.) and were tested in the elevated plus-maze test for anxiety. Mianserin and eltoprazine displayed opposite effects in the elevated plus-maze: mianserin induced anxiolytic-like effects, while eltoprazine showed anxiogenic-like ones[5].
Mianserin HCl/盐酸米安色林 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Rat anococcygeus muscle
1 nM to 10 µM
10 min
Mianserin inhibited the accumulation of noradrenaline, similar to nortriptyline
Br J Pharmacol. 1980 Feb;68(2):241-50.
Human peripheral blood mononuclear cells
80 µM
18 hours
To evaluate the inhibitory effect of MN-1 on TLR8-induced TNF production, results showed that MN-1 significantly inhibited TNF production.
Front Immunol. 2019 May 24;10:1167.
HCS-2/8 human chondrosarcoma cells
10 µM
24 hours
Screening for drugs that inhibit Rspo2-activated Wnt/β-catenin signaling, found that mianserin dose-dependently suppressed TOPFlash reporter activity
Sci Rep. 2019 Feb 26;9(1):2808.
Chinese hamster cells (B14)
200 µM
24 hours
To evaluate the effect of mianserin hydrochloride complexes with heptakis (2,6-di-O-methyl)-β-cyclodextrin on cell viability. Results showed that cells treated with the complexes had lower viability (higher toxicity) compared to mianserin alone.
Int J Mol Sci. 2021 Aug 30;22(17):9419.
Mianserin HCl/盐酸米安色林 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Sprague-Dawley rats
Anesthetized and pithed rats
Intravenous injection
0.3-3.0 mg/kg
Single dose
To study the effects of mianserin on blood pressure responses evoked by acetylcholine, histamine, and 5-hydroxytryptamine. Results showed that mianserin did not modify the hypotensive effects of acetylcholine but inhibited the vasodepressor responses to histamine and antagonized the pressor effects of 5-hydroxytryptamine.
Br J Pharmacol. 1981 Sep;74(1):143-8
Sprague-Dawley pups
Ethanol-induced locomotor activity model in preweanling rats
Intraperitoneal injection
2.5 or 5 mg/kg
Single administration, locomotor activity assessed 30 minutes later
Mianserin at 2.5 mg/kg significantly attenuated ethanol-induced locomotor stimulation without affecting locomotor activity in water controls
Pharmacol Biochem Behav. 2011 Nov;100(1):81-5
Wistar/ST rats
Osteoarthritis model induced by surgical destabilization of the medial meniscus (DMM)
Intraarticular injection
50 μM
Once weekly for 8 weeks
Evaluating the effect of mianserin on a rat OA model, found that mianserin reduced β-catenin expression and prevented OA progression
Sci Rep. 2019 Feb 26;9(1):2808.
Wistar rats
6-hydroxydopamine-induced fall in rat heart noradrenaline levels
Intraperitoneal injection
94.0 μmol/kg
Single dose, 30 min before 6-OHDA
Mianserin was active in this model, but its ability to block the 6-hydroxydopamine-induced fall in rat heart noradrenaline concentration was appreciably less than that of the tricyclics studied.
United States, Alabama
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Tuscalossa VA Mental Health Clinic
Tuscaloosa, Alabama, United States, 35404
United States, California
Harbor UCLA Family Health Care Center
Harbor City, California, United States, 90710
UCLA Internal Medicine Clinic
Los Angeles, California, United States, 90024
Veterans Affairs Medical Center/FIRM Primary Care Clinic
San Diego, California, United States, 92161
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Northwestern Psychiatric Outpatient Treatment Care Center
Chicago, Illinois, United States, 60611
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Clinical Research Institute
Wichita, Kansas, United States, 67214
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MGH/Northshore Medical Center (Salem Psychiatric Facility)
Salem, Massachusetts, United States, 01970
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General Psychiatric Ambulatory Clinic
Ann Arbor, Michigan, United States, 48105
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Irving Goldman Primary Care at North Shore Hospital
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Chapel Hill, North Carolina, United States, 27599-7160
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Bellefield Clinic of WPIC
Pittsburgh, Pennsylvania, United States, 15213
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Vine Hill Community Clinic
Nashville, Tennessee, United States, 37212
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UT Southwestern Family Medicine Clinic
Dallas, Texas, United States, 75390
United States, Virginia
VCU Outpatient Psychiatry Clinic
Richmond, Virginia, United States, 23298 收起 <<
Germany
... 展开 >> Department of Psychiatry and Psychotherapy, University Erlangen-Nuremberg
Recruiting
Erlangen, Bavaria, Germany, 91054
Contact: Stefan Bleich, MD 004991318534262 stefan.bleich@uk-erlangen.de
Principal Investigator: Stefan Bleich, MD
Sub-Investigator: Julia Wilhelm, MD
Sub-Investigator: Helge Frieling, MD 收起 <<
Brazil
... 展开 >> Clinics Hospital, Ribeirão Preto Medical School, University of São Paulo
Not yet recruiting
Ribeirão Preto, São Paulo, Brazil, 14048900
Contact: Nereida KC Lima, MD, PhD +5516992770522 nereida@fmrp.usp.br 收起 <<
United States, California
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San Francisco Department of Public Health, Substance Use Research Unit
San Francisco, California, United States, 94102 收起 <<
United States, New Hampshire
... 展开 >>
Dartmouth Medical School Department of Psychiatry's Addition Research Center
Bedford, New Hampshire, United States, 03110
Dartmouth Medical School Department of Psychiatry's Addiction Research Center
Hanover, New Hampshire, United States, 03755 收起 <<
Malaysia
... 展开 >> University Malaya Medical Centre
Recruiting
Kuala Lumpur, Malaysia, 50603
Contact: Chong Guan Ng, MBBS, MPM 0379492068 chong_guan1975@yahoo.co.uk
University Malaya Medical Centre
Not yet recruiting
Kuala Lumpur, Malaysia, 59100
Contact: Chong Guan Ng, MBBS, MPM 60379604367 chong_guan@hotmail.com
Principal Investigator: Chong Guan Ng, MBBS, MPM 收起 <<
Malaysia
... 展开 >> University Science Malaysia
Recruiting
Kota bharu, Kelantan, Malaysia, 16010
Contact: Vicknasingam B Kasinather, PhD 6046532140 vickna@usm.my
Contact: Imran Ahmad 6097676603 profimran@usm.my 收起 <<
Terminated(This trial was stop... 展开 >>ped prematurely due to the Sponsor's decision not to continue the development of esmertazapine for this indication.) 收起 <<
Terminated(This trial was stop... 展开 >>ped prematurely due to the Sponsor's decision not to continue the development of esmertazapine for this indication.) 收起 <<
United States, New Mexico
... 展开 >>
University of New Mexico Cancer Center @ Lovelace Medical Center
Albuquerque, New Mexico, United States, 87102
Universtiy of New Mexico - Cancer Center
Albuquerque, New Mexico, United States, 87106 收起 <<
Korea, Republic of
... 展开 >>
Samsung Medical Center
Recruiting
Kangnam, Seoul, Korea, Republic of, 135-710
Contact: Samsung Medical Center Kim, phD, MD 82-2-3410-3582 dohkwan.kim@samsung.com 收起 <<
Brazil
... 展开 >> Brasilia University
Recruiting
Brasilia, Distrito Federal, Brazil, 70840
Contact: Francisca M Scoralick franciscascoralick@gmail.com
Sub-Investigator: Francisca M Scoralick 收起 <<
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... 展开 >> Sube Banerjee
Recruiting
Brighton, Sussex, United Kingdom, BN1 9RY
Contact: Sube Banerjee, MD 01273877896 s.banerjee@bsms.ac.uk
Principal Investigator: Naji Tabet, MD
Principal Investigator: Chris Fox, MD
Principal Investigator: Alan Thomas, MD
Principal Investigator: Ross Dunne, MD
Principal Investigator: Gill Livingston, MD
Principal Investigator: Peter Bentham, MD
Principal Investigator: Annabel Price, MD
Principal Investigator: Ramin Nilforooshan, MD
Principal Investigator: Carol Bannister, MD
Principal Investigator: Sushanth Kamath, MD 收起 <<
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