Meclizine dihydrochloride, is a piperazine-derived histamine H1 antagonist, and has been frequently used for prevention and treatment of vomiting and nausea. In primary bone marrow-derived macrophages (BMMs), meclizine reduced osteoclast formation and bone resorption in a dose-dependent manner[3]. Meclizine is also an agonist of human pregnane X receptor (PXR). The inhibition of human liver microsomal testosterone 6β-hydroxylation by meclizine occurred by a mixed mode and with an apparent Ki of 31 ± 6μM[4]. Meclizine is a first generation antihistamine that is used largely to treat vertigo and motion sickness. It has not been linked to instances of clinically apparent acute liver injury[5]. Meclizine protected against 6-hydroxydopamine-induced apoptosis and cell death in both SH-SY5Y cells and rat primary cortical cultures. It increases the level of 6-phosphofructo-2-kinase/fructose-2,6-biphosphatase 3 (PFKFB3), which activates phosphofructokinase, a rate-determining enzyme of glycolysis[6].
Meclizine 2HCl/盐酸美克洛嗪 细胞实验
Cell Line
Concentration
Treated Time
Description
References
ST HdhQ111/111 striatal cells
50 μM
24 hours
Measure cell viability, showing that Meclizine and its enantiomers significantly improved the viability of striatal cells under serum deprivation conditions.
Stroke. 2024 May;55(5):1370-1380
LLC-PK1 cells
25 μM
17 hours
To evaluate the protective effect of Meclizine 2HCl on LLC-PK1 cells, results showed that pretreatment significantly reduced LDH release induced by chemical hypoxia.
EBioMedicine. 2015 Jul 29;2(9):1090-101
HK-2 cells
25 μM
17 hours
To evaluate the protective effect of Meclizine 2HCl on HK-2 cells, results showed that pretreatment significantly reduced LDH and cytochrome c release induced by chemical hypoxia.
EBioMedicine. 2015 Jul 29;2(9):1090-101
Astrocytes
30 μM
Meclizine induces a gradual increase in ECAR and a decrease in OCR in astrocytes, reflecting their ability to divert energy production away from oxidative phosphorylation.
Free Radic Biol Med. 2016 Oct;99:20-31
Dorsal root ganglion neurons
30 μM (short-term treatment for 2.5 h) or 15 μM (long-term treatment for 16 h)
2.5 h or 16 h
Meclizine rapidly enhances glycolysis in DRG neurons without altering mitochondrial respiration. Under hypoxic conditions, meclizine protects neurons from hypoxia-induced mitochondrial compromise by preventing ATP depletion, preserving NADPH and glutathione stores, curbing ROS, and attenuating mitochondrial clustering.
Free Radic Biol Med. 2016 Oct;99:20-31
human pluripotent stem cell-derived cardiomyocytes (hPSC-CMs)
0.5 µM
3 hours
Meclizine significantly increased ATP levels in hPSC-CMs, mitigating cell death and abnormal calcium handling induced by SARS-CoV-2 genes Nsp6, Nsp8, and M.
Stem Cell Res Ther. 2023 Sep 13;14(1):249
Meclizine 2HCl/盐酸美克洛嗪 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Mice
Transient middle cerebral artery occlusion (MCAO) model
Intraperitoneal injection
100 mg/kg
Two doses, 17 hours and 3 hours before MCAO
Evaluate the effect of Meclizine on anoxic depolarization (AD) latency, cerebral blood flow (CBF), and infarct volume after MCAO. Results showed that Meclizine significantly delayed AD onset, reduced infarct volume, and did not affect CBF.
Stroke. 2024 May;55(5):1370-1380
C57BL/6 mice
Kidney ischemia-reperfusion injury model
Intraperitoneal injection
100 mg/kg
17 and 3 hours before
To evaluate the protective effect of Meclizine 2HCl on kidney ischemia-reperfusion injury, results showed that pretreatment significantly reduced serum creatinine levels, tubular necrosis, and inflammation.
EBioMedicine. 2015 Jul 29;2(9):1090-101
Rats
Acute unilateral vestibular loss model
Intraperitoneal injection
5.2 mg/kg
Single dose
Evaluate the effect of Meclizine on spontaneous nystagmus, results showed minimal effects of Meclizine alone on nystagmus.
Israel
... 展开 >> Israeli Navy Medical Institute
Recruiting
Haifa, Israel
Contact: Dror Tal, PhD +972549096080 tldror1@gmail.com
Sub-Investigator: Daniel Lagami, BSc 收起 <<
Brazil
... 展开 >> Clinilive
Not yet recruiting
Maringá, Paraná, Brazil
Contact: Antonio Carlos da Silva 55 44 30293004
Principal Investigator: Antonio Carolos da Silva
Irmandade da Santa Casa de Misericórdia de São Paulo
Recruiting
São Paulo, SP, Brazil
Contact: Monica Alcantra 55 11 21767235
Principal Investigator: José Eduardo Lutaif Dolci
Alergoalpha
Not yet recruiting
Barueri, São Paulo, Brazil, 06454010
Contact: Thainara Bisognini 55 11 46882251
Principal Investigator: Karina Tavares
Pesquisare Saude S/S Ltda
Not yet recruiting
Santo André, São Paulo, Brazil, 09080110
Contact: Amanda Faulhaber 55 11 44273339
Principal Investigator: Amanda Faulhaber
Clinica de Alergia MarttiAntila
Not yet recruiting
Sorocaba, São Paulo, Brazil, 18040425
Contact: Simone Fernandes 55 15 35194909
Principal Investigator: Martti Anton Antila
ISPEM
Not yet recruiting
São José dos Campos, São Paulo, Brazil, 12243280
Contact: Renata Bolsolani 55 12 39131789
Principal Investigator: Marcio Antonio Pereira
CCBR SP
Not yet recruiting
São Paulo, Brazil, 04063001
Contact: Norton Sayeg, PhD 5511 43064691
Principal Investigator: Norton Sayeg, PhD 收起 <<
United States, North Carolina
... 展开 >>
Duke Center for Nicotine and Smoking Cessation Research
Charlotte, North Carolina, United States, 28210
Duke Center for Nicotine and Smoking Cessation Research
Durham, North Carolina, United States, 27705
Duke Center for Nicotine and Smoking Cessation Research
Raleigh, North Carolina, United States, 27609
Duke Center for Nicotine and Smoking Cessation Research
Winston-Salem, North Carolina, United States, 27103 收起 <<
United States, Texas
... 展开 >>
Baylor Clinic
Recruiting
Houston, Texas, United States, 77030
Contact: Brandon Smaglo, MD 713-798-3750 smaglo@bcm.edu
Baylor St. Luke's Medical Center
Recruiting
Houston, Texas, United States, 77030
Contact: Brando Smaglo, MD 713-798-3750 smaglo@bcm.edu
Dan L. Duncan Cancer Center at Baylor College of Medicine
Recruiting
Houston, Texas, United States, 77030
Contact: Clinical Trials Office - Dan L. Duncan Cancer Center at Baylor 713-798-1297 收起 <<
搜索
