Page last updated: 2024-12-05

lomerizine

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

Lomerizine is a calcium channel blocker with antihistaminic properties. It is used to treat vertigo and dizziness. Lomerizine was first synthesized in the 1970s. It is thought to work by blocking calcium channels in the brain, which helps to reduce the excitability of nerve cells. Lomerizine has been shown to be effective in treating vertigo and dizziness associated with Ménière's disease, vestibular neuritis, and other conditions. It is also being investigated for its potential use in treating other conditions, such as migraine headaches and anxiety disorders.'

lomerizine: used to treat migraines [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID3949
CHEMBL ID29188
CHEBI ID94682
SCHEMBL ID79390
MeSH IDM0148841

Synonyms (45)

Synonym
AB00003587-11
lomerizine
OPREA1_445487
1-(bis(p-fluorophenyl)methyl)-4-(2,3,4-trimethoxybenzyl)piperazine
1-(bis(p-fluorophenyl)-methyl)-4-(2,3,4-trimethoxybenzyl)piperazine
lomerizine [inn]
HMS2090A21
1-(2,3,4-trimethoxybenzyl)-4-(bis(4-fluorophenyl)methyl)piperazine
1-[bis-(4-fluoro-phenyl)-methyl]-4-(2,3,4-trimethoxy-benzyl)-piperazine(lomerizine)
bdbm50095765
CHEMBL29188 ,
1-[bis(4-fluorophenyl)methyl]-4-[(2,3,4-trimethoxyphenyl)methyl]piperazine
101477-55-8
A800395
HMS3264O04
dee37cy4vo ,
unii-dee37cy4vo
FT-0631014
AKOS015895327
lomerizine [mi]
lomerizine [who-dd]
CCG-213815
DL-244
AB00003587-09
SCHEMBL79390
AB00003587-01
DTXSID6048387
JQSAYKKFZOSZGJ-UHFFFAOYSA-N
iomerizine
1-(2,3,4-trimethoxybenzyl)-4-[bis(4-fluorophenyl)methyl]piperazine
AB00003587_12
AB00003587_13
J-000408
sr-01000763880
SR-01000763880-3
CHEBI:94682
piperazine, 1-[bis(4-fluorophenyl)methyl]-4-[(2,3,4-trimethoxyphenyl)methyl]-
NCGC00164543-04
lomerazine
DB14065
1-(bis(4-fluorophenyl)methyl)-4-(2,3,4-trimethoxybenzyl)piperazine
Q6669453
EN300-18414867
AT37184
Z164035568

Research Excerpts

Overview

Lomerizine is a calcium channel blocker that crosses the blood-brain barrier. It is used clinically in the treatment of migraines.

ExcerptReferenceRelevance
"Lomerizine (Lom) is a new generation calcium antagonist, which is mainly used in the treatment of migraine."( Design, synthesis and anti-Chikungunya virus activity of lomerizine derivatives.
Chen, CR; Jin, YS; Liu, XY; Liu, Y; Ma, Y; Meng, QG; Wang, HX, 2023
)
1.88
"Lomerizine is a calcium channel blocker that crosses the blood-brain barrier and is used clinically in the treatment of migraines. "( Lomerizine inhibits LPS-mediated neuroinflammation and tau hyperphosphorylation by modulating NLRP3, DYRK1A, and GSK3α/β.
Cho, J; Hoe, HS; Hwang, JW; Jang, GM; Jeong, YJ; Lee, HJ; Park, JH; Seo, J, 2023
)
3.8

Treatment

ExcerptReferenceRelevance
"Lomerizine treatment decreased HIT-6 scores significantly (P < .01)."( Preventive Treatment with Lomerizine Increases Cerebral Blood Flows during the Interictal Phase of Migraine.
Aoyagi, J; Ebina, J; Hanashiro, S; Ikeda, K; Ishikawa, Y; Iwasaki, Y; Kawabe, K; Kyuzen, M; Miura, K; Morioka, H; Murata, K; Nagasawa, J; Sawada, M; Takazawa, T; Yanagihashi, M, 2018
)
1.5

Pharmacokinetics

ExcerptReferenceRelevance
"A rapid, sensitive and selective high performance liquid chromatography-electrospray ionization-tandem mass spectrometry method (HPLC-ESI-MS/MS) was developed and validated for the determination and pharmacokinetic investigation of lomerizine in human plasma."( Determination of lomerizine in human plasma by liquid chromatography/tandem mass spectrometry and its application to a pharmacokinetic study.
Hu, Y; Liang, J; Liu, T; Ren, Y; Song, G, 2014
)
0.93

Bioavailability

ExcerptReferenceRelevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
diarylmethaneAny compound containing two aryl groups connected by a single C atom.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (12)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
phosphopantetheinyl transferaseBacillus subtilisPotency56.23410.141337.9142100.0000AID1490
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency1.12200.01789.637444.6684AID588834
huntingtin isoform 2Homo sapiens (human)Potency31.62280.000618.41981,122.0200AID1688
gemininHomo sapiens (human)Potency21.13600.004611.374133.4983AID624296
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency17.64070.005612.367736.1254AID624032; AID624044
lamin isoform A-delta10Homo sapiens (human)Potency10.00000.891312.067628.1838AID1487
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Delta-type opioid receptorMus musculus (house mouse)IC50 (µMol)2.43000.00010.729810.0000AID293101
Voltage-dependent L-type calcium channel subunit beta-1Rattus norvegicus (Norway rat)IC50 (µMol)0.09000.08000.09330.1100AID471769
Voltage-dependent calcium channel subunit alpha-2/delta-1Rattus norvegicus (Norway rat)IC50 (µMol)0.09000.08000.09330.1100AID471769
Voltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)IC50 (µMol)2.43000.04004.113710.0000AID293101
Voltage-dependent N-type calcium channel subunit alpha-1BRattus norvegicus (Norway rat)IC50 (µMol)0.09000.08000.32001.0000AID471769
Prostaglandin D2 receptor 2Homo sapiens (human)IC50 (µMol)0.09000.00040.10090.9600AID471769
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (12)

Processvia Protein(s)Taxonomy
modulation of chemical synaptic transmissionVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
response to amyloid-betaVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
chemical synaptic transmissionVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
calcium ion import across plasma membraneVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
chemotaxisProstaglandin D2 receptor 2Homo sapiens (human)
immune responseProstaglandin D2 receptor 2Homo sapiens (human)
G protein-coupled receptor signaling pathwayProstaglandin D2 receptor 2Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayProstaglandin D2 receptor 2Homo sapiens (human)
calcium-mediated signalingProstaglandin D2 receptor 2Homo sapiens (human)
positive regulation of G protein-coupled receptor signaling pathwayProstaglandin D2 receptor 2Homo sapiens (human)
negative regulation of male germ cell proliferationProstaglandin D2 receptor 2Homo sapiens (human)
neuropeptide signaling pathwayProstaglandin D2 receptor 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (11)

Processvia Protein(s)Taxonomy
amyloid-beta bindingVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
voltage-gated calcium channel activityVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
calcium ion bindingVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
protein bindingVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
ATP bindingVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
high voltage-gated calcium channel activityVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
prostaglandin J receptor activityProstaglandin D2 receptor 2Homo sapiens (human)
G protein-coupled receptor activityProstaglandin D2 receptor 2Homo sapiens (human)
prostaglandin D receptor activityProstaglandin D2 receptor 2Homo sapiens (human)
prostaglandin F receptor activityProstaglandin D2 receptor 2Homo sapiens (human)
neuropeptide bindingProstaglandin D2 receptor 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (5)

Processvia Protein(s)Taxonomy
plasma membraneVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
synapseVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
voltage-gated calcium channel complexVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
neuronal cell bodyVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
plasma membraneProstaglandin D2 receptor 2Homo sapiens (human)
plasma membraneProstaglandin D2 receptor 2Homo sapiens (human)
neuron projectionProstaglandin D2 receptor 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (18)

Assay IDTitleYearJournalArticle
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID680311TP_TRANSPORTER: increase in Calcein intracellular accumulation (Calcein: 1 uM, Lomerizine: 10 uM) in K562/DOX cells2001Biological & pharmaceutical bulletin, May, Volume: 24, Issue:5
Increase in doxorubicin cytotoxicity by inhibition of P-glycoprotein activity with lomerizine.
AID471769Blocking of rat N-type calcium channel alpha-1B/alpha-2-delta-1/beta-1b activity expressed in HEK293 cells assessed as whole cell current by whole cell patch clamp assay2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Scaffold-based design and synthesis of potent N-type calcium channel blockers.
AID547622Antitrypanosomal activity against Trypanosoma cruzi amastigotes infected in BESM cells measured after 88 hrs postinfection by HTS assay2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
Image-based high-throughput drug screening targeting the intracellular stage of Trypanosoma cruzi, the agent of Chagas' disease.
AID293103Selectivity for calcium channel Cav2.2 over calcium channel L type2007Bioorganic & medicinal chemistry letters, Feb-01, Volume: 17, Issue:3
Synthesis and SAR of novel 2-arylthiazolidinones as selective analgesic N-type calcium channel blockers.
AID293101Inhibition of calcium channel Cav2.2 in IMR32 cells2007Bioorganic & medicinal chemistry letters, Feb-01, Volume: 17, Issue:3
Synthesis and SAR of novel 2-arylthiazolidinones as selective analgesic N-type calcium channel blockers.
AID547804Selectivity window, ratio of EC50 for BESM cells to EC50 for Trypanosoma cruzi amastigotes infected in BESM cells2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
Image-based high-throughput drug screening targeting the intracellular stage of Trypanosoma cruzi, the agent of Chagas' disease.
AID472027Selectivity ratio of IC50 for rat Voltage-dependent L-type calcium channel to IC50 for rat N-type calcium channel2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Scaffold-based design and synthesis of potent N-type calcium channel blockers.
AID217926Inhibition of [3H]BTX binding to cardiac voltage-gated sodium channel2001Journal of medicinal chemistry, Jan-18, Volume: 44, Issue:2
Medicinal chemistry of neuronal voltage-gated sodium channel blockers.
AID547621Cytotoxicity against BESM cells after 88 hrs by HTS assay2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
Image-based high-throughput drug screening targeting the intracellular stage of Trypanosoma cruzi, the agent of Chagas' disease.
AID472026Blocking of rat Voltage-dependent L-type calcium channel alpha1c/alpha2delta-1/beta1b activity expressed in HEK293 cells assessed as whole cell current by whole cell patch clamp assay2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Scaffold-based design and synthesis of potent N-type calcium channel blockers.
AID293102Inhibition of calcium channel L type in IMR32 cells2007Bioorganic & medicinal chemistry letters, Feb-01, Volume: 17, Issue:3
Synthesis and SAR of novel 2-arylthiazolidinones as selective analgesic N-type calcium channel blockers.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (96)

TimeframeStudies, This Drug (%)All Drugs %
pre-199011 (11.46)18.7374
1990's29 (30.21)18.2507
2000's22 (22.92)29.6817
2010's26 (27.08)24.3611
2020's8 (8.33)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 34.98

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index34.98 (24.57)
Research Supply Index4.64 (2.92)
Research Growth Index4.78 (4.65)
Search Engine Demand Index46.75 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (34.98)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials3 (3.00%)5.53%
Reviews6 (6.00%)6.00%
Case Studies6 (6.00%)4.05%
Observational1 (1.00%)0.25%
Other84 (84.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]