Page last updated: 2024-12-04

cloperastine

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

Description

Cloperastine is an antihistamine and antitussive drug. It is a competitive antagonist of histamine at H1 receptors and also exhibits anticholinergic properties. Cloperastine is used for the treatment of allergic rhinitis, urticaria, and cough. Its mechanism of action involves blocking the release of histamine from mast cells and inhibiting the activity of cholinesterase. Cloperastine has been studied for its potential therapeutic effects in various conditions, including allergic asthma, chronic obstructive pulmonary disease (COPD), and Parkinson's disease. Research on cloperastine focuses on its effectiveness, safety, and potential for drug interactions.'

cloperastine: RN given refers to parent cpd [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID2805
CHEMBL ID415087
CHEBI ID94448
SCHEMBL ID284715
MeSH IDM0120036

Synonyms (83)

Synonym
AKOS005577799
BRD-A80908310-003-05-4
piperidine, 1-[2-[(4-chlorophenyl)phenylmethoxy]ethyl]-
cloperastine
KBIO1_000840
DIVK1C_000840
3703-76-2
cloperastine (inn)
D03557
SPECTRUM_001570
IDI1_000840
PRESTWICK2_000793
SPECTRUM5_001448
BSPBIO_000926
BPBIO1_001020
1-{2-((p-chloro-alpha-phenylbenzyl)oxy)ethyl}piperidine
einecs 223-042-3
cloperastina [inn-spanish]
1- 2-((p-chloro-alpha-phenylbenzyl)oxy)ethyl piperidine
piperidine, 1-(2-((p-chloro-alpha-phenylbenzyl)oxy)ethyl)-
cloperastinum [inn-latin]
brn 0275589
piperidine, 1-(2-((4-chlorophenyl)phenylmethoxy)ethyl)-
cloperastine [inn]
ht 11
1-(2-((4-chlorophenyl)phenylmethoxy)ethyl)piperidine
AB00053681
PRESTWICK3_000793
BSPBIO_003430
KBIO2_004618
KBIOGR_001447
KBIO2_007186
KBIO3_002933
KBIO2_002050
KBIOSS_002050
SPECTRUM3_001895
SPBIO_001592
SPECTRUM2_001596
PRESTWICK1_000793
NINDS_000840
PRESTWICK0_000793
SPECTRUM4_000844
SPBIO_002865
NCGC00178069-01
NCGC00178069-02
ht-11
nsc-758635
CHEMBL415087
VU0244436-2
1-[2-[(4-chlorophenyl)-phenylmethoxy]ethyl]piperidine
1-{2-[(4-chlorophenyl)(phenyl)methoxy]ethyl}piperidine
NCGC00178069-03
cloperastinum
unii-69m5l7bxek
nsc 758635
cloperastina
5-20-02-00105 (beilstein handbook reference)
69m5l7bxek ,
STK646871
cloperastine [who-dd]
cloperastine [mart.]
cloperastine [mi]
1-(2-((p-chloro-.alpha.-phenylbenzyl)oxy)ethyl)piperidine
SCHEMBL284715
DTXSID7048532
1-(2-[(4-chlorophenyl)(phenyl)methoxy]ethyl)piperidine #
FLNXBVJLPJNOSI-UHFFFAOYSA-N
piperidine, 1-(2-((p-chloro-.alpha.-phenylbenzyl)oxy)ethyl)-
1-(2-[(p-chloro-.alpha.-phenylbenzyl)oxy]ethyl)piperidine
1-(2-((4-chlorophenyl)(phenyl)methoxy)ethyl)piperidine
AB00053681_08
DB09002
CHEBI:94448
1-[2-[(4-chlorophenyl)-phenyl-methoxy]ethyl]piperidine
piperidine, 1-[2-[(4-chlorophenyl)phenylmethoxy]ethyl]-, hydrochloride
SBI-0051861.P002
FT-0746924
Q2055825
BRD-A80908310-003-08-8
cloperastine-fendizoate
bdbm50237287
EN300-18567806
levocloperastineih

Research Excerpts

Overview

Cloperastine is an antitussive drug, which can be received as an over-the-counter cold medicine. It is effective for the treatment of cough in patients of all ages.

ExcerptReferenceRelevance
"Cloperastine is an antitussive drug, which can be received as an over-the-counter cold medicine. "( Effects of the antitussive drug cloperastine on ventricular repolarization in halothane-anesthetized guinea pigs.
Fujiwara, K; Namekata, I; Ohtsuki, A; Oka, T; Takahara, A; Tanaka, H, 2012
)
2.11
"Levocloperastine is an effective antitussive agent for the treatment of cough in patients of all ages."( Levocloperastine in the treatment of chronic nonproductive cough: comparative efficacy versus standard antitussive agents.
Aliprandi, P; Bernorio, S; Carrara, M; Castelli, C; Dell'Abate, E, 2004
)
1.36

Dosage Studied

ExcerptRelevanceReference
" After cerebral infarction, intravenous dosing of saline had no effect on these parameters."( Ameliorating effects of cloperastine on dysfunction of the urinary bladder caused by cerebral infarction in conscious rats.
Shirasaki, T; Soeda, F; Takahama, K; Yamamoto, G, 2009
)
0.66
[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 (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Solute carrier family 22 member 1 Homo sapiens (human)IC50 (µMol)14.89000.21005.553710.0000AID1442001
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (29)

Processvia Protein(s)Taxonomy
xenobiotic metabolic processSolute carrier family 22 member 1 Homo sapiens (human)
neurotransmitter transportSolute carrier family 22 member 1 Homo sapiens (human)
serotonin transportSolute carrier family 22 member 1 Homo sapiens (human)
establishment or maintenance of transmembrane electrochemical gradientSolute carrier family 22 member 1 Homo sapiens (human)
organic cation transportSolute carrier family 22 member 1 Homo sapiens (human)
quaternary ammonium group transportSolute carrier family 22 member 1 Homo sapiens (human)
prostaglandin transportSolute carrier family 22 member 1 Homo sapiens (human)
monoamine transportSolute carrier family 22 member 1 Homo sapiens (human)
putrescine transportSolute carrier family 22 member 1 Homo sapiens (human)
spermidine transportSolute carrier family 22 member 1 Homo sapiens (human)
acetylcholine transportSolute carrier family 22 member 1 Homo sapiens (human)
dopamine transportSolute carrier family 22 member 1 Homo sapiens (human)
norepinephrine transportSolute carrier family 22 member 1 Homo sapiens (human)
thiamine transportSolute carrier family 22 member 1 Homo sapiens (human)
xenobiotic transportSolute carrier family 22 member 1 Homo sapiens (human)
epinephrine transportSolute carrier family 22 member 1 Homo sapiens (human)
serotonin uptakeSolute carrier family 22 member 1 Homo sapiens (human)
norepinephrine uptakeSolute carrier family 22 member 1 Homo sapiens (human)
thiamine transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
metanephric proximal tubule developmentSolute carrier family 22 member 1 Homo sapiens (human)
purine-containing compound transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
dopamine uptakeSolute carrier family 22 member 1 Homo sapiens (human)
monoatomic cation transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
transport across blood-brain barrierSolute carrier family 22 member 1 Homo sapiens (human)
(R)-carnitine transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
acyl carnitine transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
spermidine transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
cellular detoxificationSolute carrier family 22 member 1 Homo sapiens (human)
xenobiotic transport across blood-brain barrierSolute carrier family 22 member 1 Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (19)

Processvia Protein(s)Taxonomy
acetylcholine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
neurotransmitter transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
dopamine:sodium symporter activitySolute carrier family 22 member 1 Homo sapiens (human)
norepinephrine:sodium symporter activitySolute carrier family 22 member 1 Homo sapiens (human)
protein bindingSolute carrier family 22 member 1 Homo sapiens (human)
monoamine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
secondary active organic cation transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
organic anion transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
organic cation transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
prostaglandin transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
pyrimidine nucleoside transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
thiamine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
putrescine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
spermidine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
quaternary ammonium group transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
toxin transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
identical protein bindingSolute carrier family 22 member 1 Homo sapiens (human)
xenobiotic transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
(R)-carnitine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (7)

Processvia Protein(s)Taxonomy
plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
basal plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
membraneSolute carrier family 22 member 1 Homo sapiens (human)
basolateral plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
apical plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
lateral plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
presynapseSolute carrier family 22 member 1 Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (9)

Assay IDTitleYearJournalArticle
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.
AID1409611AUC (cytotoxicity %) of compound against Vero E6 cells by MTT assay.2020Nature, 07, Volume: 583, Issue:7816
A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
AID1409608AUC (viral infection %) for SARS-CoV-2 in the Vero E6 cell line at 48 h by immunofluorescence-based assay (detecting the viral NP protein in the nucleus of the Vero E6 cells).2020Nature, 07, Volume: 583, Issue:7816
A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
AID1409613Selectivity ratio: ratio of AUC (viral infection %) of SARS-CoV-2 in the Vero E6 cell line compared to AUC (cytotoxicity %) of compound against Vero E6 cells by MTT assay.2020Nature, 07, Volume: 583, Issue:7816
A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
AID311932Inhibition of ASM in human H4 cells assessed as residual activity at 10 uM2008Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2
Identification of new functional inhibitors of acid sphingomyelinase using a structure-property-activity relation model.
AID1409607IC50 for antiviral activity against SARS-CoV-2 in the Vero E6 cell line at 48 h by immunofluorescence-based assay (detecting the viral NP protein in the nucleus of the Vero E6 cells).2020Nature, 07, Volume: 583, Issue:7816
A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
AID1409614Overall antiviral activity against SARS-CoV-2 (isolate France/IDF0372/2020) in the Vero E6 cell line at 48 h based on three assays 1) detection of viral RNA by qRT-PCR (targeting the N-gene), 2) plaque assay using lysate 3 days after addition of compound 2020Nature, 07, Volume: 583, Issue:7816
A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
AID1409609Cytotoxicity of compound against Vero E6 cells by MTT assay.2020Nature, 07, Volume: 583, Issue:7816
A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
AID1442001Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assay2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Discovery of Competitive and Noncompetitive Ligands of the Organic Cation Transporter 1 (OCT1; SLC22A1).
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (24)

TimeframeStudies, This Drug (%)All Drugs %
pre-19903 (12.50)18.7374
1990's0 (0.00)18.2507
2000's4 (16.67)29.6817
2010's9 (37.50)24.3611
2020's8 (33.33)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 62.15

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 very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index62.15 (24.57)
Research Supply Index3.47 (2.92)
Research Growth Index4.66 (4.65)
Search Engine Demand Index100.18 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (62.15)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials4 (14.81%)5.53%
Reviews4 (14.81%)6.00%
Case Studies1 (3.70%)4.05%
Observational0 (0.00%)0.25%
Other18 (66.67%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]