Page last updated: 2024-12-05

brompheniramine

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

Description

Brompheniramine is an antihistamine that is used to treat allergic symptoms such as sneezing, runny nose, itchy eyes, and hives. It is available over-the-counter (OTC) and by prescription. Brompheniramine is a competitive antagonist of histamine at H1 receptors. It works by blocking the effects of histamine, a chemical that is released by the body in response to an allergen. When histamine binds to H1 receptors, it causes the symptoms of an allergic reaction. Brompheniramine prevents histamine from binding to these receptors, thus relieving allergic symptoms. It is synthesized by a multi-step process involving various chemical reactions, including alkylation, acylation, and cyclization. The synthesis of brompheniramine typically starts with a substituted pyrimidine derivative, followed by a series of reactions to introduce the desired substituents and form the final compound. Brompheniramine is effective in treating allergic rhinitis, urticaria, and other allergic conditions. It is also used to prevent motion sickness. It is studied to understand its pharmacokinetic properties, safety profile, and potential for therapeutic applications. Studies are also conducted to investigate its interaction with other medications and its effectiveness in treating specific allergic conditions.'

Brompheniramine: Histamine H1 antagonist used in treatment of allergies, rhinitis, and urticaria. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

brompheniramine : Pheniramine in which the hydrogen at position 4 of the phenyl substituent is substituted by bromine. A histamine H1 receptor antagonist, brompheniramine is used (commonly as its maleate salt) for the symptomatic relief of allergic conditions, including rhinitis and conjunctivitis. [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]

Cross-References

ID SourceID
PubMed CID6834
CHEMBL ID811
CHEBI ID3183
SCHEMBL ID4814
MeSH IDM0002955

Synonyms (114)

Synonym
AC-15955
brompheniraminum
bromfeniramina
BRD-A68723818-050-05-1
SPECTRUM5_001537
PRESTWICK2_000475
LOPAC0_000201
DIVK1C_006846
3-(4-bromophenyl)-n,n-dimethyl-3-pyridin-2-ylpropan-1-amine
SPECTRUM_001682
PDSP1_000146
BSPBIO_002641
BSPBIO_000610
OPREA1_690847
PRESTWICK3_000475
PDSP2_000145
BPBIO1_000672
D07543
brompheniramine (inn)
brotane (tn)
antihistamine compound
AB00053703
86-22-6
C06857
brompheniramine
[3-(4-bromophenyl)-3-(2-pyridyl)propyl]dimethylamine
3-(4-bromophenyl)-n,n-dimethyl-3-(2-pyridyl)propan-1-amine
2-pyridinepropanamine, .gamma.-(4-bromophenyl)-n,n-dimethyl-
[3-(4-bromo-phenyl)-3-pyridin-2-yl-propyl]-dimethyl-amine
1-(p-bromophenyl)-1-(2-pyridyl)-3-dimethylaminopropane
2-(p-bromo-alpha-(2-dimethylaminoethyl)benzyl)pyridine
DB00835
3-(4-bromophenyl)-n,n-dimethyl-3-(2-pyridinyl)-1-propanamine
3-(p-bromophenyl)-3-(2-pyridyl)-n,n-dimethylpropylamine
brompheniraminum [inn-latin]
bromfeniramina [inn-spanish]
pyridine, 2-(p-bromo-alpha-(2-(dimethylamino)ethyl)benzyl)-
2-pyridinepropanamine, gamma-(4-bromophenyl)-n,n-dimethyl-
hsdb 3017
ilvin
einecs 201-657-8
parabromdylamine
gamma-(4-bromophenyl)-n,n-dimethyl-2-pyridinepropanamine
brompheniramine [inn:ban]
KBIO1_001790
KBIOGR_001554
KBIO2_002162
KBIO3_001861
KBIO2_004730
KBIOSS_002162
KBIO2_007298
SPBIO_001619
SPBIO_002549
SPECPLUS_000750
SPECTRUM2_001610
PRESTWICK0_000475
SPECTRUM3_000981
SPECTRUM4_001107
PRESTWICK1_000475
NCGC00089782-02
NCGC00015146-07
CHEMBL811 ,
chebi:3183 ,
bromfed
brotane
bromfenex
L001031
3-(4-bromophenyl)-n,n-dimethyl-3-(pyridin-2-yl)propan-1-amine
STL058559
bdbm50017666
parabromodylamine
CCG-204296
AKOS005711313
NCGC00015146-05
NCGC00015146-08
NCGC00015146-04
unii-h57g17p2fn
h57g17p2fn ,
FT-0603299
gtpl7133
[3-(4-bromophenyl)-3-(pyridin-2-yl)propyl]dimethylamine
brompheniramine [who-dd]
brompheniramine [hsdb]
brompheniramine [vandf]
brompheniramine [inn]
brompheniramine [mi]
156428-33-0
SCHEMBL4814
drauxin (salt/mix)
dimetane (salt/mix)
pyridine, 2-[p-bromo-.alpha.-[2-(dimethylamino)ethyl]benzyl]-
ZDIGNSYAACHWNL-UHFFFAOYSA-N
bromopheniramine
2-[p-bromo-.alpha.-[2-(dimethylamino)ethyl]benzyl]pyridine
allent (salt/mix)
HMS3604F03
AB00053703_20
AB00053703_19
DTXSID5022691
dexbrompheniramine maleate salt
dexbrompheniramine brompheniramine
SBI-0050189.P003
FT-0772799
Q2606497
(+/-)-brompheniramine;bromphen; brompheniramine; parabromdylamine; parabromodylamine
BRD-A68723818-050-18-4
SDCCGSBI-0050189.P004
NCGC00015146-21
NCGC00015146-17
(6r,7r)-7-amino-8-oxo-3-(1-propenyl)-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylicacid
()-brompheniramine;bromphen; brompheniramine; parabromdylamine; parabromodylamine
EN300-18563906
CS-0013144
HY-B0480A

Research Excerpts

Effects

ExcerptReferenceRelevance
"Brompheniramine has been widely used in the treatment of allergic rhinitis and other disorders during the past 4 decades. "( The clinical pharmacology of brompheniramine in children.
Gu, X; Kapur, S; Roberts, JR; Simons, FE; Simons, KJ, 1999
)
2.04

Treatment

ExcerptReferenceRelevance
"Treatment with brompheniramine was associated with the adverse effects of somnolence (n = 3) and confusion (n = 1)."( Efficacy of brompheniramine maleate for the treatment of rhinovirus colds.
Druce, HM; Gwaltney, JM, 1997
)
1.02

Toxicity

ExcerptReferenceRelevance
" Ten asthmatic children who reported a feeling of chest tightness and subsequent wheezing after taking a preparation containing brompheniramine maleate were studied in addition to 10 control asthmatic children who reported no such adverse effect."( Adverse effects of brompheniramine on pulmonary function in a subset of asthmatic children.
Schuller, DE, 1983
)
0.8
"Many adverse drug reactions are caused by the cytochrome P450 (CYP)-dependent activation of drugs into reactive metabolites."( Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.
Jones, LH; Nadanaciva, S; Rana, P; Will, Y, 2016
)
0.43

Pharmacokinetics

ExcerptReferenceRelevance
"This article reviews clinical pharmacokinetic data on the H1-receptor antagonists, commonly referred to as the antihistamines."( Clinical pharmacokinetics of H1-receptor antagonists (the antihistamines).
Paton, DM; Webster, DR,
)
0.13
" The serum elimination half-life values of these agents are variable: a few hours for terfenadine and triprolidine; about 9 hours for cetirizine, azatadine, and loratadine; from 20 to 25 hours for hydroxyzine, chlorpheniramine, and brompheniramine; and from 5 to 14 days for astemizole."( The comparative pharmacokinetics of H1-receptor antagonists.
Chung, M; Simons, FE; Simons, KJ; Yeh, J, 1987
)
0.46
" The mean serum half-life value was 24."( The pharmacokinetics and antihistaminic effects of brompheniramine.
Frith, EM; Simons, FE; Simons, KJ, 1982
)
0.52
"To evaluate the clinical efficacy, tolerance and pharmacokinetic properties of zimelidine in elderly people, twelve hospitalized depressed patients with a mean age of 80 years were included in a clinical trial."( Zimelidine to geriatric patients: a pharmacokinetic and clinical study.
Björnsson, G; Dehlin, O; Lundström, J, 1981
)
0.26
" Pharmacokinetic investigations have shown the drug to be highly bound to blood proteins, mainly serum albumin, and to have a low brain uptake, explaining its lack of sedative effects."( Molecular properties and pharmacokinetic behavior of cetirizine, a zwitterionic H1-receptor antagonist.
Carrupt, PA; Jolliet, P; Morin, C; Morin, D; Pagliara, A; Rihoux, JP; Testa, B; Tillement, JP; Urien, S, 1998
)
0.3

Bioavailability

ExcerptReferenceRelevance
" Bioavailability of pseudoephedrine was 91% for fed relative to fasted treatment; for brompheniramine it was 89%."( Effect of food on bioavailability of pseudoephedrine and brompheniramine administered from a gastrointestinal therapeutic system.
Chao, ST; Coen, P; Knowles, M; Pinson, D; Place, V; Prather, D; Pruitt, B, 1991
)
0.75
" For most of these drugs, the absolute bioavailability is unknown because no intravenous formulations are available for comparative purposes."( The comparative pharmacokinetics of H1-receptor antagonists.
Chung, M; Simons, FE; Simons, KJ; Yeh, J, 1987
)
0.27
" In addition, the major bioavailability parameters (Cmin, Cmax, tmax, and AUC) for days 6 and 7 of dosing were determined and statistically evaluated."( Steady-state bioavailability of dexbrompheniramine and pseudoephedrine from a repeat-action combination tablet.
Digiore, C; Gural, R; Kim, HK; Lim, J; Lin, CC; Symchowicz, S, 1985
)
0.55
" The results obtained may indicate a reduction in the rate of metabolism for zimelidine in the elderly, possibly combined with increased total bioavailability of the drug."( Zimelidine to geriatric patients: a pharmacokinetic and clinical study.
Björnsson, G; Dehlin, O; Lundström, J, 1981
)
0.26
" It appears that zimelidine is completely absorbed from the gastrointestinal tract and "first-pass metabolism" in the liver reduces the bioavailability to 50%."( Pharmacokinetics of zimelidine in humans--plasma levels and urinary excretion of zimelidine and norzimelidine after intravenous and oral administration of zimelidine.
Chaturvedi, S; Love, BL; Moore, RG; Thomas, J, 1981
)
0.26

Dosage Studied

Brompheniramine was considered significantly better than clemastine in long-term control. The results showed that both antihistamines were significantly effective compared to placebo.

ExcerptRelevanceReference
" Each child received a standard dosage of the study medicine according to a double-blind, crossover design."( A decongestant-antihistamine mixture in the prevention of otitis media in children with colds.
Hendley, JO; Randall, JE, 1979
)
0.26
" For H1-receptor antagonists with long half-life values, steady state may not be reached for several days (chlorpheniramine and brompheniramine) or several weeks (astemizole), and significant accumulation of drug occurs if the dosing interval is more frequent than every half-life."( The comparative pharmacokinetics of H1-receptor antagonists.
Chung, M; Simons, FE; Simons, KJ; Yeh, J, 1987
)
0.48
" The results showed that both antihistamines were significantly effective compared to placebo and that at the dosage used brompheniramine was considered significantly better than clemastine in long-term control."( A placebo-controlled comparative study of sustained-release brompheniramine maleate against clemastine fumarate in the treatment of chronic urticaria.
Jolliffe, DS; Sim-Davis, D; Templeton, JS, 1985
)
0.72
" Blood samples for subsequent assay were obtained at frequent time intervals throughout each 7-d dosing phase."( Steady-state bioavailability of dexbrompheniramine and pseudoephedrine from a repeat-action combination tablet.
Digiore, C; Gural, R; Kim, HK; Lim, J; Lin, CC; Symchowicz, S, 1985
)
0.55
"Sprague-Dawley male albino rats showed in a dose-response study a maximal drinking response to a 5 U/kg dose of SC insulin in a 2-hr test."( Histaminergic mechanism for drinking elicited by insulin in the rat.
Hecht, ES; Kraly, FS; Miller, LA, 1983
)
0.27
" The dosage was flexible, maintenance doses varying between 50-150 mg in the amitriptyline group and 50-300 mg in the zimelidine group."( A double-blind comparison of zimelidine and amitriptyline in depressive out-patients.
Lehtinen, V; Salminen, J; Syvälahti, E, 1982
)
0.26
" An initial dosage of 150 mg/day was used for up to 6 weeks."( Zimelidine: a placebo-controlled trial in depression.
Burrows, GD; Davies, BM; Marriott, PF; McIntyre, IM; Moore, RG; Norman, TR, 1983
)
0.27
" Dosage range was 75-300 mg/day for active medications."( A double-blind evaluation of zimelidine in comparison to placebo and amitriptyline in patients with major depressive disorder.
Behrnetz, S; Bush, DF; Claghorn, J; Gershon, S; Goldstein, BJ; Huitfeldt, B, 1983
)
0.27
" With the applied, probably suboptimal, dosage the therapeutic response was only satisfactory in five cases."( Plasma levels of zimelidine and norzimelidine in endogenous depression.
Hansen, LB; Hvidberg, EF; Larsen, NE; Thomsen, IS; Vestergård, P, 1980
)
0.26
" These three dosage schedules were studied."( Zimelidine: comparison of different dosage regimes in general practice.
Tiplady, B; Watson, JM, 1981
)
0.26
" Blood and urine samples were collected for a period of 28 hours after dosing and the concentrations of zimelidine and norzimelidine determined."( Pharmacokinetics of zimelidine in humans--plasma levels and urinary excretion of zimelidine and norzimelidine after intravenous and oral administration of zimelidine.
Chaturvedi, S; Love, BL; Moore, RG; Thomas, J, 1981
)
0.26
"25-20 mg/kg) in a dose-response study."( A probe for a histaminergic component of drinking in the rat.
Kraly, FS, 1983
)
0.27
" Single dosage of the drug occurred at 08."( Differences in performance impairment due to brompheniramine maleate as a function of the sustained-release system.
Millar, K; Standen, PJ, 1982
)
0.52
" In healthy volunteers full dose-response curves were constructed by infusing histamine, before and after administration of an H1 or H2 antagonist or both antagonists, into dorsal hand veins preconstricted with the alpha-adrenergic agonist phenylephrine."( Histamine-induced venodilation in human beings involves both H1 and H2 receptor subtypes.
Bedarida, G; Blaschke, TF; Dachman, WD; Hoffman, BB, 1994
)
0.29
" Revised dosage regimens may be needed in this population."( The clinical pharmacology of brompheniramine in children.
Gu, X; Kapur, S; Roberts, JR; Simons, FE; Simons, KJ, 1999
)
0.59
" We explore the toxicities of OTC cough and cold medications, discuss mechanisms of dosing errors, and suggest why physicians should be more vigilant in specifically inquiring about OTCs when evaluating an ill child."( Toxicity of over-the-counter cough and cold medications.
Gunn, VL; Liebelt, EL; Serwint, JR; Taha, SH, 2001
)
0.31
" The taste masked complexes can be potentially developed as suitable dosage forms for pediatric use."( Tannate complexes of antihistaminic drug: sustained release and taste masking approaches.
Berendt, RT; Khan, MA; Rahman, Z; Zidan, AS, 2012
)
0.38
" The dose-response curve and nociceptive block duration of brompheniramine were constructed and compared with mepivacaine."( Subcutaneous brompheniramine for cutaneous analgesia in rats.
Chen, JY; Chen, YW; Chiu, CC; Hung, CH; Wang, JJ, 2019
)
1.13
" An optimized dose-response curve is then presented, introducing (±) amphetamine hydrochloride (0."( A Molecularly Imprinted Polymer-based Dye Displacement Assay for the Rapid Visual Detection of Amphetamine in Urine.
Arreguin-Campos, R; Caldara, M; Cleij, TJ; Diliën, H; Eersels, K; Heidt, B; Jimenez-Monroy, KL; Lowdon, JW; Rogosic, R; van Grinsven, B, 2020
)
0.56
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (2)

RoleDescription
H1-receptor antagonistH1-receptor antagonists are the drugs that selectively bind to but do not activate histamine H1 receptors, thereby blocking the actions of endogenous histamine.
anti-allergic agentA drug used to treat allergic reactions.
[role 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]

Drug Classes (2)

ClassDescription
pyridinesAny organonitrogen heterocyclic compound based on a pyridine skeleton and its substituted derivatives.
organobromine compoundA compound containing at least one carbon-bromine bond.
[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]

Pathways (1)

PathwayProteinsCompounds
Brompheniramine H1-Antihistamine Action87

Protein Targets (9)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
thioredoxin reductaseRattus norvegicus (Norway rat)Potency0.10000.100020.879379.4328AID588453
GLS proteinHomo sapiens (human)Potency0.50120.35487.935539.8107AID624146
arylsulfatase AHomo sapiens (human)Potency37.93301.069113.955137.9330AID720538
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency3.76860.035520.977089.1251AID504332
atrial natriuretic peptide receptor 2 precursorHomo sapiens (human)Potency18.49270.00669.809418.4927AID1347050
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency3.16230.009610.525035.4813AID1479145
Ataxin-2Homo sapiens (human)Potency7.94330.011912.222168.7989AID588378
[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)
Bile salt export pumpHomo sapiens (human)IC50 (µMol)100.00000.11007.190310.0000AID1443986
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC50 (µMol)0.89130.00091.901410.0000AID576612
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (50)

Processvia Protein(s)Taxonomy
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by hormonePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of DNA-templated transcriptionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion homeostasisPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cardiac muscle contractionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cellular response to xenobiotic stimulusPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane depolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion import across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of receptor internalizationAtaxin-2Homo sapiens (human)
regulation of translationAtaxin-2Homo sapiens (human)
RNA metabolic processAtaxin-2Homo sapiens (human)
P-body assemblyAtaxin-2Homo sapiens (human)
stress granule assemblyAtaxin-2Homo sapiens (human)
RNA transportAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (22)

Processvia Protein(s)Taxonomy
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
transcription cis-regulatory region bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
delayed rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ubiquitin protein ligase bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
identical protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein homodimerization activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
C3HC4-type RING finger domain bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
scaffold protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
RNA bindingAtaxin-2Homo sapiens (human)
epidermal growth factor receptor bindingAtaxin-2Homo sapiens (human)
protein bindingAtaxin-2Homo sapiens (human)
mRNA bindingAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (22)

Processvia Protein(s)Taxonomy
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cell surfacePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
perinuclear region of cytoplasmPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cytoplasmAtaxin-2Homo sapiens (human)
Golgi apparatusAtaxin-2Homo sapiens (human)
trans-Golgi networkAtaxin-2Homo sapiens (human)
cytosolAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
membraneAtaxin-2Homo sapiens (human)
perinuclear region of cytoplasmAtaxin-2Homo sapiens (human)
ribonucleoprotein complexAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (39)

Assay IDTitleYearJournalArticle
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID1636474Drug activation in human Hep3B cells assessed as human CYP2D6-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 7 uM pre-incubated with BSO for 18 hrs followed by incubation with compound for 3 hrs in presence of NADP2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.
AID77799Histamine induced lethality, at 60-min pretreatment time when 0.3 mg/kg compound was administered perorally in guinea pigs1989Journal of medicinal chemistry, Sep, Volume: 32, Issue:9
Benzo- and pyrido-1,4-oxazepin-5-ones and -thiones: synthesis and structure-activity relationships of a new series of H1 antihistamines.
AID22246Pharmacokinetic parameter :volume apparent of distribution was reported1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Molecular properties and pharmacokinetic behavior of cetirizine, a zwitterionic H1-receptor antagonist.
AID576612Inhibition of human ERG2011European journal of medicinal chemistry, Feb, Volume: 46, Issue:2
Predicting hERG activities of compounds from their 3D structures: development and evaluation of a global descriptors based QSAR model.
AID47777The compound dose required to elicit marked cortical slowing and spindling, when administarted intra venously in cats1989Journal of medicinal chemistry, Sep, Volume: 32, Issue:9
Benzo- and pyrido-1,4-oxazepin-5-ones and -thiones: synthesis and structure-activity relationships of a new series of H1 antihistamines.
AID47776The compound dose required for 50% block of H1 histamine activity, when administarted intra venously in cats1989Journal of medicinal chemistry, Sep, Volume: 32, Issue:9
Benzo- and pyrido-1,4-oxazepin-5-ones and -thiones: synthesis and structure-activity relationships of a new series of H1 antihistamines.
AID205268Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on voltage dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex at 10 uM1985Journal of medicinal chemistry, Mar, Volume: 28, Issue:3
[3H]Batrachotoxinin A 20 alpha-benzoate binding to voltage-sensitive sodium channels: a rapid and quantitative assay for local anesthetic activity in a variety of drugs.
AID132665In vitro inhibition of accumulation of (-)-[3H]Norepinephrine (NA) in mouse brain slices1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
Synthesis of pyridylallylamines related to zimelidine and their inhibition of neuronal monoamine uptake.
AID1443992Total Cmax in human administered as single dose2014Hepatology (Baltimore, Md.), Sep, Volume: 60, Issue:3
Human drug-induced liver injury severity is highly associated with dual inhibition of liver mitochondrial function and bile salt export pump.
AID1636412Drug activation in human Hep3B cells assessed as human CYP3A4-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 150.3 uM pre-incubated with BSO for 18 hrs followed by incubation with compound for 3 hrs in presence of 2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.
AID76970Effective dose that protects guinea pigs against histamine induced lethality at 6 hours pretreatment time1989Journal of medicinal chemistry, Sep, Volume: 32, Issue:9
Benzo- and pyrido-1,4-oxazepin-5-ones and -thiones: synthesis and structure-activity relationships of a new series of H1 antihistamines.
AID16029Pharmacokinetic parameter :drug bound to plasma was reported1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Molecular properties and pharmacokinetic behavior of cetirizine, a zwitterionic H1-receptor antagonist.
AID781330pKa (acid-base dissociation constant) as determined by potentiometric titration2014Pharmaceutical research, Apr, Volume: 31, Issue:4
Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds.
AID205267Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on voltage dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex1985Journal of medicinal chemistry, Mar, Volume: 28, Issue:3
[3H]Batrachotoxinin A 20 alpha-benzoate binding to voltage-sensitive sodium channels: a rapid and quantitative assay for local anesthetic activity in a variety of drugs.
AID1443995Hepatotoxicity in human assessed as drug-induced liver injury2014Hepatology (Baltimore, Md.), Sep, Volume: 60, Issue:3
Human drug-induced liver injury severity is highly associated with dual inhibition of liver mitochondrial function and bile salt export pump.
AID130700In vivo inhibition of accumulation of [14C]5-HT (5-HT) in mouse brain slices after intraperitoneal administration1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
Synthesis of pyridylallylamines related to zimelidine and their inhibition of neuronal monoamine uptake.
AID1443986Inhibition of recombinant human BSEP expressed in baculovirus infected sf9 cell membrane vesicles assessed as reduction in ATP or AMP-dependent [3H]-taurocholic acid uptake in to vesicles preincubated for 5 mins followed by ATP/AMP addition measured after2014Hepatology (Baltimore, Md.), Sep, Volume: 60, Issue:3
Human drug-induced liver injury severity is highly associated with dual inhibition of liver mitochondrial function and bile salt export pump.
AID77685Histamine induced lethality, at 60-min pretreatment time of 0.1 mg/kg p.o. in guinea pigs.1989Journal of medicinal chemistry, Sep, Volume: 32, Issue:9
Benzo- and pyrido-1,4-oxazepin-5-ones and -thiones: synthesis and structure-activity relationships of a new series of H1 antihistamines.
AID132666In vitro inhibition of accumulation of [14C]5-HT (5-HT) in mouse brain slices1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
Synthesis of pyridylallylamines related to zimelidine and their inhibition of neuronal monoamine uptake.
AID76971Effective dose that protects guinea pigs against histamine induced lethality, at 1 hour pretreatment time1989Journal of medicinal chemistry, Sep, Volume: 32, Issue:9
Benzo- and pyrido-1,4-oxazepin-5-ones and -thiones: synthesis and structure-activity relationships of a new series of H1 antihistamines.
AID130699In vivo inhibition of accumulation of (-)-[3H]Norepinephrine (NA) in mouse brain slices after intraperitoneal administration1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
Synthesis of pyridylallylamines related to zimelidine and their inhibition of neuronal monoamine uptake.
AID1443991Induction of mitochondrial dysfunction in Sprague-Dawley rat liver mitochondria assessed as inhibition of mitochondrial respiration per mg mitochondrial protein measured for 20 mins by A65N-1 oxygen probe based fluorescence assay2014Hepatology (Baltimore, Md.), Sep, Volume: 60, Issue:3
Human drug-induced liver injury severity is highly associated with dual inhibition of liver mitochondrial function and bile salt export pump.
AID24562Pharmacokinetic parameter :half life in humans was reported1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Molecular properties and pharmacokinetic behavior of cetirizine, a zwitterionic H1-receptor antagonist.
AID1474166Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID1474167Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID1636356Drug activation in human Hep3B cells assessed as human CYP2C9-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 300 uM pre-incubated with BSO for 18 hrs followed by incubation with compound for 3 hrs in presence of NA2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.
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 (329)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990235 (71.43)18.7374
1990's34 (10.33)18.2507
2000's26 (7.90)29.6817
2010's27 (8.21)24.3611
2020's7 (2.13)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 91.70

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 Index91.70 (24.57)
Research Supply Index6.09 (2.92)
Research Growth Index4.38 (4.65)
Search Engine Demand Index167.44 (26.88)
Search Engine Supply Index2.02 (0.95)

This Compound (91.70)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials91 (26.07%)5.53%
Reviews14 (4.01%)6.00%
Case Studies20 (5.73%)4.05%
Observational0 (0.00%)0.25%
Other224 (64.18%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (3)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Multicenter Clinical Trial, Phase III, Controlled, Open, Parallel Group, Randomized, Comparing the Fixed Dose Combination of Diphenhydramine + Dropropizine + Pseudoephedrine and the Combined Use of Dropropizine and Fixed Dose Combination of Pseudoephedrin [NCT01177852]Phase 30 participants (Actual)Interventional2011-10-31Withdrawn
A Single-Dose, Open-Label, Pharmacokinetic Study of Brompheniramine Maleate Liquid in Children and Adolescents [NCT00894634]Phase 137 participants (Actual)Interventional2009-03-21Completed
Multicenter, Phase III, Randomized, Open, Parallel, Comparative to Evaluate the Efficacy and Safety of the Treatment of Nasal Congestion and Runny Nose Present in Acute Crisis of Viral Rhinitis and Allergic Reactions, in Pediatric Patients [NCT01393548]Phase 3879 participants (Actual)Interventional2014-08-31Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]