Page last updated: 2024-11-04

naphazoline

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Description

Naphazoline is an imidazoline derivative that acts as a potent alpha-adrenergic agonist. It is primarily used as a nasal decongestant, but also finds applications in ophthalmology to constrict blood vessels and reduce redness in the eyes. Naphazoline is synthesized from 2-imidazoline and an aromatic aldehyde through a condensation reaction. The compound exerts its effects by stimulating alpha-adrenergic receptors, leading to vasoconstriction in the nasal mucosa and conjunctiva. This constriction reduces nasal congestion and ocular redness, respectively. Naphazoline is studied for its potential therapeutic applications, particularly in treating allergic rhinitis, conjunctivitis, and other inflammatory conditions. However, its use can be associated with adverse effects like rebound congestion, hypertension, and cardiac arrhythmias. Research into naphazoline continues to focus on its potential benefits and risks, aiming to optimize its therapeutic use and minimize its potential adverse effects.'

Naphazoline: An adrenergic vasoconstrictor agent used as a decongestant. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID4436
CHEMBL ID761
CHEBI ID93363
SCHEMBL ID34532
MeSH IDM0014455

Synonyms (122)

Synonym
nafazolina
h231gf11bv ,
unii-h231gf11bv
nafazoline
naphazolinum
5-23-08-00293 (beilstein handbook reference)
2-(naphthyl-(1')-methyl)imidazolin
AB00053505-12
BRD-K77641333-003-05-7
naphazoline
1h-imidazole, 4,5-dihydro-2-(1-naphthalenylmethyl)-
ENAMINE_000333 ,
KBIO1_000456
DIVK1C_000456
nafazolina [dcit]
2-imidazoline, 2-(1-naphthylmethyl)-
antan
2-(alpha-naphthylmethyl)-imidazoline
4,5-dihydro-2-(1-naphthylmethyl)imidazole
nafazoline [spanish]
clearine
naphazolinum [inn-latin]
2-(1-naphthylmethyl)-2-imidazoline
naphazolinum [latin]
2-(naphthyl-(1')-methyl)imidazolin [german]
einecs 212-641-5
naphthizine
ciba 2020/r
naphazoline [inn:ban]
alpha-naphthylmethyl imidazoline
brn 0151864
SPECTRUM_000975
NCGC00016506-01
IDI1_000456
BSPBIO_002065
BPBIO1_000189
SPECTRUM5_001424
PRESTWICK3_000046
PRESTWICK2_000046
STK300042
2-(naphthalen-1-ylmethyl)-4,5-dihydro-1h-imidazole
NCGC00024349-03
KBIO3_001565
KBIOGR_000595
KBIO2_004023
KBIO2_001455
KBIO2_006591
KBIOSS_001455
SPBIO_002092
PRESTWICK1_000046
SPECTRUM3_000513
PRESTWICK0_000046
NINDS_000456
SPECTRUM2_001054
SPECTRUM4_000068
SPBIO_001008
BSPBIO_000171
NCGC00016506-02
HMS2090D15
CHEMBL761
AKOS000295230
nafazolin
DB06711
HMS1394P03
L000878
naphazoline (inn)
nafazolin (tn)
835-31-4
D08253
cid_11079
2-naphthalen-1-ylmethyl-4,5-dihydro-1h-imidazole; hydrochloride
bdbm50001922
A840596
2-(1-naphthylmethyl)-4,5-dihydro-1h-imidazole;naphazoline
imidin
tox21_113058
cas-835-31-4
tox21_113645
dtxsid3048449 ,
dtxcid90198485
BBL012612
NCGC00016506-03
NCGC00016506-04
NCGC00016506-05
naphazoline [mart.]
naphazoline [who-dd]
naphazoline [vandf]
naphazoline [inn]
naphazoline [mi]
gtpl5509
SCHEMBL34532
AB00053505-11
2-(1-naphthylmethyl)-4,5-dihydro-1h-imidazole #
.alpha.-naphthylmethyl imidazoline
privine (salt/mix)
rhinazine
2-(.alpha.-naphthylmethyl)-imidazoline
2-(1-naphthalenylmethyl)-2-imidazoline
CNIIGCLFLJGOGP-UHFFFAOYSA-N
sanorin (salt/mix)
AB00053505_13
AB00053505_14
CCG-250339
CHEBI:93363
2-(1-naphthalenylmethyl)-4,5-dihydro-1h-imidazole
HY-111326
Z56762888
SBI-0051454.P003
Q415433
FT-0725973
VS-03410
2-[(naphthalen-1-yl)methyl]-4,5-dihydro-1h-imidazole
BRD-K77641333-003-15-6
BRD-K77641333-003-25-5
CS-0034952
EN300-16752
r01ab02
r01aa08
s01ga01
naphazolinum (latin)
naphazoline (mart.)
naphazolinum (inn-latin)

Research Excerpts

Overview

Naphazoline is a drug commonly used as a decongestant in adult patients.

ExcerptReferenceRelevance
"Naphazoline is a drug commonly used as a decongestant in adult patients. "( [Severe poisoning with naphazoline: update from a therapeutic error].
Alava, J; Díaz, M; Gabrielli, T; Granson, E; Mendoza, L; Taiman, J, 2018
)
2.23

Treatment

ExcerptReferenceRelevance
"Pretreatment with naphazoline administered topically also inhibited impedance changes cause by histamine application."( Effects of diphenhydramine, naphazoline and m-amino-alpha(1-aminoethyl)benzyl alcohol dihydrochloride on the nasal mucosa determined by impedance method: a simple method for evaluation of nasal decongestant.
Akagi, M; Tasaka, K, 1976
)
0.87

Pharmacokinetics

ExcerptReferenceRelevance
" This simple, accurate, non aggressive method is used for pharmacodynamic tests."( [Radioisotopic study of the nasal muco-ciliary clearance (author's transl)].
Laurens, MH; Robert, J; Simeons, P; Thouvenot, P; Wayoff, M, 1980
)
0.26

Bioavailability

ExcerptReferenceRelevance
" Systemic clearance of nafimidone from plasma after iv administration was approximately 2 times higher than hepatic blood flow in rats, and the oral bioavailability was 15%."( Disposition of nafimidone in rats.
Chaplin, MD; Graham, DJ; Hall, DJ; Hama, KM; Kurz, L; Smith, SA,
)
0.13
"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

Dosage Studied

The case was also of forensic interest, because the naphazoline mixture was prepared in a pharmacy in a concentration 80 times above the adequate dosage for children. The patient interview revealed consumption to supra-therapeutic dosage of naphzoline and prednisolone nasal sprays.

ExcerptRelevanceReference
" The dose-response curves generated by the model for partial agonists were similar to the curves obtained experimentally in vitro."( Relationship between alpha-adrenoceptor occupancy and contractile response in rat vas deferens. Experimental and theoretical analysis.
Díaz-Toledo, A; Martí, MC, 1988
)
0.27
" within 30 min of dosing before electrical stimulation."( The anticonvulsant action of nafimidone on kindled amygdaloid seizures in rats.
Albertson, TE; Walby, WF,
)
0.13
" Conformity to Beer's law enabled the assay of dosage forms of these drugs."( Utility of chloranil in assay of naphazoline, clemizole, penicillin G sodium, and piperazine.
Abdel-Hamid, ME; Abdine, H; Belal, S; Elsayed, MA, 1981
)
0.54
" Hypotensive potency after intravenous administration to anesthetized, normotensive rats was determined as a measure of central alpha-adrenergic activity and expressed as pC25, obtained from log dose-response curves."( Characterization of alpha-adrenoceptor populations. Quantitative relationships between cardiovascular effects initiated at central and peripheral alpha-adrenoceptors.
de Jonge, A; Lam, E; Slothorst-Grisdijk, FP; Timmermans, PB; van Meel, JC; van Zwieten, PA, 1981
)
0.26
" In rat mesenteric artery, the pA2 value for yohimbine against clonidine was not statistically different from values obtained with the other agonists; however, in the presence of prazosin the dose-response curve to clonidine was biphasic, suggesting that the action of clonidine is mediated through two distinct sites to which prazosin has different affinities."( Pharmacological characterization of the postsynaptic alpha adrenoceptors in vascular smooth muscle from canine and rat mesenteric vascular beds.
Agrawal, DK; Daniel, EE; Triggle, CR, 1984
)
0.27
" The three preparations were found to vary greatly in patient comfort and acceptability but were not different in their ability to ameliorate the itching, tearing, redness, edema and discomfort when dosed topically for the relief of allergic conjunctivitis."( A double-masked comparison of ocular decongestants as therapy for allergic conjunctivitis.
deFaller, JM; Lanier, BQ; Smith, JP; Tremblay, N, 1983
)
0.27
" It was found that the dose-effect curve based on the survival parameters of irradiated animals had two-phase character for cystamin and heparin with maxima of efficiency in the field of low and standard dosage of radioprotectors."( [Comparative study of the radiation-protective effectiveness of low doses of cysteamine, heparin, and naphtizine in experiments on mice].
Grebeniuk, AN; Lukashin, BP,
)
0.13
" The method was applied to the quantitation of the three components in a commercial dosage form."( Simultaneous determination of naphazoline, diphenhydramine and phenylephrine in nasal solutions by capillary electrophoresis.
Goicoechea, HC; Mantovani, VE; Marchesini, AF; Robles, JC; Williner, MR, 2003
)
0.61
" The case was also of forensic interest, because the naphazoline mixture was prepared in a pharmacy in a concentration 80 times above the adequate dosage for children."( Naphazoline intoxication in a child-a clinical and forensic toxicological case.
Gerschlauer, A; Madea, B; Musshoff, F, 2003
)
2.01
" Attention should be paid to galenic properties and dosage of the active."( [The tolerability of nasal drugs with special regard to preservatives and physico-chemical parameters].
Klöcker, N; Rudolph, P; Sikora, C; Verse, T, 2003
)
0.32
" The treatment duration was 5 days at usual recommended dosage regimens."( [Efficacy of Derinox assessed with one PNIF (Peak Nasal Inspiratory Flow) in patients suffering from common cold].
Bruhwyler, J; Concas, V; Dessanges, JF; Peynegre, R, 2005
)
0.33
" The patient interview revealed consumption to supra-therapeutic dosage of an association of naphazoline and prednisolone nasal sprays."( [Malignant hypertension and cardiac decompensation after overuse of nasal decongestant: A case report and literature review].
Bontemps, H; Bourdelin, M; Le Vavasseur, O; Novais, T, 2016
)
0.65
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
naphthalenesAny benzenoid aromatic compound having a skeleton composed of two ortho-fused benzene rings.
[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 (18)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Microtubule-associated protein tauHomo sapiens (human)Potency0.79430.180013.557439.8107AID1468
aryl hydrocarbon receptorHomo sapiens (human)Potency29.84930.000723.06741,258.9301AID743085; AID743122
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency7.94330.00207.533739.8107AID891
mitogen-activated protein kinase 1Homo sapiens (human)Potency3.98110.039816.784239.8107AID1454
lamin isoform A-delta10Homo sapiens (human)Potency1.99530.891312.067628.1838AID1487
[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)
Bile salt export pumpHomo sapiens (human)IC50 (µMol)1,000.00000.11007.190310.0000AID1449628
Alpha-2C adrenergic receptorHomo sapiens (human)Ki0.00230.00030.483410.0000AID1232265
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)Ki0.00570.00000.929610.0000AID35187
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)Ki0.00570.00000.970810.0000AID35187
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)Ki0.00570.00000.937510.0000AID35187
NischarinHomo sapiens (human)Ki0.12160.00420.21923.8019AID342861
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Alpha-2C adrenergic receptorHomo sapiens (human)EC50 (µMol)0.05490.00050.55416.7100AID1232266
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)EC50 (µMol)0.06310.00543.251020.9400AID36629
Alpha-1D adrenergic receptorHomo sapiens (human)EC50 (µMol)5.01190.00151.72275.6000AID32972; AID35453
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)EC50 (µMol)0.06310.01260.03790.0631AID36629
5-hydroxytryptamine receptor 1DRattus norvegicus (Norway rat)EC50 (µMol)0.06310.00130.03880.0970AID36629
5-hydroxytryptamine receptor 1FRattus norvegicus (Norway rat)EC50 (µMol)0.06310.01260.03190.0631AID36629
Alpha-1A adrenergic receptorHomo sapiens (human)EC50 (µMol)0.06310.00010.50987.1000AID32967; AID36629
Alpha-1B adrenergic receptorHomo sapiens (human)EC50 (µMol)5.01190.00011.30105.6000AID32970; AID37350
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (72)

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 smooth muscle contractionAlpha-2C adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-2C adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-2C adrenergic receptorHomo sapiens (human)
negative regulation of norepinephrine secretionAlpha-2C adrenergic receptorHomo sapiens (human)
regulation of vasoconstrictionAlpha-2C adrenergic receptorHomo sapiens (human)
platelet activationAlpha-2C adrenergic receptorHomo sapiens (human)
activation of protein kinase B activityAlpha-2C adrenergic receptorHomo sapiens (human)
negative regulation of epinephrine secretionAlpha-2C adrenergic receptorHomo sapiens (human)
receptor transactivationAlpha-2C adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-2C adrenergic receptorHomo sapiens (human)
positive regulation of neuron differentiationAlpha-2C adrenergic receptorHomo sapiens (human)
adrenergic receptor signaling pathwayAlpha-2C adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-2C adrenergic receptorHomo sapiens (human)
negative regulation of insulin secretionAlpha-2C adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of cell population proliferationAlpha-1D adrenergic receptorHomo sapiens (human)
neuron-glial cell signalingAlpha-1D adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-1D adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of vasoconstrictionAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-1D adrenergic receptorHomo sapiens (human)
MAPK cascadeAlpha-1A adrenergic receptorHomo sapiens (human)
negative regulation of heart rate involved in baroreceptor response to increased systemic arterial blood pressureAlpha-1A adrenergic receptorHomo sapiens (human)
norepinephrine-epinephrine vasoconstriction involved in regulation of systemic arterial blood pressureAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of heart rate by epinephrine-norepinephrineAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of the force of heart contraction by epinephrine-norepinephrineAlpha-1A adrenergic receptorHomo sapiens (human)
apoptotic processAlpha-1A adrenergic receptorHomo sapiens (human)
smooth muscle contractionAlpha-1A adrenergic receptorHomo sapiens (human)
signal transductionAlpha-1A adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-1A adrenergic receptorHomo sapiens (human)
activation of phospholipase C activityAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationAlpha-1A adrenergic receptorHomo sapiens (human)
adult heart developmentAlpha-1A adrenergic receptorHomo sapiens (human)
negative regulation of cell population proliferationAlpha-1A adrenergic receptorHomo sapiens (human)
response to xenobiotic stimulusAlpha-1A adrenergic receptorHomo sapiens (human)
response to hormoneAlpha-1A adrenergic receptorHomo sapiens (human)
negative regulation of autophagyAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of cardiac muscle hypertrophyAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of synaptic transmission, GABAergicAlpha-1A adrenergic receptorHomo sapiens (human)
intracellular signal transductionAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of action potentialAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of vasoconstrictionAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of smooth muscle contractionAlpha-1A adrenergic receptorHomo sapiens (human)
calcium ion transport into cytosolAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of cardiac muscle contractionAlpha-1A adrenergic receptorHomo sapiens (human)
cell growth involved in cardiac muscle cell developmentAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of protein kinase C signalingAlpha-1A adrenergic receptorHomo sapiens (human)
pilomotor reflexAlpha-1A adrenergic receptorHomo sapiens (human)
neuron-glial cell signalingAlpha-1A adrenergic receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayAlpha-1A adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-1A adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-1A adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-1B adrenergic receptorHomo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayAlpha-1B adrenergic receptorHomo sapiens (human)
regulation of vasoconstrictionAlpha-1B adrenergic receptorHomo sapiens (human)
intracellular signal transductionAlpha-1B adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-1B adrenergic receptorHomo sapiens (human)
regulation of cardiac muscle contractionAlpha-1B adrenergic receptorHomo sapiens (human)
neuron-glial cell signalingAlpha-1B adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-1B adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-1B adrenergic receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayAlpha-1B adrenergic receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationAlpha-1B adrenergic receptorHomo sapiens (human)
apoptotic processNischarinHomo sapiens (human)
Rac protein signal transductionNischarinHomo sapiens (human)
actin cytoskeleton organizationNischarinHomo sapiens (human)
negative regulation of cell migrationNischarinHomo sapiens (human)
outer dynein arm assemblyNischarinHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (20)

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)
alpha2-adrenergic receptor activityAlpha-2C adrenergic receptorHomo sapiens (human)
protein bindingAlpha-2C adrenergic receptorHomo sapiens (human)
alpha-2A adrenergic receptor bindingAlpha-2C adrenergic receptorHomo sapiens (human)
protein homodimerization activityAlpha-2C adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-2C adrenergic receptorHomo sapiens (human)
epinephrine bindingAlpha-2C adrenergic receptorHomo sapiens (human)
guanyl-nucleotide exchange factor activityAlpha-2C adrenergic receptorHomo sapiens (human)
protein bindingAlpha-1D adrenergic receptorHomo sapiens (human)
identical protein bindingAlpha-1D adrenergic receptorHomo sapiens (human)
alpha1-adrenergic receptor activityAlpha-1D adrenergic receptorHomo sapiens (human)
alpha1-adrenergic receptor activityAlpha-1A adrenergic receptorHomo sapiens (human)
protein bindingAlpha-1A adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-1A adrenergic receptorHomo sapiens (human)
protein bindingAlpha-1B adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-1B adrenergic receptorHomo sapiens (human)
alpha1-adrenergic receptor activityAlpha-1B adrenergic receptorHomo sapiens (human)
integrin bindingNischarinHomo sapiens (human)
protein bindingNischarinHomo sapiens (human)
phosphatidylinositol bindingNischarinHomo sapiens (human)
identical protein bindingNischarinHomo sapiens (human)
dynein heavy chain bindingNischarinHomo sapiens (human)
alpha-tubulin bindingNischarinHomo 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)
cytoplasmAlpha-2C adrenergic receptorHomo sapiens (human)
endosomeAlpha-2C adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2C adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2C adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1D adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1D adrenergic receptorHomo sapiens (human)
nucleusAlpha-1A adrenergic receptorHomo sapiens (human)
nucleoplasmAlpha-1A adrenergic receptorHomo sapiens (human)
cytoplasmAlpha-1A adrenergic receptorHomo sapiens (human)
cytosolAlpha-1A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1A adrenergic receptorHomo sapiens (human)
caveolaAlpha-1A adrenergic receptorHomo sapiens (human)
nuclear membraneAlpha-1A adrenergic receptorHomo sapiens (human)
intracellular membrane-bounded organelleAlpha-1A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1A adrenergic receptorHomo sapiens (human)
nucleusAlpha-1B adrenergic receptorHomo sapiens (human)
cytoplasmAlpha-1B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1B adrenergic receptorHomo sapiens (human)
caveolaAlpha-1B adrenergic receptorHomo sapiens (human)
nuclear membraneAlpha-1B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1B adrenergic receptorHomo sapiens (human)
nucleoplasmNischarinHomo sapiens (human)
early endosomeNischarinHomo sapiens (human)
cytosolNischarinHomo sapiens (human)
plasma membraneNischarinHomo sapiens (human)
microtubule cytoskeletonNischarinHomo sapiens (human)
membraneNischarinHomo sapiens (human)
intracellular membrane-bounded organelleNischarinHomo sapiens (human)
intercellular bridgeNischarinHomo sapiens (human)
recycling endosomeNischarinHomo sapiens (human)
cytoplasmNischarinHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (50)

Assay IDTitleYearJournalArticle
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
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.
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.
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.
AID625279Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID342863Selectivity ratio of pKi for human imidazoline receptor 1 to pKi for human alpha2 adrenoceptors2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
QSAR study of imidazoline antihypertensive drugs.
AID32970Potency against cloned human alpha 1B adrenoceptor expressed in rat-1 fibroblasts.2001Bioorganic & medicinal chemistry letters, Nov-05, Volume: 11, Issue:21
2-(Anilinomethyl)imidazolines as alpha(1)-adrenoceptor agonists: the identification of alpha(1A) subtype selective 2'-carboxylic acid esters and amides.
AID1232267Agonist activity at recombinant human alpha2c adrenergic receptor expressed in CHOK1 cells co-expressing Gqi5 assessed as induction of cytoplasmic calcium mobilization measured for 40 secs by fluorometric analysis relative to UK143042015Bioorganic & medicinal chemistry, Jul-15, Volume: 23, Issue:14
Cell-based and virtual fragment screening for adrenergic α2C receptor agonists.
AID23715Apparent partion coefficient of compound was evaluated in octanol/buffer at pH of 7.4 at 37 degree Centigrade1984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists.
AID1137409Displacement of [3H]clonidine from alpha-adrenergic receptor in rat brain1979Journal of medicinal chemistry, Nov, Volume: 22, Issue:11
Ultraviolet photoelectron spectroscopy of cyclic amidines. 1. Electronic structure of some alpha-adrenergic benzylimidazolines.
AID23716Partition coefficient (logD7.4)1981Journal of medicinal chemistry, May, Volume: 24, Issue:5
Characterization of alpha-adrenoceptor populations. Quantitative relationships between cardiovascular effects initiated at central and peripheral alpha-adrenoceptors.
AID197167Hypotensive activity (25% decrease in arterial pressure) after i.v. administration to anesthetized normotensive rats.1984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists.
AID625287Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625290Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID32967Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.2001Bioorganic & medicinal chemistry letters, Nov-05, Volume: 11, Issue:21
2-(Anilinomethyl)imidazolines as alpha(1)-adrenoceptor agonists: the identification of alpha(1A) subtype selective 2'-carboxylic acid esters and amides.
AID36792Binding affinity against Alpha-2 adrenergic receptor is the ability to inhibit the specific [3H]clonidine binding (0.4 nM) to rat isolated brain membranes by 50% was reported; 4.8*10e-91984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists.
AID625288Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625282Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625285Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1232265Displacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysis2015Bioorganic & medicinal chemistry, Jul-15, Volume: 23, Issue:14
Cell-based and virtual fragment screening for adrenergic α2C receptor agonists.
AID33252Peripheral hypertensive activity in pithed normotensive rats.1981Journal of medicinal chemistry, May, Volume: 24, Issue:5
Characterization of alpha-adrenoceptor populations. Quantitative relationships between cardiovascular effects initiated at central and peripheral alpha-adrenoceptors.
AID342860Displacement of [125I]PIC from human alpha2 adrenoceptors expressed in CHO cells2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
QSAR study of imidazoline antihypertensive drugs.
AID37350In vitro activation of human Alpha-1B receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay2002Bioorganic & medicinal chemistry letters, Feb-25, Volume: 12, Issue:4
2-(anilinomethyl)imidazolines as alpha1A adrenergic receptor agonists: 2'-heteroaryl and 2'-oxime ether series.
AID1449628Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method2012Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12
Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.
AID1137408Binding affinity to alpha-adrenergic receptor in rabbit jejunum1979Journal of medicinal chemistry, Nov, Volume: 22, Issue:11
Ultraviolet photoelectron spectroscopy of cyclic amidines. 1. Electronic structure of some alpha-adrenergic benzylimidazolines.
AID33250Central hypotensive activity in anesthetized normotensive rats.1981Journal of medicinal chemistry, May, Volume: 24, Issue:5
Characterization of alpha-adrenoceptor populations. Quantitative relationships between cardiovascular effects initiated at central and peripheral alpha-adrenoceptors.
AID36629In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay2002Bioorganic & medicinal chemistry letters, Feb-25, Volume: 12, Issue:4
2-(anilinomethyl)imidazolines as alpha1A adrenergic receptor agonists: 2'-heteroaryl and 2'-oxime ether series.
AID32966Efficacy against alpha 1A adrenoceptor in human expressed as phenylephrine response at the dose of 40 uM2001Bioorganic & medicinal chemistry letters, Nov-05, Volume: 11, Issue:21
2-(Anilinomethyl)imidazolines as alpha(1)-adrenoceptor agonists: the identification of alpha(1A) subtype selective 2'-carboxylic acid esters and amides.
AID342861Displacement of [125I]PIC from human imidazoline receptor 1 in human platelets analyzed under norepinephrine mask of alpha 2AR2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
QSAR study of imidazoline antihypertensive drugs.
AID227718Binding energy by using the equation deltaG obsd = -RT ln KD1984Journal of medicinal chemistry, Dec, Volume: 27, Issue:12
Functional group contributions to drug-receptor interactions.
AID36719Binding affinity against alpha-1 adrenergic receptor is the ability to inhibit the specific [3H]prazosin binding (0.2 nM) to rat isolated brain membranes by 50% was reported; 4.1*10e-71984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists.
AID1232266Agonist activity at recombinant human alpha2c adrenergic receptor expressed in CHOK1 cells co-expressing Gqi5 assessed as induction of cytoplasmic calcium mobilization measured for 40 secs by fluorometric analysis2015Bioorganic & medicinal chemistry, Jul-15, Volume: 23, Issue:14
Cell-based and virtual fragment screening for adrenergic α2C receptor agonists.
AID625289Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625286Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID35187Displacement of [3H]clonidine from Alpha-2 adrenergic receptor of rat brain membranes1982Journal of medicinal chemistry, Dec, Volume: 25, Issue:12
alpha 2 adrenoceptors: classification, localization, mechanisms, and targets for drugs.
AID625291Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625280Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID197169Hypertensive activity (increase in arterial pressure to 60 mmHg)) after i.v. administration to pithed rats.1984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists.
AID625292Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID32972Potency against cloned human alpha 1D-adrenoceptor expressed in rat-1 fibroblasts.2001Bioorganic & medicinal chemistry letters, Nov-05, Volume: 11, Issue:21
2-(Anilinomethyl)imidazolines as alpha(1)-adrenoceptor agonists: the identification of alpha(1A) subtype selective 2'-carboxylic acid esters and amides.
AID625284Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID35453In vitro activation of human alpha-1D receptor expressed in rat-1 fibroblasts via calcium using mobilization through the Gq coupled PLC pathway as functional assay2002Bioorganic & medicinal chemistry letters, Feb-25, Volume: 12, Issue:4
2-(anilinomethyl)imidazolines as alpha1A adrenergic receptor agonists: 2'-heteroaryl and 2'-oxime ether series.
AID625283Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625281Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1347154Primary screen GU AMC 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.
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.
AID1345434Mouse TAAR4P (Class A Orphans)2010PloS one, Jun-15, Volume: 5, Issue:6
Structural and functional evolution of the trace amine-associated receptors TAAR3, TAAR4 and TAAR5 in primates.
AID1345466Rat TAAR4P (Class A Orphans)2010PloS one, Jun-15, Volume: 5, Issue:6
Structural and functional evolution of the trace amine-associated receptors TAAR3, TAAR4 and TAAR5 in primates.
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 (367)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990200 (54.50)18.7374
1990's55 (14.99)18.2507
2000's52 (14.17)29.6817
2010's44 (11.99)24.3611
2020's16 (4.36)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 67.85

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 Index67.85 (24.57)
Research Supply Index6.11 (2.92)
Research Growth Index4.42 (4.65)
Search Engine Demand Index140.75 (26.88)
Search Engine Supply Index2.39 (0.95)

This Compound (67.85)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials37 (8.98%)5.53%
Reviews11 (2.67%)6.00%
Case Studies40 (9.71%)4.05%
Observational1 (0.24%)0.25%
Other323 (78.40%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (7)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Phase I Clinical Study, to Evaluate the Safety and Tolerability of the Ophthalmic Solution PRO-185 When Applied on the Ocular Surface of Healthy Volunteers [NCT05470868]Phase 122 participants (Actual)Interventional2023-02-04Completed
Clinical Evaluation of Safety and Efficacy of Pediatric Naridrin in Comparison to Afrin on the Improval of Nasal Congestion. [NCT02601235]Phase 3292 participants (Actual)Interventional2018-01-16Completed
Comparison of Tolerability Between Two Allergy Drops [NCT01390961]Phase 448 participants (Anticipated)Interventional2011-08-31Enrolling by invitation
A Multi-center, Double-masked, Randomized, Placebo-controlled Evaluation of the Onset and Duration of Action of KetoNaph Ophthalmic Solution in the Conjunctival Allergen Challenge (CAC) Model of Acute Allergic Conjunctivitis. [NCT00770133]Phase 3141 participants (Actual)Interventional2010-02-28Completed
A Randomized, Double-blind, Prospective, Multicentric, Superior Efficacy and Safety of Naphazoline Hydrocloride + Pheniramine Maleate + Panthenol Compared With Naphazoline Hydrocloride in the Symptomatic Control of Nasal Congestion and Nasopharyngeal Due [NCT01533220]Phase 3132 participants (Actual)Interventional2013-01-01Completed
A Phase I Study to Evaluate Safety and Pharmacokinetics of SAR408701 Administered Intravenously as Monotherapy in Japanese Patients With Advanced Malignant Solid Tumors [NCT03324113]Phase 134 participants (Actual)Interventional2017-10-17Completed
A Multi-Center, Double-Masked, Randomized, Vehicle and Active Controlled Evaluation of the Onset and Duration of Action of KetoNaph Ophthalmic Solution in the Conjunctival Allergen Challenge Model of Acute Allergic Conjunctivitis [NCT00769886]Phase 3144 participants (Actual)Interventional2008-10-31Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00769886 (8) [back to overview]Chemosis
NCT00769886 (8) [back to overview]Ciliary Redness
NCT00769886 (8) [back to overview]Conjunctival Hyperemia
NCT00769886 (8) [back to overview]Episcleral Redness
NCT00769886 (8) [back to overview]Eyelid Swelling
NCT00769886 (8) [back to overview]Ocular Itching
NCT00769886 (8) [back to overview]Percentage of Eyes With Ocular Mucus Drainage
NCT00769886 (8) [back to overview]Percentage of Eyes With Tearing
NCT00770133 (8) [back to overview]Chemosis
NCT00770133 (8) [back to overview]Ciliary Redness
NCT00770133 (8) [back to overview]Conjunctival Redness
NCT00770133 (8) [back to overview]Episcleral Redness
NCT00770133 (8) [back to overview]Eyelid Swelling
NCT00770133 (8) [back to overview]Ocular Itching
NCT00770133 (8) [back to overview]Percentage of Eyes With hTearing
NCT00770133 (8) [back to overview]Percentage of Eyes With Ocular Mucus Discharge

Chemosis

Chemosis was evaluated by the Investigator at 7, 15, and 20 minutes post challenge on a 0-4 numerical analog scale, allowing 0.5-unit increments, where: 0.0 = None and 4.0 = Extremely severe. (NCT00769886)
Timeframe: 7, 15, and 20 minutes post challenge at 14 days

,,
Interventionscore on a scale (Mean)
7 minutes post-challenge15 minutes post-challenge20 minutes post-challenge
KetoNaph0.220.290.34
Ketotifen0.220.420.41
Naphazoline0.510.660.66

[back to top]

Ciliary Redness

Ciliary hyperemia (redness) was evaluated by the Investigator at 7, 15, and 20 minutes post challenge. Assessments were made using a 0-4 scale, allowing 0.5- unit increments, with 0.0 = None and 4.0 = Extremely severe. (NCT00769886)
Timeframe: 7, 15, and 20 minutes post challenge at 14 days

,,
Interventionunits on a scale (Mean)
7 minutes post-challenge15 minutes post-challenge20 minutes post-challenge
KetoNaph1.051.281.15
Ketotifen1.391.791.77
Naphazoline1.661.711.58

[back to top]

Conjunctival Hyperemia

Conjunctival hyperemia was evaluated by the Investigator at 7, 15, and 20 minutes post challenge. Assessments were completed using a 0-4 numerical analog scale, allowing 0.5-unit increments, where: 0.0 = None and 4.0 = Extremely severe. (NCT00769886)
Timeframe: 7, 15, and 20 minutes post challenge at 14 days

,,,
Interventionunits on a scale (Mean)
7 minutes post-challenge15 minutes post-challenge20 minutes post-challenge
KetoNaph1.131.391.26
Ketotifen1.491.891.77
Naphazoline1.621.681.53
Vehicle2.242.332.24

[back to top]

Episcleral Redness

Episcleral hyperemia (redness) was evaluated by the Investigator at 7, 15, and 20 minutes post challenge. Assessments were made using a 0-4 scale, allowing 0.5- unit increments, with 0.0 = None and 4.0 = Extremely severe. (NCT00769886)
Timeframe: 7, 15, and 20 minutes post challenge at 14 days

,,
Interventionscore on a scale (Mean)
7 minutes post-challenge15 minutes post-challenge20 minutes post-challenge
KetoNaph1.211.411.35
Ketotifen1.521.871.88
Naphazoline1.711.771.68

[back to top]

Eyelid Swelling

Lid swelling was evaluated by the subject at 7, 15, and 20 minutes post challenge on a 0- 3 numerical analog scale, with 0.5-unit increments disallowed, where: 0.0 = None and 3.0 = Severe. (NCT00769886)
Timeframe: 7, 15, and 20 minutes post challenge at 14 days

,,
Interventionscore on a scale (Mean)
7 minutes post-challenge15 minutes post-challenge20 minutes post-challenge
KetoNaph0.130.250.26
Ketotifen0.320.370.39
Naphazoline0.610.610.59

[back to top]

Ocular Itching

Ocular itching was evaluated by the participant at 3, 5, and 7 minutes post challenge. Assessments were made using a 0-4 numerical analog scale, allowing 0.5-unit increments (but disallowing 0.25-unit increments), where: 0.0 = None and 4.0 = Incapacitating itch with an irresistible urge to rub. (NCT00769886)
Timeframe: 3, 5, and 7 minutes post challenge at 14 days

,,,
Interventionscore on a scale (Mean)
3 minutes post-challenge5 minutes post-challenge7 minutes post-challenge
KetoNaph0.500.560.56
Ketotifen0.490.690.72
Naphazoline1.871.901.75
Vehicle1.932.171.97

[back to top]

Percentage of Eyes With Ocular Mucus Drainage

Ocular mucous discharge was evaluated by the Investigator at 7, 15, and 20 minutes post challenge. Mucous discharged was recorded as either absent or present. (NCT00769886)
Timeframe: 7, 15, and 20 minutes post challenge at 14 days

,,
Interventioneyes (Count of Units)
7 minutes post-challenge15 minutes post-challenge20 minutes post-challenge
KetoNaph71110
Ketotifen121916
Naphazoline131818

[back to top]

Percentage of Eyes With Tearing

Tearing was evaluated by the subject at 7, 15, and 20 minutes post challenge (absent or present). Tearing was recorded as either absent or present. (NCT00769886)
Timeframe: 7, 15, and 20 minutes post challenge at 14 days

,,
Interventioneyes (Count of Units)
7 minutes post-challenge15 minutes post-challenge20 minutes post-challenge
KetoNaph365
Ketotifen1177
Naphazoline231613

[back to top]

Chemosis

Chemosis was evaluated by the Investigator at 7, 15, and 20 minutes post challenge on a 0-4 numerical analog scale, allowing 0.5-unit increments, where: 0.0=None and 4.0=Extremely severe. (NCT00770133)
Timeframe: 7, 15, and 20 minutes post challenge at 14 days

,,
Interventionscore on a scale (Mean)
7 minutes post-challenge15 minutes post-challenge20 minutes post-challenge
Ketotifen0.280.460.49
Ketotifen/Naphazoline0.270.340.39
Naphazoline0.390.540.54

[back to top]

Ciliary Redness

Ciliary hyperemia (redness) was evaluated by the Investigator at 7, 15, and 20 minutes post challenge. Assessments were made using the same 0-4 scale, allowing 0.5-unit increments, where: 0.0=None and 4.0=Extremely severe. (NCT00770133)
Timeframe: 7, 15, and 20 minutes post challenge at 14 days

,,
Interventionscore on a scale (Mean)
7 minutes post-challenge15 minutes post-challenge20 minutes post-challenge
Ketotifen1.331.761.76
Ketotifen/Naphazoline0.811.051.04
Naphazoline1.491.591.54

[back to top]

Conjunctival Redness

Conjunctival hyperemia was evaluated by the Investigator at 7, 15, and 20 minutes post challenge. Assessments were completed using a 0-4 numerical analog scale, allowing 0.5-unit increments, where: 0.0=None and 4.0=Extremely severe. (NCT00770133)
Timeframe: 7, 15, and 20 minutes post challenge at 14 days

,,,
Interventionscore on a scale (Mean)
7 minutes post-challeng15 minutes post-challenge20 minutes post-challenge
Ketotifen1.491.801.88
Ketotifen/Naphazoline0.891.131.13
Naphazoline1.631.691.57
Vehicle2.062.262.18

[back to top]

Episcleral Redness

Episcleral hyperemia (redness) was evaluated by the Investigator at 7, 15, and 20 minutes post challenge. Assessments were made using the same 0-4 scale, allowing 0.5-unit increments, where: 0.0=None and 4.0=Extremely severe. (NCT00770133)
Timeframe: 7, 15, and 20 minutes post challenge at 14 days

,,
Interventionscore on a scale (Mean)
7 minutes post-challenge15 minutes post-challenge20 minutes post-challenge
Ketotifen1.511.761.88
Ketotifen/Naphazoline0.911.171.15
Naphazoline1.651.681.60

[back to top]

Eyelid Swelling

Lid swelling was evaluated by the participant at 7, 15, and 20 minutes post challenge on a 0-3 numerical analog scale, with 0.5-unit increments disallowed, where: 0.0=None and 3.0=Severe. (NCT00770133)
Timeframe: 7, 15, and 20 minutes post challenge at 14 days

,,
Interventionscore on a scale (Mean)
7 minutes post-challenge15 minutes post-challenge20 minutes post-challenge
Ketotifen0.20.20.2
Ketotifen/Naphazoline0.20.20.2
Naphazoline0.20.20.2

[back to top]

Ocular Itching

Ocular itching was evaluated by the participant at 3, 5, and 7 minutes post challenge. Assessments were made using a 0-4 numerical analog scale, allowing 0.5-unit increments (but disallowing 0.25-unit increments), where: 0.0=None and 4.0=Incapacitating itch with an irresistible urge to rub (NCT00770133)
Timeframe: 3, 5, and 7 minutes post challenge at 14 days

,,,
Interventionscore on a scale (Mean)
3 minutes post-challenge5 minutes post-challenge7 minutes post-challenge
Ketotifen0.400.590.56
Ketotifen/Naphazoline0.430.650.60
Naphazoline1.601.671.54
Vehicle1.811.961.84

[back to top]

Percentage of Eyes With hTearing

Tearing was evaluated by the participant at 7, 15, and 20 minutes post challenge. Tearing was recorded as either absent or present. (NCT00770133)
Timeframe: 7, 15, and 20 minutes post challenge at 14 days

,,
Interventioneyes (Count of Units)
7 minutes post-challenge15 minutes post-challenge20 minutes post-challenge
Ketotifen1196
Ketotifen/Naphazoline745
Naphazoline131211

[back to top]

Percentage of Eyes With Ocular Mucus Discharge

Ocular mucous discharge was evaluated by the Investigator at 7, 15, and 20 minutes post challenge. Mucous discharged was recorded as either absent or present. (NCT00770133)
Timeframe: 7, 15, and 20 minutes post challenge at 14 days

,,
Interventioneyes (Count of Units)
7 minutes post-challenge15 minutes post-challenge20 minutes post-challenge
Ketotifen000
Ketotifen/Naphazoline000
Naphazoline000

[back to top]