Page last updated: 2024-11-04

chlorpheniramine

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Description

Chlorpheniramine is an antihistamine medication used to treat allergic symptoms like sneezing, runny nose, itchy eyes, and hives. It blocks the effects of histamine, a chemical released by the body during allergic reactions. Chlorpheniramine is typically taken by mouth as a tablet, capsule, or syrup. It can also be administered as an injection. Chlorpheniramine is synthesized through a multi-step process involving the reaction of various organic compounds. It is studied to understand its mechanism of action, efficacy, and safety. Its importance lies in its ability to alleviate allergic symptoms and improve the quality of life for people with allergies.'

Chlorpheniramine: A histamine H1 antagonist used in allergic reactions, hay fever, rhinitis, urticaria, and asthma. It has also been used in veterinary applications. One of the most widely used of the classical antihistaminics, it generally causes less drowsiness and sedation than PROMETHAZINE. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

chlorphenamine : A tertiary amino compound that is propylamine which is substituted at position 3 by a pyridin-2-yl group and a p-chlorophenyl group and in which the hydrogens attached to the nitrogen are replaced by methyl groups. A histamine H1 antagonist, it is used to relieve the symptoms of hay fever, rhinitis, urticaria, and asthma. [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 CID2725
CHEMBL ID505
CHEBI ID52010
SCHEMBL ID4219
MeSH IDM0004190

Synonyms (129)

Synonym
BRD-A04553218-050-03-0
KBIO1_000596
DIVK1C_000596
3-(4-chlorophenyl)-n,n-dimethyl-3-pyridin-2-ylpropan-1-amine
2-pyridinepropanamine, .gamma.-(4-chlorophenyl)-n,n-dimethyl-
n.-propanamine, 3-(4-chlorophenyl)-3-(2-pyridyl)-n,n-dimethyl-
BSPBIO_000134
LOPAC0_000261
clofeniramina (tn)
D07398
chlorphenamine (inn)
IDI1_000596
BPBIO1_000148
PRESTWICK3_000117
clorfeniramina [italian]
chloroprophenpyridamine
einecs 205-054-0
clorfenamina [inn-spanish]
4-chloropheniramine
haynon
histadur
polaronil
chlorpheniraminum
chlorphenaminum [inn-latin]
2-(p-chloro-alpha-(2-(dimethylamino)ethyl)benzyl)pyridine
hsdb 3032
chlorprophenpyridamine
cloropiril
chlorphenamine [inn]
allergican
chloropheniramine
allergisan
chloropiril
hayon
chlorpheniramine
C06905
chlorphenamine
132-22-9
chlor-pro
3-(4-chlorophenyl)-n,n-dimethyl-3-(2-pyridyl)propan-1-amine
chlor-trimeton
telachlor
piriiton
2-pyridinepropanamine, gamma-(4-chlorophenyl)-n,n-dimethyl-
aller-chlor
teldrin
phenetron
chlorophenylpyridamine
DB01114
chlorpheniramine polistirex
1-(p-chlorophenyl)-1-(2-pyridyl)-3-n,n-dimethylpropylamine
gamma-(4-chlorophenyl)-n,n-dimethyl-2-pyridinepropanamine
gamma-(4-chlorophenyl)-gamma-(2-pyridyl)propyldimethylamine
2-[p-chloro-alpha-[2-(dimethylamino)ethyl]benzyl]pyridine
3-(p-chlorophenyl)-3-(2-pyridyl)-n,n-dimethylpropylamine
1-(p-chlorophenyl)-1-(2-pyridyl)-3-dimethylaminopropane
NINDS_000596
PRESTWICK1_000117
PRESTWICK0_000117
SPBIO_002073
PRESTWICK2_000117
OPREA1_779072
NCGC00162108-01
chlorphenaminum
clorfeniramina
CHEBI:52010 ,
clofeniramina
chlorphenamin
clorfenamina
HMS2090M21
NCGC00015227-05
5-ht,n-acetyl
[3h]chlorpheniramine
bdbm35938
[3h]chlorphenamine
chembl505 ,
L000003
STK736174
3-(4-chlorophenyl)-n,n-dimethyl-3-(pyridin-2-yl)propan-1-amine
AKOS001650136
NCGC00162108-02
chlorpheniramine polistirex [usan]
3u6io1965u ,
unii-3u6io1965u
chlorphenamine [inn:ban]
BBL012285
CCG-108982
NCGC00015227-06
NCGC00015227-03
NCGC00015227-09
gtpl6976
chlorpheniramine [hsdb]
chlorpheniramine component of tuzistra
783ahi015x
chlorpheniramine [mi]
chlorpheniramine [vandf]
2-(p-chloro-.alpha.-(2-(dimethylamino)ethyl)benzyl)pyridine
tuzistra componenet of chlorpheniramine
chlorphenamine [who-dd]
AKOS022060794
SCHEMBL4219
n-[3-(4-chlorophenyl)-3-(2-pyridinyl)propyl]-n,n-dimethylamine #
pyridine, 2-[p-chloro-.alpha.-[2-(dimethylamino)ethyl]benzyl]-, (s)-(+)-
s-(+)-chlorpheniramine
.gamma.-(4-chlorophenyl)-n,n-dimethyl-2-pyridinepropanamine
2-pyridinepropanamine, .gamma.-(4-chlorophenyl)-n,n-dimethyl-, (s)-
W-108317
HMS3428J07
DTXSID0022804 ,
chlorpheniaramine maleate
Q420133
FT-0665002
FT-0772034
chlorpheniramine-d6see c424303
chloropheniramine-d4
BRD-A04553218-050-08-9
SB19135
SDCCGSBI-0050249.P002
NCGC00015227-19
dexchlorpheniramine free base
25523-97-1 (free base)
EN300-708772
[3-(4-chlorophenyl)-3-(pyridin-2-yl)propyl]dimethylamine
HY-B0286
CS-0009285
clorfenamina (inn-spanish)
chlorphenaminum (inn-latin)
dtxcid402804
r06ab04

Research Excerpts

Overview

Chlorpheniramine is an H1 receptor antagonist of the alkylamine class. It is a pharmaceutical pollutant and a precursor of carcinogenic nitrosamines during disinfection/oxidation.

ExcerptReferenceRelevance
"Chlorpheniramine is an H1 receptor antagonist of the alkylamine class. "( Chlorpheniramine poisoning as a potential cause of rhabdomyolysis.
Guo, Q; Lin, H; Lin, J, 2022
)
3.61
"Chlorpheniramine is a pharmaceutical widely used and found in water environments. "( Catalytic degradation of chlorpheniramine over GO-Fe
Chen, WH; Huang, CP; Huang, JR; Lin, CH, 2020
)
2.3
"Chlorpheniramine maleate (CPM) is a first-generation antihistamine, which also has anticholinergic effects."( Effects of Chlorpheniramine Maleate on Catheter-Related Bladder Discomfort in Patients Undergoing Ureteroscopic Stone Removal: A Randomized Double-Blind Study.
Cho, CK; In, CB; Jee, YS; Lee, SJ; Sung, TY, 2021
)
1.73
"Chlorpheniramine (CPM) is an illegal additive found in herbal teas and health foods, and its excessive intake can cause health problems. "( A fluorescence based immunochromatographic sensor for monitoring chlorpheniramine and its comparison with a gold nanoparticle-based lateral-flow strip.
Guo, L; Kuang, H; Liu, L; Wang, L; Xu, C; Xu, X; Zhou, S, 2021
)
2.3
"Chlorpheniramine is a potent antihistaminic administered as a racemic mixture, while its clinical activity is mainly associated with the S-enantiomer. "( The cation-selective exhaustive injection and sweeping capillary electrophoresis method for the analysis of chlorpheniramine enantiomers in rat plasma.
Guo, X; Li, M; Yao, Y; Zhou, L, 2018
)
2.14
"Chlorpheniramine is a pharmaceutical pollutant and a precursor of carcinogenic nitrosamines during disinfection/oxidation. "( Removal of chlorpheniramine and variations of nitrosamine formation potentials in municipal wastewaters by adsorption onto the GO-Fe
Chen, CH; Chen, WH; Li, CM; Lin, CH, 2019
)
2.35
"Chlorpheniramine is a selective antagonist of the H1 histaminergic receptor subtype and its effects in humans include somnolence. "( The H1 histamine receptor blocker, chlorpheniramine, completely prevents the increase in REM sleep induced by immobilization stress in rats.
Cintra-McGlone, L; Esqueda-Leon, E; Jimenez-Anguiano, A; Mendoza Melendez, MA; Rojas-Zamorano, JA; Velazquez Moctezuma, J, 2009
)
2.07
"Chlorpheniramine is an anti-histamine agent on IgE-mediated inflammation. "( Enhancement of B cell and monocyte populations in rats exposed to chlorpheniramine.
Choi, WH; Jung, KJ; Koh, WS; Lee, SH; Park, SY; Yoo, JS, 2012
)
2.06
"Dexchlorpheniramine (DH) is a classical or first generation antihistamine belonging to the ethanolamine group. "( Allergy to dexchlorpheniramine. Study of a case.
Cáceres Calle, O; Fernández-Benítez, M,
)
1.11
"Chlorpheniramine maleate is a stable, most potent, sedative first generation anti-histamine and is effective in the treatment of allergic disorders."( To evaluate and compare the effects of first generation anti-histamine (chlorpheniramine maleate) and second generation anti-histamine (loratadine) on isolated trachea of rabbit.
Aamir, K; Ashraf, R; Jalbani, GA; Shaikh, AM; Soomro, FM; Unar, MA, 2004
)
1.28
"Chlorpheniramine (CPAM) is a chiral antihistaminic drug commercialized as a racemic mixture. "( Intestinal absorption and metabolism of chlorpheniramine enantiomers in rat.
Banide, H; Farinotti, R; Fernandez, C; Gimenez, F; Hiep, BT; Lacour, B; Thuillier, A; Tod, M, 2001
)
2.02

Effects

Chlorpheniramine has a serum half-life of approximately 20 hours in adults, and elimination from the body is primarily by metabolism to monodesmethyl and didesmethyl compounds. Chlor pheniramine maleate has some side effects when taken orally.

ExcerptReferenceRelevance
"Chlorpheniramine has a serum half-life of approximately 20 hours in adults, and elimination from the body is primarily by metabolism to monodesmethyl and didesmethyl compounds."( Clinical pharmacokinetics of chlorpheniramine.
Rumore, MM, 1984
)
1.28
"Chlorpheniramine has antimuscarinic properties."( Effect of chlorpheniramine administration on postoperative catheter-related bladder discomfort in patients undergoing transurethral excision of bladder tumor: a prospective randomized study.
Cho, JE; Huh, H; Kim, HC; Lee, SW, 2021
)
1.75
"Chlorpheniramine also has the potential to be administered transdermally."( Chlorpheniramine for motion sickness.
Alvarenga, D; Buckey, JC; Cole, B; Rigas, JR, 2004
)
2.49
"Chlorpheniramine maleate has some side effects when taken orally."( In vitro and ex vivo permeation studies of chlorpheniramine maleate gels prepared by carbomer derivatives.
Baykara, T; Ozkan, Y; Savaşer, A; Taş, C, 2004
)
1.31
"Chlorpheniramine might have been the first safe, non-cardiotoxic and well-tolerated antidepressant."( Chlorpheniramine, selective serotonin-reuptake inhibitors (SSRIs) and over-the-counter (OTC) treatment.
Hellbom, E, 2006
)
2.5
"Chlorpheniramine has a serum half-life of approximately 20 hours in adults, and elimination from the body is primarily by metabolism to monodesmethyl and didesmethyl compounds."( Clinical pharmacokinetics of chlorpheniramine.
Rumore, MM, 1984
)
1.28

Actions

ExcerptReferenceRelevance
"Chlorpheniramine is known to cause drowsiness, and this side effect has a potential to impair performance and could be a factor in accidents."( Prevalence of chlorpheniramine in aviation accident pilot fatalities, 1991-1996.
Canfield, DV; Chaturvedi, AK; Soper, JW, 2000
)
2.11

Treatment

Pretreatment with chlorpheniramine (50 nmol icv) inhibited the increase in MAP, PP, HR and survival rate produced by histamine. The scratching behavior induced by norbinaltorphimine was dose-dependently and significantly inhibited by pretreatment with U-50,488H (trans-(+/-)-2-(3,4-dichlorophenyl)-N-methyl-N-[2-(1-pyrrolidinyl)cyclohexyl] acetamide methansulfonate.

ExcerptReferenceRelevance
"Chlorpheniramine as a simple treatment was provided for this syndrome."( A 14-year-old female with fever, rash, lymphadenopathy, and pancytopenia: a case report.
Bayatmakoo, Z; Naghili, B; Poorshahverdi, P; Ravanbakhsh Gavgani, F; Ravanbakhsh Gavgani, R; Varshochi, M, 2020
)
2
"Chlorpheniramine pretreatment prevented death, delayed the onset of respiratory symptoms and decreased the severity of the hypersensitivity reaction."( Use of a simple in vivo technique to investigate components of the immediate hypersensitivity reaction in conscious guinea pigs.
Hammerbeck, DM; Swingle, KF, 1984
)
0.99
"Chlorpheniramine pretreatment (0.2 mg/kg iv) reduced the response to the initial dose of atracurium to only 26 +/- 14% (10 sublobar segments)."( Mechanism of action of atracurium on airways.
Hirshman, CA; Lindeman, KS; Mehr, EH, 1992
)
1
"Chlorpheniramine pretreatment prevented increases in resistance but not decreases in compliance."( Immunoglobulin E anaphylaxis in rabbits: mechanisms of pulmonary resistance and compliance changes.
Baumgartener, CC; Dunn, AM; Habib, MP; Halonen, M; Newell, JD; Sobonya, RE, 1988
)
1
"pretreatment with chlorpheniramine attenuated the histamine-induced increase in MAP, HR and decreased vascular conductance."( A role for the central histaminergic system in the leptin-mediated increase in cardiovascular dynamics.
Dunbar, JC; Rao, SP, 2005
)
0.65
"Pretreatment with chlorpheniramine did not change the histamine-induced analgesia, whereas the histamine effect on pain was inhibited with ranitidine pretreatment."( Central effect of histamine in a rat model of acute trigeminal pain.
Hamzeh-Gooshchi, N; Khalilzadeh, E; Seiednejhad-Yamchi, S; Tamaddonfard, E,
)
0.45
"Treatment with chlorpheniramine prevented the inhibitory effect of aspirin or tranylcypromine."( Involvement of endogenous prostaglandin I2 in the vascular action of histamine in dogs.
Konishi, M; Miyazaki, M; Toda, N, 1982
)
0.6
"Pretreatment with chlorpheniramine (50 nmol icv), H1 receptor antagonist, inhibited the increase in MAP, PP, HR and survival rate produced by histamine, while chlorpheniramine given alone had no effect."( Cardiovascular effects of histamine administered intracerebroventricularly in critical haemorrhagic hypotension in rats.
Jochem, J, 2000
)
0.63
"pretreatment with chlorpheniramine. The scratching behavior induced by norbinaltorphimine was dose-dependently and significantly inhibited by pretreatment with U-50,488H (trans-(+/-)-2-(3,4-dichlorophenyl)-N-methyl-N-[2-(1-pyrrolidinyl)cyclohexyl] acetamide methansulfonate), a kappa-opioid receptor agonist."( Norbinaltorphimine, a selective kappa-opioid receptor antagonist, induces an itch-associated response in mice.
Kamei, J; Nagase, H, 2001
)
0.63
"Pretreatment with chlorpheniramine antagonized the effects of morphine on pulmonary resistance, dynamic compliance and arterial blood pressure."( Effect of butorphanol and morphine on pulmonary mechanics, arterial blood pressure and venous plasma histamine in the anesthetized dog.
Buyniski, JP; Cavanagh, RL; Schurig, JE, 1978
)
0.58
"Pretreatment with chlorpheniramine (0.2 mg/kg iv) totally prevented increases in Rcs (9 sublobar segments)."( Mechanism of action of atracurium on airways.
Hirshman, CA; Lindeman, KS; Mehr, EH, 1992
)
0.61
"Pretreatment with chlorpheniramine (H1-antagonist) blocked the changes in Vtr and VH2O, and attenuated the increase in Qtrn."( Effect of histamine on tracheal mucosal perfusion, water content and airway smooth muscle in sheep.
Chediak, AD; Csete, ME; Elsasser, S; Gazeroglu, H; Wanner, A, 1991
)
0.6

Toxicity

The antihistamine chlorpheniramine presents multiple adverse side effects on the central nervous system. The groups that received 2 sprays of azelastine per nostril once and twice daily had statistically significantly more improvement.

ExcerptReferenceRelevance
" Cards were completed hourly to evaluate symptoms of allergic rhinitis and adverse experiences caused by therapy."( Randomized, double-blind, parallel groups, placebo-controlled study of efficacy and safety of Rynatan in the treatment of allergic rhinitis using an acute model.
Donnelly, A; Gellhaus, M; Weiler, JM; Weiler, K, 1990
)
0.28
" Loratadine appears to be a simple, effective and safe therapy for seasonal allergic rhinitis."( Efficacy and safety of loratadine suspension in the treatment of children with allergic rhinitis.
Andreoli, A; Boner, AL; Marchesi, E; Miglioranzi, P; Richelli, C, 1989
)
0.28
" Elicited, volunteered, and observed adverse experiences were recorded for each subject and compared among groups."( Multicenter, double-blind, multiple-dose, parallel-groups efficacy and safety trial of azelastine, chlorpheniramine, and placebo in the treatment of spring allergic rhinitis.
Campbell, BH; Connell, JT; Diamond, L; Donnelly, A; Hamilton, LH; Hemsworth, GR; Perhach, JL; Rosenthal, RR; Weiler, JM, 1988
)
0.49
" Diary cards were completed hourly (11:00 AM to 4:00 PM) and at 6:00, 8:00, and 10:00 PM on Saturday and again hourly on Sunday (from 8:00 AM to 4:00 PM) to evaluate rhinitis symptoms and adverse events."( A dose-ranging study of the efficacy and safety of azelastine nasal spray in the treatment of seasonal allergic rhinitis with an acute model.
Benson, PM; Freitag, J; Meltzer, EO; Weiler, JM; Weiler, K; Widlitz, MD, 1994
)
0.29
" The groups that received 2 sprays of azelastine per nostril once and twice daily and the chlorpheniramine group had statistically significantly more improvement in total rhinitis symptoms than the placebo group without serious adverse events."( A dose-ranging study of the efficacy and safety of azelastine nasal spray in the treatment of seasonal allergic rhinitis with an acute model.
Benson, PM; Freitag, J; Meltzer, EO; Weiler, JM; Weiler, K; Widlitz, MD, 1994
)
0.51
" There were no clinical or statistical differences in adverse effects between the two medications or between each medication and baseline."( Comparison of CNS adverse effects between astemizole and chlorpheniramine in children: a randomized, double-blind study.
Feldman, W; Leikin, L; Peterson, R; Pong, AH; Shanon, A; Williams, V, 1993
)
0.53
"The two antihistamines studied had no adverse effects on the performance of children."( Comparison of CNS adverse effects between astemizole and chlorpheniramine in children: a randomized, double-blind study.
Feldman, W; Leikin, L; Peterson, R; Pong, AH; Shanon, A; Williams, V, 1993
)
0.53
" The toxic effect was observed only in mice with a cryptococcal infection and was reduced or absent in the early and late stages of disease."( Acute lethal toxicity following passive immunization for treatment of murine cryptococcosis.
Kozel, TR; Lupan, DM; Manalo, PB; Roberts, JS; Savoy, AC; Schlageter, AM; Weinhold, LC, 1997
)
0.3
"The antihistamine chlorpheniramine presents multiple adverse side effects on the central nervous system."( [The potential P300 in the evaluation of the side effects of dexchlorpheniramine].
Escera, C; Grau, C; Sánchez-Turet, M; Serra-Grabulosa, JM,
)
0.7
" However, there are many reports in the literature of life-threatening adverse effects of these drugs."( [Herbal medicines and severe adverse effects: uvular angioedema caused by Echballium elaterium].
Cabrera, D; Caiozzi, G; Mardónez, JM; Saldías, F, 2002
)
0.31
" There were 54 patients who reported 61 adverse events."( [A clinical trial to evaluate the efficacy and safety of compound pseudoephedrine hydrochloride sustained release capsule in patients with seasonal allergic rhinitis].
, 2004
)
0.32
"To compare the adverse effects of two regimens of chlorpheniramine plus chloroquine (CP+CQ) in children who live in a country where chloroquine resistant malaria is endemic."( Potential toxicity of chlorpheniramine plus chloroquine for the treatment of childhood malaria.
Adedapo, AD; Adedapo, KS; Ademowo, OG; Demissie, K; Osinubi, OY, 2009
)
0.92
" Secondary end-points were the rate of control of chronic cough at each step of therapy, the duration of treatment required, changes in cough symptom score, health-related quality of life and possible adverse effects."( Efficacy and safety of modified sequential three-step empirical therapy for chronic cough.
Li, X; Liang, S; Liu, B; Lü, H; Qiu, Z; Wang, L; Wang, Y; Wei, W; Yu, L, 2010
)
0.36
" Using chlorpheniramine maleate as a representative analyte and n-butyl acetate as a less toxic and non-ozone depleting extractant, the miniaturized method was less laborious and much faster."( Operator care and eco-concerned development of a fast, facile and economical assay for basic nitrogenous drugs based on simplified ion-pair mini-scale extraction using safer solvent combined with drop-based spectrophotometry.
Buacheen, P; Ngawhirunpat, T; Opanasopit, P; Plianwong, S; Rojanarata, T; Sripattanaporn, A; Waewsa-nga, K, 2012
)
0.83
"Auron Misheil therapy was shown to be well tolerated, revealing no severe or serious adverse events."( A phase I trial assessing the safety, tolerability, pharmacokinetic and pharmacodynamic characteristics of single-dose Auron Misheil therapy in healthy male subjects.
Diergarten, K; Drevs, J; Niazi, FR; Scheele, J, 2013
)
0.39
"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
"We selected adverse drug reaction (ADR) reports on H1-antihistamines in children (0-16 years) up to June 2014 from VigiBase."( Safety profile of H1-antihistamines in pediatrics: an analysis based on data from VigiBase.
Biagi, C; Calamelli, E; Cipriani, F; Donati, M; Melis, M; Monaco, L; Motola, D; Ricci, G; Vaccheri, A, 2017
)
0.46

Pharmacokinetics

Chlorpheniramine half-life is longer than previously reported. Serum concentrations and urinary recovery of (S)-(+)- and (R)-(-)-chlorpheniramines were unaffected by administration of ranitidine.

ExcerptReferenceRelevance
" 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
" Recent studies have established that the half-life of chlorpheniramine is longer than previously reported."( Clinical pharmacokinetics of chlorpheniramine.
Rumore, MM, 1984
)
0.81
" In 11 patients with allergic rhinitis, ages 6 to 16 yr, we found a mean serum chlorpheniramine half-life of 13."( Pharmacokinetics and efficacy of chlorpheniramine in children.
Luciuk, GH; Simons, FE; Simons, KJ, 1982
)
0.77
" Valproic acid elimination half-life was 3 h during the 190 min hemoperfusion cycle."( Delayed peak serum valproic acid in massive divalproex overdose--treatment with charcoal hemoperfusion.
Aaron, CK; Graudins, A, 1996
)
0.29
"The chlorpheniramine and diphenhydramine terminal elimination half-life values and area under the curve values were significantly increased, and the systemic clearance rates were significantly decreased, during concomitant administration of cimetidine."( Effect of cimetidine on the pharmacokinetics and pharmacodynamics of chlorpheniramine and diphenhydramine in rabbits.
Chen, X; Fraser, TG; Simons, FE; Simons, KJ, 1996
)
1.09
"Any enhanced peripheral H1-blockade observed could be attributed, at least in part, to a pharmacokinetic interaction."( Effect of cimetidine on the pharmacokinetics and pharmacodynamics of chlorpheniramine and diphenhydramine in rabbits.
Chen, X; Fraser, TG; Simons, FE; Simons, KJ, 1996
)
0.53
" 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
"Two methods to confirm attainment of steady-state conditions in multiple-dose bioequivalence studies are described and evaluated: (1) the Cmin method and (2) the Area Below the Cmin plasma-concentration-versus-time-curve method (ABCM method)."( Evaluation of a Cmin and a normalized Cmin method for the confirmation of steady-state in bioequivalence studies.
Jackson, AJ, 1998
)
0.3
"The Cmin method more accurately predicted the attainment of steady-state conditions for immediate-release formulations compared to the ABCM method."( Evaluation of a Cmin and a normalized Cmin method for the confirmation of steady-state in bioequivalence studies.
Jackson, AJ, 1998
)
0.3
" Serum concentrations and urinary recovery of (S)-(+)- and (R)-(-)-chlorpheniramine were unaffected by administration of ranitidine, indicating no pharmacokinetic drug-drug interaction."( Stereoselective pharmacokinetics of chlorpheniramine and the effect of ranitidine.
Davis, IM; Koch, KM; O'Connor-Semmes, RL; Yin, Y, 1998
)
0.81
" The effects of this combination therapy on the pharmacokinetic disposition of CQ is, however, unpredictable."( Effect of chlorpheniramine on the pharmacokinetics of and response to chloroquine of Nigerian children with falciparum malaria.
Afolabi, BM; Agomo, CO; Agomo, PU; Coker, HA; Mafe, AG; Ogunbanwo, JA; Okonkwo, CA,
)
0.53
" The various pharmacokinetic parameters of phenylpropanolamine were calculated using model independent methods."( Time dependent pharmacokinetic interaction between phenylpropanolamine and chlorpheniramine maleate in human subjects.
Rambhau, D; Rao, BR; Rao, VV; Srinivasu, P, 1999
)
0.53
"In extensive metabolizers, mean Cmax was greater (12."( The roles of CYP2D6 and stereoselectivity in the clinical pharmacokinetics of chlorpheniramine.
Fried, KM; Wainer, IW; Woosley, RL; Yasuda, SU; Young, AE; Zannikos, P, 2002
)
0.54
" A comparison is also presented between several methods based on animal pharmacokinetic data, using the same set of proprietary compounds, and it lends further support for the use of this method, as opposed to methods that require the gathering of pharmacokinetic data in laboratory animals."( Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics.
Gao, F; Lombardo, F; Obach, RS; Shalaeva, MY, 2004
)
0.32
"As the mechanism involved in the serious adverse effects associated with phenylpropanolamine (PPA) has not yet been clarified, and as PPA in usual cases is not being ingested without other drugs combination, the aim of this study was to characterize the possibility of pharmacokinetic interactions between PPA and most often combined drugs existing in the same dosage."( Pharmacokinetic interactions between phenylpropanolamine, caffeine and chlorpheniramine in rats.
Kaddoumi, A; Nakashima, K; Nakashima, MN; Wada, M, 2004
)
0.56
"Quantitative structure-pharmacokinetic relationships (QSPkR) have increasingly been used for the prediction of the pharmacokinetic properties of drug leads."( Quantitative structure-pharmacokinetic relationships for drug clearance by using statistical learning methods.
Chen, YZ; Li, ZR; Yap, CW, 2006
)
0.33
" pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data."( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
Lombardo, F; Obach, RS; Waters, NJ, 2008
)
0.35
"5 × 10(-7)g/L based on a signal-to-noise of 3 (S/N=3) with 751- to 1372-fold increases in detection sensitivity for analytes, and it was successfully applied to the pharmacokinetic study of three antihistamines in human urine after an oral administration."( Trace analysis of three antihistamines in human urine by on-line single drop liquid-liquid-liquid microextraction coupled to sweeping micellar electrokinetic chromatography and its application to pharmacokinetic study.
Chen, G; Chen, Y; Gao, W; Xi, J; Xu, N; Yang, J, 2012
)
0.38
" This phase I study was conducted to assess the safety, tolerability, and pharmacokinetic (PK) and pharmacodynamic (PD) properties of AMT in a controlled trial environment."( A phase I trial assessing the safety, tolerability, pharmacokinetic and pharmacodynamic characteristics of single-dose Auron Misheil therapy in healthy male subjects.
Diergarten, K; Drevs, J; Niazi, FR; Scheele, J, 2013
)
0.39
"To investigate the herb-drug pharmacokinetic interaction of artificial calculus bovis (ACB) with diclofenac sodium (DS) and chlorpheniramine maleate (CPM) in rats."( Herb-drug pharmacokinetic interaction of artificial calculus bovis with diclofenac sodium and chlorpheniramine maleate in rats.
Huang, Y; Lv, M; Peng, C; Tian, J; Tian, Y; Zhang, Z, 2013
)
0.82
" The proposed method was successfully applied to compare the herb-drug pharmacokinetic interaction of ACB with DS and CPM in rats following intragastric administration."( Herb-drug pharmacokinetic interaction of artificial calculus bovis with diclofenac sodium and chlorpheniramine maleate in rats.
Huang, Y; Lv, M; Peng, C; Tian, J; Tian, Y; Zhang, Z, 2013
)
0.61
" There was no apparent pharmacokinetic interaction between DS and CPM."( Herb-drug pharmacokinetic interaction of artificial calculus bovis with diclofenac sodium and chlorpheniramine maleate in rats.
Huang, Y; Lv, M; Peng, C; Tian, J; Tian, Y; Zhang, Z, 2013
)
0.61
"This study indicated that co-administration of ACB with DS and CPM can result in an apparent herb-drug pharmacokinetic interaction in rats."( Herb-drug pharmacokinetic interaction of artificial calculus bovis with diclofenac sodium and chlorpheniramine maleate in rats.
Huang, Y; Lv, M; Peng, C; Tian, J; Tian, Y; Zhang, Z, 2013
)
0.61
"Volume of distribution is one of the most important pharmacokinetic properties of a drug candidate."( Volume of Distribution in Drug Design.
Beaumont, K; Di, L; Maurer, TS; Smith, DA, 2015
)
0.42

Compound-Compound Interactions

Single doses of d-amphetamine, chlorpheniramine or diazepam were combined with ethanol under two conditions. The H1 blockers produced antinociception when given alone to mice and also caused potentiation when combined with morphine. We found that some antihistamines significantly potentiate methamphetamine-induced psychomotor activation in rats.

ExcerptReferenceRelevance
" The woman described in this article died after taking her usual dose of thioridazine, 100 mg/d, in combination with a single capsule of Contac."( Death attributed to ventricular arrhythmia induced by thioridazine in combination with a single Contac C capsule.
Chouinard, G; Ghadirian, AM; Jones, BD, 1978
)
0.26
" The potentiation of dihydrocodeine-conditioned place preference was observed by combination with chlorpheniramine (0."( Drug interactions in the reinforcing effects of over-the-counter cough syrups.
Masukawa, Y; Misawa, M; Suzuki, T, 1990
)
0.5
" The H1 blockers, including an ethylenediamine (pyrilamine), an ethanolamine (diphenhydramine), a phenothiazine (methdilazine), a piperazine (cyclizine) and an alkylamine (chlorpheniramine), all produced antinociception when given alone to mice and also caused potentiation when combined with morphine."( Effect of H1 blockers alone and in combination with morphine to produce antinociception in mice.
Hanig, JP; Hui, FW; Sun, CL, 1985
)
0.46
" The present study was designed to compare the effects of astemizole and chlorpheniramine, alone and in combination with alcohol, on an objective measure of psychomotor performance relating to car-driving ability."( Psychomotor effects of astemizole and chlorpheniramine, alone and in combination with alcohol.
Bhatti, JZ; Hindmarch, I, 1987
)
0.78
"Single doses of d-amphetamine, chlorpheniramine or diazepam were combined with ethanol under two conditions: (i) in drug-naive mice and (ii) in mice which had been given a single dose of ethanol 72 hr previously."( Drug interactions with ethanol. Effects on body temperature and motor impairment.
Maickel, RP; Nash, JF, 1986
)
0.56
" We found that some antihistamines significantly potentiate methamphetamine-induced psychomotor activation in rats and that plasma and brain tissue concentrations of methamphetamine in rats treated with methamphetamine in combination with D-chlorpheniramine were markedly higher than those in rats treated with methamphetamine alone."( Drug interaction between methamphetamine and antihistamines: behavioral changes and tissue concentrations of methamphetamine in rats.
Goto, J; Hishinuma, T; Ito, Y; Iwabuchi, K; Kitaichi, K; Nakagawa, N; Okuda, T; Tsukamoto, H; Watanabe, T; Yanai, K, 2004
)
0.51
"A fast, facile, and economical assay for basic nitrogenous drugs has been developed based on the mini-scale extraction of the drug-dye ion pair complex combined with the use of safe-for-analyst and eco-friendlier organic extractant and drop-based micro-spectrophotometry."( Operator care and eco-concerned development of a fast, facile and economical assay for basic nitrogenous drugs based on simplified ion-pair mini-scale extraction using safer solvent combined with drop-based spectrophotometry.
Buacheen, P; Ngawhirunpat, T; Opanasopit, P; Plianwong, S; Rojanarata, T; Sripattanaporn, A; Waewsa-nga, K, 2012
)
0.38

Bioavailability

The bioavailability of chlorpheniramine regular-release versus controlled-release products was compared using 15 human subjects. A male Caucasian who participated in six bioavailability studies in our laboratory over a period of several years showed extremely low clearance of two drugs.

ExcerptReferenceRelevance
" The in vivo bioavailability and pharmacokinetics of these formulations were evaluated in 24 healthy subjects under fasting conditions."( Correlation of in vitro release rate and in vivo absorption characteristics of four chlorpheniramine maleate extended-release formulations.
Cho, P; Lin, CC; Mojaverian, P; Radwanski, E; Rosen, JM; Vadino, WA, 1992
)
0.51
" A small (four subjects) relative bioavailability study based on average cumulative excretion of intact drug in urine gave results in parallel with substantially nonequivalent dissolution data for three products."( Chlorpheniramine dissolution and relative urinary excretion from commercial products.
Ayres, JW; Hsu, HY, 1989
)
1.72
" 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
" Absolute bioavailability from oral solution (10 mg) was 59 and 34%, and from tablets (8 mg) 44 and 25%, respectively, indicating extensive gut first-pass metabolism."( Pharmacokinetics of chlorpheniramine after intravenous and oral administration in normal adults.
Athanikar, NK; Chiou, WL; Huang, SM; Huang, YC; Sridhar, K, 1982
)
0.59
"The bioavailability of chlorpheniramine regular-release versus controlled-release products was compared using 15 human subjects."( Bioavailability of regular and controlled-release chlorpheniramine products.
Brown, WJ; Dighe, SV; Kotzan, JA; Malinowski, R; Needham, TE; Stewart, JT; Vallner, JJ; Viswanathan, CT, 1982
)
0.83
" The individual bioavailability data and the AUC of one of the demethylated metabolites, desdimethyl CPM (DDCPM) obtained following different doses suggested the existence of saturable presystemic elimination."( Oral absorption and presystemic first-pass effect of chlorpheniramine in rabbits.
Chiou, WL; Huang, SM; Huang, YC, 1981
)
0.51
"This investigation compared the bioavailability of chlorpheniramine and pseudoephedrine from a sustained-action capsule and a combination of two reference standard tablets in 24 normal human subjects."( Evaluation of sustained-action chlorpheniramine-pseudoephedrine dosage form in humans.
Amann, AH; Baaske, DM; Carter, JE; Chao, GC; Kamath, BL; Lai, CM; Stoll, RG; Yacobi, A, 1980
)
0.8
"This study was carried out to evaluate the bioavailability of a new regular release tablet formulation of chlorphenamine (CPA) (Histop) relative to a reference formula (Piriton) using 13 human healthy volunteers."( Bioequivalence and pharmacokinetics of chlorpheneramine in healthy human volunteers.
Al-Alsheikh, OA; Al-Dhawailie, AA; Najjar, TA; Shereif, A, 1995
)
0.29
" It also appears that the intranasal delivery of drugs with optimal physicochemical characteristics can result in an improved CNS bioavailability compared to those achieved from an equivalent parenteral dose."( Distribution of antihistamines into the CSF following intranasal delivery.
Chou, KJ; Donovan, MD, 1997
)
0.3
" A male Caucasian who participated in six bioavailability studies in our laboratory over a period of several years showed extremely low clearance of two drugs: phenytoin and glipizide (both substrates of CYP2C9), but not for nifedipine (a CYP3A4 substrate) and chlorpheniramine (a CYP2D6 substrate)."( Pharmacokinetics of chlorpheniramine, phenytoin, glipizide and nifedipine in an individual homozygous for the CYP2C9*3 allele.
Blaisdell, J; Dalton, JT; Goldstein, JA; Kidd, RS; Meyer, MC; Straughn, AB, 1999
)
0.81
"05) decrease in the rate of absorption of phenylpropanolamine following its administration in combination with chlorpheniramine maleate at 2200 hours."( Time dependent pharmacokinetic interaction between phenylpropanolamine and chlorpheniramine maleate in human subjects.
Rambhau, D; Rao, BR; Rao, VV; Srinivasu, P, 1999
)
0.75
"The quantitative structure-bioavailability relationship of 232 structurally diverse drugs was studied to evaluate the feasibility of constructing a predictive model for the human oral bioavailability of prospective new medicinal agents."( QSAR model for drug human oral bioavailability.
Topliss, JG; Yoshida, F, 2000
)
0.31
" The nasal administration showed that the systemic bioavailability at the two dose levels used was comparable to that for the tablet."( Systemic bioavailability of nasally applied chlorphenamine maleate (0.4% nasal spray) relative to tablets administered perorally.
Buchwald, A; de Mey, CM; Gercek, C; Stengele, E; Trenk, D; Van Toor, BS, 2001
)
0.31
" Because nicotine was postulated to be a beneficial component of tobacco smoke for ulcerative colitis, various formulations of nicotine have been developed to improve the local bioavailability within the gastrointestinal tissue."( Transport mechanisms of nicotine across the human intestinal epithelial cell line Caco-2.
Fukada, A; Inui, K; Saito, H, 2002
)
0.31
" Buccal formulations were developed with hydroxyethylcellulose (HEC) and evaluated for in vitro release, moisture absorption, mechanical properties, and bioadhesion, and optimized formulation was subjected for bioavailability studies in healthy human volunteers."( Transbuccal delivery of chlorpheniramine maleate from mucoadhesive buccal patches.
Gannu, R; Kishan, V; Naidu, KV; Rao, YM; Sekhar, KC; Vishnu, YV,
)
0.44
"Oral bioavailability (F) is a product of fraction absorbed (Fa), fraction escaping gut-wall elimination (Fg), and fraction escaping hepatic elimination (Fh)."( Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
Chang, G; El-Kattan, A; Miller, HR; Obach, RS; Rotter, C; Steyn, SJ; Troutman, MD; Varma, MV, 2010
)
0.36
"The intestinal mucosa plays a capital role in dictating the bioavailability of a large array of orally ingested drugs and toxicants."( Characterization of xenobiotic metabolizing enzymes in bovine small intestinal mucosa.
Cantiello, M; Carletti, M; Della Donna, L; Gardini, G; Girolami, F; Nebbia, C; Virkel, G, 2010
)
0.36
"Nasal administration has been of special interest in the last decade due to its feasibility and relative high bioavailability compared to the oral rout of administration."( Formulation and stability study of chlorpheniramine maleate nasal gel.
Abdou, EM; Soliman, II; Soliman, NA,
)
0.41
" The floating tablets of DCPM developed may be used clinically for prolonged drug release for at least 16 hrs, thereby improving bioavailability and patient compliance."( An approach to formulating an oral floating drug delivery system for dexchlorpheniramine maleate using factorial design.
Alabazi, MY; Elzein, H, 2012
)
0.61
"5mg/kg BW) resulted in a bioavailability of 38%, which induced a peak plasma drug concentration at 1h and a maximal inhibition of wheal formation (39%) at 2h."( Pharmacokinetics and pharmacodynamics of d-chlorpheniramine following intravenous and oral administration in healthy Thoroughbred horses.
Hariu, K; Kuroda, T; Kusano, K; Mizobe, F; Nagata, S; Takizawa, Y; Tamura, N, 2013
)
0.65
" The preclinical drug absorption rate was lower with calcium acetate loaded than calcium-free alginate pellets."( Drug release, preclinical and clinical pharmacokinetics relationships of alginate pellets prepared by melt technology.
Bose, A; Dan, S; Harjoh, N; Pal, TK; Wong, TW, 2016
)
0.43

Dosage Studied

A high-performance liquid chromatographic (HPLC) method has been developed for the quantitation of acetaminophen, chlorpheniramine maleate, dextromethorphan hydrobromide, and phenylpropanolamine hydrochloride. The principle of charge transfer complexation involving a pi-acceptor and an n-donor was utilized in the assay of the later in its pure form and in tablet dosage forms.

ExcerptRelevanceReference
" This drug is preferred over ephedrine primarily because of its sustained release, allowing dosage twice a day, and because of its relative freedom from side effects."( Urethral pressure profiles before and after Ornade administration in patients with stress urinary incontinence.
Montague, DK; Stewart, BH, 1979
)
0.26
"A specific high-pressure liquid chromatographic method for the determination of chlorpheniramine and pseudoephedrine in urine was developed and applied in a urinary excretion study of normal healthy subjects who received a sustained-release dosage form contianing 8 mgof chlorpheniramine maleate and 120 mg of pseudoephedrine hydrochloride."( Urinary excretion of chlorpheniramine and pseudoephedrine in humans.
Lai, CM; Look, ZM; Stoll, RG; Yacobi, A, 1979
)
0.81
" The provocation doses which produced a 20% fall in forced expiratory volume in 1 sec (FEV1) and the slopes of the dose-response curves were analyzed."( Bronchial hyperreactivity to histamine and methacholine in asthmatic children after inhalation of SCH 1000 and chlorpheniramine maleate.
Kattan, M; Levison, H; Orange, RP; Woenne, R, 1978
)
0.47
" Cocaine (2 x 10(-6) M and 10(-5) M) produced 2 and 7 fold shifts to the left of the dose-response curve to (-)-noradrenaline recorded isotonically in isolated splenic capsular strips of the cat."( Investigation of the role of calcium in the supersensitivity produced by cocaine in cat spleen strips.
Summers, RJ; Tillman, J, 1979
)
0.26
" After intravenous dosing the decline in chlorpheniramine plasma concentration was typically biexponential."( Chlorpheniramine. II. Effect of the first-pass metabolism on the oral bioavailability in dogs.
Athanikar, NK; Chiou, WL, 1979
)
1.97
"A simple and sensitive high-pressure liquid chromatographic (HPLC) determination of pseudoephedrine and chlorpheniramine in a pharmaceutical dosage form is described."( Simultaneous determination of pseudoephedrine and chlorpheniramine in pharmaceutical dosage forms.
Lai, CM; Look, ZM; Yacobi, A, 1978
)
0.73
" The application of the guaiacolsulfonate potassium assay method to commercial dosage forms is reported."( Colorimetric determinations of chlorpheniramine maleate, ephedrine hydrochloride, and guaiacolsulfonate potassium in a cough syrup.
Das Gupta, V; de Lara, AJ, 1975
)
0.54
" A general procedure is described for the isolation and infrared identification of the maleic acid moiety of pharmaceutical salts from drug substances or dosage forms."( Infrared identification of maleic acid in pharmaceutical maleate salts.
Brannon, WL; Levine, J; Schwartzman, G, 1976
)
0.26
" This short absorption time may be due to a short intestinal residence time for these dosage forms in the dog."( In vitro and in vivo correlation for controlled-release formulation of d-chlorpheniramine maleate.
Aoyagi, N; Katori, N; Okudaira, K; Takeda, Y; Uchiyama, M, 1991
)
0.51
" On the other hand, concurrent dosing of dihydrocodeine (2 mg/kg, IP) and a mixture (SC) of methylephedrine (4 mg/kg), caffeine (4 mg/kg) and chlorpheniramine (0."( Drug interactions in the reinforcing effects of over-the-counter cough syrups.
Masukawa, Y; Misawa, M; Suzuki, T, 1990
)
0.48
" All 43 dogs were known to be unresponsive to chlorpheniramine and the manufacturer's recommended dosage of the fatty acid supplement when either drug was used alone."( Nonsteroidal management of canine pruritus: chlorpheniramine and a fatty acid supplement (DVM Derm Caps) in combination, and the fatty acid supplement at twice the manufacturer's recommended dosage.
Miller, WH; Scott, DW, 1990
)
0.8
"Dissolution profiles were determined for seven commercially available nonprescription solid dosage forms containing chlorpheniramine (four sustained release and three immediate release)."( Chlorpheniramine dissolution and relative urinary excretion from commercial products.
Ayres, JW; Hsu, HY, 1989
)
1.93
" The inhibition of wheal size was maximal by 2 hr after dosing and was present at 8 hr."( Temelastine, a new H1-receptor antagonist.
Alexander, F; Allison, N; Dubb, JW; Familiar, RG; Stote, RM; Tatoian, D, 1986
)
0.27
"The dose-response curves of the central and peripheral airways to intravenously injected nicotine were studied in 55 anesthetized dogs."( Dose-response curves of central and peripheral airways to nicotine injections in dogs.
Haga, T; Miyano, M; Nakamura, M; Sasaki, H; Takishima, T, 1986
)
0.27
" All three antihistaminics, at some dosage levels, slightly increased activity when given alone, but strongly enhanced morphine-induced hyperactivity."( Enhancement of morphine-induced hyperactivity by antihistaminic drugs in mice.
Castellano, C; D'Amato, FR; Sansone, M, 1986
)
0.27
" A method that avoided tachyphylaxis encountered in prior investigations was developed for isometric measurement of multiple dose-response effects."( Parasympathetic involvement in PAF-induced contraction in canine trachealis in vivo.
Leff, AR; Munoz, NM; Popovich, KJ; Shioya, T; Stimler-Gerard, NP; White, SR, 1987
)
0.27
" All three antihistaminics, at some dosage levels, enhanced morphine-induced hyperactivity, but did not change or even reduce locomotor stimulation induced by amphetamine and scopolamine."( Antihistaminics enhance morphine-, but not amphetamine- and scopolamine-induced hyperactivity in mice.
D'Udine, B; Renzi, P; Sansone, M; Vetulani, J, 1987
)
0.27
" 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
)
0.49
" The cumulative results indicate that the nonsedative antihistamine terfenadine, given orally at a dosage of 60 mg twice daily, is effective in the treatment of seasonal allergic rhinitis in both adults and children."( The use of antihistamines for the treatment of airway disease.
Meltzer, EO, 1988
)
0.27
" The selective histamine H1-receptor antagonist chlorpheniramine shifted the dose-response curves of histamine and 2-PEA for inducing vasoconstriction to the right."( Characteristics of histamine receptors in the isolated and perfused canine coronary arteries.
Chiba, S; Nakane, T, 1987
)
0.53
" We determined the nebulizer concentration of PAF which reduced specific airway conductance (SGaw) 35% (PC35 SGaw) and the slope of the PAF dose-response curve."( Mechanism of platelet activating factor-induced bronchoconstriction in humans.
Patterson, R; Rubin, AH; Smith, LJ, 1988
)
0.27
"Cumulative dose-response curves for histamine induced responses in mesometrial (ME) and antimesometrial (AME) regions of uterine horns isolated from rats at 7th, 16th and 22nd days of pregnancy, were constructed."( Is there a prostaglandin involvement in the positive inotropic action of histamine in isolated pregnant rat uterus, apparently mediated via H1-receptors activation?
Dveksler, G; Franchi, AM; Gimeno, AL; Gimeno, MF; Viggiano, M, 1987
)
0.27
" The maximum effect of muricidal suppression lasted for 1-2 hr after oral dosage (10 mg/kg)."( Effect of chlorpheniramine on muricide induced by thiamine deficiency: pharmacokinetic and behavioral studies.
Niwa, H; Onodera, K; Sakurai, E, 1987
)
0.68
" One such case is reported in which a self administered high dosage of such a medication can be linked with a potentially life threatening anaesthetic complication."( Contac 400: a possible cause of aspiration under anaesthesia.
Wilkinson, DJ, 1987
)
0.27
"05) shifts to the right of the histamine dose-response curve in normal physiological salt solution (PSS)."( Differential effects of adenosine and verapamil on histamine vascular contractions.
Merrill, GF; Tozzi, CA, 1986
)
0.27
" Cimetidine shifted the dose-response curve for histamine to the right, but chlorpheniramine did not alter the response."( Mechanisms of histamine-induced relaxation in isolated monkey and dog coronary arteries.
Toda, N, 1986
)
0.5
" This was a 4-week study with a 1-week observation (baseline) period and a 3-week period during which the response to three dosage regimens (2 mg per day, 4 mg per day, and 8 mg per day) of FCB and placebo were compared to baseline observations of rhinitis."( Efficacy and tolerance of fluocortin butyl administered twice daily in adult patients with perennial rhinitis.
Hartley, TF; Lieberman, PL; Meltzer, EO; Noyes, JN; Pearlman, DS; Tinkelman, DG, 1985
)
0.27
" Dosage was two sprays into each nostril 4 times a day."( Sodium cromoglycate/chlorpheniramine and sodium cromoglycate nasal sprays in the treatment of seasonal rhinitis.
van Niekerk, CH, 1985
)
0.59
" The dose of chlorpheniramine (or placebo) was doubled from days 22 to 24 to assess the response to dosage increase."( The development of subsensitivity to chlorpheniramine.
Long, WF; Nelson, HS; Taylor, RJ, 1985
)
0.91
" Dose-response studies indicate that bradykinin is more potent than serotonin or histamine in respect of wealing."( Responses of skin blood vessels to bradykinin, histamine and 5-hydroxytryptamine.
Greaves, M; Shuster, S, 1967
)
0.25
" After daily repeated dosing with chlorpheniramine, [methylene-14C]chlorpheniramine maleate was given as a tracer and urine was collected until less than 1% of the labeled dose was excreted daily."( Isolation and identification of the polar metabolites of chlorpheniramine in the dog.
Carter, DE; Karakaya, A; Osterloh, JD,
)
0.66
" None of the terfenadein dosage schedules up to 200 mg tid caused sedation significantly different from that of placebo."( Clinical investigation of terfenadine, a non-sedating antihistamine.
Brandon, ML; Weiner, M, 1980
)
0.26
"This study was designed to determine the effect of a clinically used surfactant, docusate sodium, on the release of chlorpheniramine from a controlled-release dosage form (encapsulated coated pellets)."( Effect of docusate sodium on drug release from a controlled-release dosage form.
Chambliss, WG; Cleary, RW; Fischer, R; Jones, AB; Kibbe, AH; Nicholes, W; Skierkowski, P, 1981
)
0.47
" Substance P was shown to produce rapid, small contractions of trhe lung strip at doses from 10(-9) to 10(-5) M, and there was no apparent dose-response relationship."( The effect of substance P and related peptides on the guinea-pig lung strip.
Foreman, JC; Webber, SE, 1984
)
0.27
" The H1-antagonist chlorpheniramine shifted to the right the dose-response curves to histamine and to 2-aminoethylthiazole with the kinetics of the competitive antagonism."( Histamine receptors in the human ureter.
Bertaccini, G; Bezzi, E; Potenzoni, D; Zappia, L, 1983
)
0.59
" Three separate dosage regimens were employed."( Multi-center, double-blind, placebo-controlled trial of fluocortin butyl in perennial rhinitis.
Arbesman, C; Bernstein, IL; Bierman, CW; Bocles, JS; Katz, R; Lieberman, PL; Mattucci, K; Meltzer, EO; Middleton, E; Noyes, J; Pearlman, DS; Pence, HL; Slavin, RG; Spector, SL, 1983
)
0.27
" In 8 asthmatic subjects, dose-response curves were determined to isocapnic hyperventilation of cold air 30 min after inhalation of chlorpheniramine maleate (18 mg nebulized during tidal breathing), 2 doses of atropine sulphate (3 mg and 18 mg nebulized), or placebo."( The protective effect of inhaled chlorpheniramine and atropine on bronchoconstriction stimulated by airway cooling.
Daniel, EE; Hargreave, FE; Morris, M; O'Byrne, PM; Roberts, RS; Thomson, NC, 1983
)
0.75
" Cumulative log dose-response curves were constructed."( Methacholine dose-response curves in normal and asthmatic man: effect of starting conductance and pharmacological antagonism.
Chung, KF; Snashall, PD, 1984
)
0.27
"A high-performance liquid chromatographic (HPLC) method has been developed for the quantitation of acetaminophen, chlorpheniramine maleate, dextromethorphan hydrobromide, and phenylpropanolamine hydrochloride in combination in pharmaceutical dosage forms using a single column and three different mobile phases."( Quantitation of acetaminophen, chlorpheniramine maleate, dextromethorphan hydrobromide, and phenylpropanolamine hydrochloride in combination using high-performance liquid chromatography.
Das Gupta, V; Heble, AR, 1984
)
0.76
" The dosage forms evaluated were a conventional 4 mg tablet, and 8 mg barrier coated-bead capsule, and an 8 mg repeat action tablet."( Blood levels following multiple oral dosing of chlorpheniramine conventional and controlled release preparations.
Brown, WJ; Dighe, SV; Honigberg, IL; Kotzan, JA; Needham, TE; Stewart, JT; Vallner, JJ,
)
0.39
" The above results suggest the need to reexamine the current practice of frequent daily dosing and the use of sustained or controlled release dosage forms of this drug."( Pharmacokinetics of chlorpheniramine after intravenous and oral administration in normal adults.
Athanikar, NK; Chiou, WL; Huang, SM; Huang, YC; Sridhar, K, 1982
)
0.59
" The dosage forms evaluated were an 8-mg barrier coated-bead capsule, an 8-mg repeat action tablet, two 4-mg tablets, and 4- and 8-mg syrups."( Bioavailability of regular and controlled-release chlorpheniramine products.
Brown, WJ; Dighe, SV; Kotzan, JA; Malinowski, R; Needham, TE; Stewart, JT; Vallner, JJ; Viswanathan, CT, 1982
)
0.52
" We constructed cumulative log dose-response curves and determined the steepest slope and the provocative dose of histamine (PD35) needed to cause a 35% fall in specific airway conductance (SGaw)."( Histamine dose-response relationships in normal and asthmatic subjects. The importance of starting airway caliber.
Chung, KF; Keyes, SJ; Morgan, B; Snashall, PD, 1982
)
0.26
" Bronchial response was monitored with serial measurements of specific airways conductance (sGaw) and a dose-response curve was constructed for each challenge."( The role of histamine receptors in asthma.
Eiser, NM; Guz, A; Mills, J; Snashall, PD, 1981
)
0.26
"Proliferation of both mouse and human breast cancer cells was inhibited by chlorpheniramine (CPA) in a dose-response manner."( Chlorpheniramine inhibits the synthesis of ornithine decarboxylase and the proliferation of human breast cancer cell lines.
García de Veas, R; Lozano, J; Medina, MA; Morata, P; Sánchez-Jiménez, F, 1995
)
1.96
" Assessments were made prior to dosing and at one, three, and five hours after dosing; a 7-hour post-drug assessment was included in the second trial."( Characterization of daytime sleepiness and psychomotor performance following H1 receptor antagonists.
Canestrari, DA; Miller, RD; Riker, DK; Witek, TJ; Yang, JY, 1995
)
0.29
"05) and slower choice reaction times were noted one and three hours after dosing (P < ."( Characterization of daytime sleepiness and psychomotor performance following H1 receptor antagonists.
Canestrari, DA; Miller, RD; Riker, DK; Witek, TJ; Yang, JY, 1995
)
0.29
" The low permeability of a water-soluble drug, chlorpheniramine maleate, and the weak mechanical properties of Aquacoat films could suggest osmotic driven/rupturing effects as the release mechanisms from Aquacoat-coated dosage forms."( Mechanical properties of dry and wet cellulosic and acrylic films prepared from aqueous colloidal polymer dispersions used in the coating of solid dosage forms.
Bodmeier, R; Paeratakul, O, 1994
)
0.55
" Based on the pharmacokinetic results obtained frequent (ie, Q 4-6 h) CPA daily dosing may not be required particularly for the adults because of its long elimination half-life."( Bioequivalence and pharmacokinetics of chlorpheneramine in healthy human volunteers.
Al-Alsheikh, OA; Al-Dhawailie, AA; Najjar, TA; Shereif, A, 1995
)
0.29
" Ethylcellulose-coated beads were soaked in peanut oil prior to testing to simulate the influence of concomitant administration of the dosage form with ingestion of fatty meals."( An in vitro method to investigate food effects on drug release from film-coated beads.
Liu, J; Sriwongjanya, M; Williams, RO, 1997
)
0.3
"Dissolution profiles of various multiparticulate controlled-release dosage forms prepared by applying lipophilic materials using a hot-melt coating technique were analyzed to determine release kinetics."( Release kinetics of a controlled-release multiparticulate dosage form prepared using a hot-melt fluid bed coating method.
Griffin, EN; Niebergall, PJ, 1999
)
0.3
"5 hours after dosing were latency of the P300 event-related potential in which increased latency reflects a decreased rate of cognitive processing, visual analogue scale for subjective somnolence, and histamine skin tests for measurement of peripheral H1-blockade."( Central nervous system effects of H1-receptor antagonists in the elderly.
Fraser, TG; Maher, J; Pillay, N; Simons, FE; Simons, KJ, 1999
)
0.3
" The present work suggests that Rhinopront is an effective nasal decongestant in adults and children with acute congestive rhinitis and supports the adequacy of the proposed twice-daily dosing rate."( Exploratory study of the decongestive effect of Rhinopront syrup in adults and in children with acute rhinitis.
Calderon, P; Deroubaix, X; Gline, JP; Joue, P; Lebacq, E; Schwegler, F; Stockis, A; Van Schoor, O, 1994
)
0.29
"The principle of charge transfer complexation involving a pi-acceptor (chloranilic acid) and an n-donor (chlorpheniramine) was utilized in the assay of the later in its pure form and in its tablet dosage forms."( Spectrophotometric and some thermodynamic parameters of the charge transfer complexation between chloranilic acid and chlorpheniramine.
Ajali, U; Ofoefule, SI,
)
0.55
"A rapid, precise, and specific high-performance liquid chromatographic method is described for the simultaneous determination of paracetamol, phenylephrine HCI, and chlorpheniramine maleate in combined pharmaceutical dosage forms."( Simultaneous high-performance liquid chromatographic determination of paracetamol, phenylephrine HCl, and chlorpheniramine maleate in pharmaceutical dosage forms.
Ozden, T; Senyuva, H, 2002
)
0.72
" Before dosing and at 1, 3, 6, 9, and 24 hours after the first antihistamine dose as well as at 168, 192, and 216 hours after the first dose (ie, 12, 36, and 60 hours after the seventh and last consecutive daily H(1)-antihistamine dose), we measured fexofenadine, loratadine, or chlorpheniramine concentrations in plasma and in skin tissue samples obtained through use of punch biopsies, along with suppression of histamine-induced skin wheals and flares."( Clinical pharmacology of H1-antihistamines in the skin.
Gu, X; Silver, NA; Simons, FE; Simons, KJ, 2002
)
0.49
"A high-performance liquid chromatography procedure for the simultaneous determination of aminophylline, methoxyphenamine hydrochloride, noscapine and chlorphenamine maleate in commercially available compound capsule dosage forms has been developed and validated."( HPLC determination of aminophylline, methoxyphenamine hydrochloride, noscapine and chlorphenamine maleate in compound dosage forms with an aqueous-organic mobile phase.
Tang, C; Wu, X; Yin, C, 2003
)
0.32
" Changes in liver function tests were seen in 17 out of 56 patients treated for more than three months and were correlated with the dosage of the drug and the duration of treatment."( Clinical experience with chlorpro-pamide.
KINSELL, LW; WALKER, G, 1961
)
0.24
" The proposed method was applied to the determination of chlorpheniramine maleate alone in tablet and syrup dosage forms."( Determination of chlorpheniramine maleate and tincture ipecac in dosage form by liquid chromatography with ultraviolet detection.
El-Barbary, FA; Eldawy, MA; Mabrouk, MM,
)
0.72
" At present, the drug is marketed in tablet, capsule, syrup, cream, and injectable dosage forms."( In vitro and ex vivo permeation studies of chlorpheniramine maleate gels prepared by carbomer derivatives.
Baykara, T; Ozkan, Y; Savaşer, A; Taş, C, 2004
)
0.59
"We report a case of probable poisoning with codeine phosphate in a 3-month-old infant, which was associated with excessive dosing and concomitant use of antihistamines."( A case of probable codeine poisoning in a young infant after the use of a proprietary cough and cold medicine.
Chan, R; Lee, AC; So, KT, 2004
)
0.32
") produced a 12-fold shift in the histamine bronchoconstrictor dose-response curve."( Airway closure after antigen challenge in cynomolgus monkeys: effect of the histamine H1 receptor antagonist, chlorpheniramine maleate.
Celly, CS; Chapman, RW; Hey, JA; House, A; Lamca, JE; Skeans, S, 2005
)
0.54
" The results of the proposed method were in excellent agreement with those obtained from PLS and HPLC methods and can be satisfactorily used for routine analysis of multicomponent dosage forms."( Content uniformity and dissolution tests of triplicate mixtures by a double divisor-ratio spectra derivative method.
Koundourellis, JE; Malliou, ET; Markopoulou, CK, 2005
)
0.33
" This work reports the successful development of a derivative ultraviolet spectrophotometry for dexchlorpheniramine maleate (DPM) determination in solid dosage forms, in spite of the color imparted to tablets solution."( Derivative ultraviolet spectrophotometric determination of dexchlorpheniramine maleate in tablets in presence of coloring agents.
Moreira-Campos, LM; Viana, NS; Vianna-Soares, CD,
)
0.59
"Alginates are useful natural polymers suitable for use in the design of pharmaceutical dosage forms."( Evaluation of sodium alginate as drug release modifier in matrix tablets.
Chan, LW; Ching, AL; Heng, PW; Liew, CV, 2006
)
0.33
" Therefore, this study assessed the effects of repeated dosing of these antihistamines on driving and psychomotor performance."( Repeated-dose effects of mequitazine, cetirizine and dexchlorpheniramine on driving and psychomotor performance.
Ramaekers, JG; Theunissen, EL; Vermeeren, A, 2006
)
0.58
"The method was proved to be highly sensitive, selective, and suitable for pharmacokinetics investigations of different compound preparations containing low dosage of both ephedrine and chlorpheniramine."( [Simultaneous determination of ephedrine and chlorpheniramine in human plasma by a highly sensitive liquid chromatography-tandem mass spectrometric method].
Chen, XY; Duan, XT; Ren, S; Zhong, DF, 2006
)
0.78
"In the current study, the influence of plasticizer level on drug release was investigated for solid dosage forms prepared by hot-melt extrusion and film coating."( Influence of plasticizer level on the drug release from sustained release film coated and hot-melt extruded dosage forms.
McGinity, JW; Mehta, KA; Zhu, Y, 2006
)
0.33
"As there is strong interest in coating increasingly smaller particles or pellets for use in compacted dosage forms, there is a need for better small particle coating systems."( Use of swirling airflow to enhance coating performance of bottom spray fluid bed coaters.
Chan, LW; Heng, PW; Tang, ES, 2006
)
0.33
" Based on this knowledge, the effects of the films' composition and thickness on the resulting drug release kinetics (also from coated solid dosage forms) can be predicted in a quantitative way."( Drugs acting as plasticizers in polymeric systems: a quantitative treatment.
Le Brun, V; Siepmann, F; Siepmann, J, 2006
)
0.33
"46 times higher than the oral dosage form and the results showed statistically significant difference."( Transbuccal delivery of chlorpheniramine maleate from mucoadhesive buccal patches.
Gannu, R; Kishan, V; Naidu, KV; Rao, YM; Sekhar, KC; Vishnu, YV,
)
0.44
" The method was applied to nine commercial CP preparations in six dosage forms and CP enantiomers were well separated without any disturbance of other ingredients or impurities present."( Enantioselective determination of chlorpheniramine in various formulations by HPLC using carboxymethyl-beta-cyclodextrin as a chiral additive.
Chen, QC; Hwang, GS; Jeong, SJ; Kang, JS; Kim, KH, 2008
)
0.63
"A simple and reliable high-performance liquid chromatographic method was developed for the simultaneous determination of mixture of phenylephrine hydrochloride (PHENYL), guaifenesin (GUAIF), and chlorpheniramine maleate (CHLO) either in pure form or in the presence of methylparaben and propylparaben in a commercial cough syrup dosage form."( Simultaneous determination of phenylephrine hydrochloride, guaifenesin, and chlorpheniramine maleate in cough syrup by gradient liquid chromatography.
Abbas, SS; Ali, NM; Amer, SM; Shehata, MA,
)
0.55
" No significant change in latency for REM sleep or percentage REM sleep after dosing with fexofenadine was observed."( The effects of fexofenadine at steady-state on sleep architecture: a study using polysomnography in healthy Korean volunteers.
Ahn, JH; Kim, JE; Kim, MJ; Kim, SD; Lee, HW; Moon, SO; Park, DJ; Yoon, YR, 2008
)
0.35
" Particularly when this combined dosage is administered as outpatient chemotherapy, the doctor must prescribe diphenhydramine hydrochloride tablets, and the patient must not forget to bring them on the day in which chemotherapy is administered."( [Evaluation of short-time premedication with d-chlorpheniramine maleate injection for paclitaxel-induced hypersensitivity reaction].
Akase, T; Doi, M; Harada, T; Yamada, Y, 2008
)
0.6
" In study 2 the AMT dosage was increased up to 4-fold by doubling individual doses and switching to a twice daily schedule."( Anti-tumor effects of AMT in the renal cell carcinoma model.
Caballero, M; Diergarten, K; Drevs, J; Esser, N; Rentschler, J; Schächtele, C; Scheele, J; Soltau, J; Zirrgiebel, U, 2010
)
0.36
"In this study, a simple, specific and accurate reverse phase high performance liquid chromatographic method was developed for the simultaneous determination of nimesulide (NS), phenylephrine hydrochloride (PE), chlorpheniramine maleate (CPM) and caffeine anhydrous (CF) in pharmaceutical dosage forms."( Development and validation of RP-HPLC method for simultaneous estimation of nimesulide, phenylephrine hydrochloride, chlorpheniramine maleate and caffeine anhydrous in pharmaceutical dosage form.
Kumar, A; Nair, A; Saini, G; Sharma, R,
)
0.53
" Both dosage forms disintegrated immediately (less than 40 s) in simulated saliva solutions."( Evaluation of Chlorpheniramine Maleate microparticles in orally disintegrating film and orally disintegrating tablet for pediatrics.
Almoazen, H; Brunson, E; Hu, Z; Johnson, J; Liu, M; Lou, H; Qu, W, 2014
)
0.76
" The subsequent cycles were prescribed at reduced dosage without acute complications."( Reversible bilateral blepharoptosis following oxaliplatin infusion: a case report and literature review.
Buzzoni, R; Fanetti, G; Ferrari, LA; Pietrantonio, F,
)
0.13
"Simple, accurate, and selective methods have been developed and validated for simultaneous determination of a ternary mixture of Chlorpheniramine maleate (CPM), Pseudoephedrine HCl (PSE) and Ibuprofen (IBF), in tablet dosage form."( Evaluating the efficiency of spectral resolution of univariate methods manipulating ratio spectra and comparing to multivariate methods: an application to ternary mixture in common cold preparation.
Ali, O; Hegazy, M; Moustafa, AA; Salem, H, 2015
)
0.62
" Indeed, histamine elicited a sigmoid dose-response curve for IP3 production, shifted to the right by chlorpheniramine maleate, and elicited a double bell-shaped curve for cAMP production, partially suppressed by the selective H2R, H3R and H4R antagonists when each added alone, and completely ablated when combined together."( Histamine receptor expression in human renal tubules: a comparative pharmacological evaluation.
Camussi, G; Chazot, PL; Grange, C; Lanzi, C; Moggio, A; Pini, A; Rosa, AC; Veglia, E, 2015
)
0.63
" It is a major determinant of half-life and dosing frequency of a drug."( Volume of Distribution in Drug Design.
Beaumont, K; Di, L; Maurer, TS; Smith, DA, 2015
)
0.42
" Orodispersible films (ODF) have increasingly been evaluated as a suitable dosage form for extemporaneous oral preparations."( Application of miniaturized near-infrared spectroscopy for quality control of extemporaneous orodispersible films.
Chan, SY; Foo, WC; Gokhale, R; Khong, YM; Widjaja, E, 2018
)
0.48
" Naringenin, naringenin chalcone, and quercetin all showed strong antiallergic activity after intravenous dosing (0."( In Vivo Anti-inflammatory and Antiallergic Activity of Pure Naringenin, Naringenin Chalcone, and Quercetin in Mice.
Boix Montañés, A; Escribano-Ferrer, E; Garcia-Sala, X; Lamuela-Raventos, RM; Queralt Regué, J, 2019
)
0.51
" Solid oral dosage forms can be taste-masked quite simply by polymer coating, which prevents drug release in the mouth, without unwantedly impairing drug release further down the gastrointestinal tract."( In Vitro Dissolution Model Can Predict the in Vivo Taste Masking Performance of Coated Multiparticulates.
Ali, Z; Frost, J; Ghimire, M; Keeley, A; Orlu, M; Rajabi-Siahboomi, A; Teo, M; Tuleu, C, 2019
)
0.51
" After dissolution of the PVP interlayer, the capsule separates in two, with inner and outer capsules for continuous drug dosing and targeting."( Precision Printing of Customized Cylindrical Capsules with Multifunctional Layers for Oral Drug Delivery.
Chang, MW; Chen, X; Li, X; Mai, J; Wu, S; Zhang, C, 2019
)
0.51
" The dog was immediately treated with an intramuscular injection of a commercially available antihistamine treatment, Pen-Hista-Strep® containing a suspension of benzylpenicillin, chlorphenamine, dexamethasone, dihydrostreptomycin, and procaine at a dosage of 1 mL per 10 kg."( Aedes (Stegomyia) aegypti mosquito bite hypersensitivity in a dog: a case report.
Lekouch, N; Meyer, LN; Tahir, D; Varloud, M, 2020
)
0.56
"A combination of paracetamol, pseudoephedrine, chlorpheniramine, and sodium benzoate in (Cold-Flu) 1,2,3 Syrup dosage form is specified for the treatment of common cold and flu symptoms."( Stability-Indicating New RP-UPLC Method for Simultaneous Determination of a Quaternary Mixture of Paracetamol, Pseudoephedrine, Chlorpheniramine, and Sodium Benzoate in (Cold-Flu) Syrup Dosage Form.
Mohamed, MA, 2022
)
1.18
"The functional role of this study is to develop a novel, reliable, and selective stability-indicating reversed-phase ultra-performance liquid chromatography (RP-UPLC) method for simultaneous identification of a quaternary mixture of paracetamol, pseudoephedrine, chlorpheniramine, and sodium benzoate in (Cold-Flu) 1,2,3 Syrup dosage form."( Stability-Indicating New RP-UPLC Method for Simultaneous Determination of a Quaternary Mixture of Paracetamol, Pseudoephedrine, Chlorpheniramine, and Sodium Benzoate in (Cold-Flu) Syrup Dosage Form.
Mohamed, MA, 2022
)
1.11
"The proposed stability-indicating UPLC method for simultaneous determination of the three drugs, paracetamol, pseudoephedrine, and chlorpheniramine, with a preservative sodium benzoate in (Cold-Flu) 1,2,3 Syrup dosage form is successfully accomplished, developed, and validated, and can be easily used in the analysis of drugs in pure or dosage form."( Stability-Indicating New RP-UPLC Method for Simultaneous Determination of a Quaternary Mixture of Paracetamol, Pseudoephedrine, Chlorpheniramine, and Sodium Benzoate in (Cold-Flu) Syrup Dosage Form.
Mohamed, MA, 2022
)
1.13
"The novelty of the current research work lies in the development of the UPLC method for simultaneous determination of a quaternary mixture of paracetamol, pseudoephedrine, chlorpheniramine, and sodium benzoate in (Cold-Flu) 1,2,3 Syrup dosage form."( Stability-Indicating New RP-UPLC Method for Simultaneous Determination of a Quaternary Mixture of Paracetamol, Pseudoephedrine, Chlorpheniramine, and Sodium Benzoate in (Cold-Flu) Syrup Dosage Form.
Mohamed, MA, 2022
)
1.12
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (6)

RoleDescription
anti-allergic agentA drug used to treat allergic reactions.
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.
antipruritic drugA drug, usually applied topically, that relieves pruritus (itching).
histamine antagonistHistamine antagonists are the drugs that bind to but do not activate histamine receptors, thereby blocking the actions of histamine or histamine agonists.
serotonin uptake inhibitorA compound that specifically inhibits the reuptake of serotonin in the brain. This increases the serotonin concentration in the synaptic cleft which then activates serotonin receptors to a greater extent.
antidepressantAntidepressants are mood-stimulating drugs used primarily in the treatment of affective disorders and related conditions.
[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 (3)

ClassDescription
pyridinesAny organonitrogen heterocyclic compound based on a pyridine skeleton and its substituted derivatives.
tertiary amino compoundA compound formally derived from ammonia by replacing three hydrogen atoms by organyl groups.
monochlorobenzenesAny member of the class of chlorobenzenes containing a mono- or poly-substituted benzene ring in which only one substituent is chlorine.
[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
Chlorphenamine H1-Antihistamine Action87

Protein Targets (19)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
arylsulfatase AHomo sapiens (human)Potency0.01201.069113.955137.9330AID720538
atrial natriuretic peptide receptor 1 precursorHomo sapiens (human)Potency8.49210.134610.395030.1313AID1347049
atrial natriuretic peptide receptor 2 precursorHomo sapiens (human)Potency23.28090.00669.809418.4927AID1347050
flap endonuclease 1Homo sapiens (human)Potency8.43680.133725.412989.1251AID588795
Ataxin-2Homo sapiens (human)Potency25.11890.011912.222168.7989AID588378
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency8.49210.060110.745337.9330AID485368
[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)
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50 (µMol)133.00000.63154.45319.3000AID1473740
Multidrug resistance-associated protein 4Homo sapiens (human)IC50 (µMol)133.00000.20005.677410.0000AID1473741
Bile salt export pumpHomo sapiens (human)IC50 (µMol)134.00000.11007.190310.0000AID1443980; AID1473738
Histamine H1 receptorHomo sapiens (human)IC50 (µMol)0.06600.00000.44365.1768AID351895
Histamine H1 receptorHomo sapiens (human)Ki0.00410.00000.511010.0000AID1063784; AID591511
MBT domain-containing protein 1Homo sapiens (human)IC50 (µMol)34.00009.00009.00009.0000AID537070
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC50 (µMol)16.93440.00091.901410.0000AID161281; AID240820; AID243151; AID408340; AID576612
Solute carrier family 22 member 1Rattus norvegicus (Norway rat)IC50 (µMol)14.00000.18003.68578.8000AID681348
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50 (µMol)133.00002.41006.343310.0000AID1473739
Lethal(3)malignant brain tumor-like protein 3Homo sapiens (human)IC50 (µMol)42.00000.02401.40964.7000AID537068
Solute carrier family 22 member 2Rattus norvegicus (Norway rat)IC50 (µMol)26.00001.00004.446710.0000AID681345
Lethal(3)malignant brain tumor-like protein 1Homo sapiens (human)IC50 (µMol)41.00000.09804.29968.9000AID537067
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (98)

Processvia Protein(s)Taxonomy
xenobiotic metabolic processATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
bile acid and bile salt transportATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transportATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
leukotriene transportATP-binding cassette sub-family C member 3Homo sapiens (human)
monoatomic anion transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transport across blood-brain barrierATP-binding cassette sub-family C member 3Homo sapiens (human)
prostaglandin secretionMultidrug resistance-associated protein 4Homo sapiens (human)
cilium assemblyMultidrug resistance-associated protein 4Homo sapiens (human)
platelet degranulationMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic metabolic processMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
bile acid and bile salt transportMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transportMultidrug resistance-associated protein 4Homo sapiens (human)
urate transportMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
cAMP transportMultidrug resistance-associated protein 4Homo sapiens (human)
leukotriene transportMultidrug resistance-associated protein 4Homo sapiens (human)
monoatomic anion transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
export across plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
transport across blood-brain barrierMultidrug resistance-associated protein 4Homo sapiens (human)
guanine nucleotide transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
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)
inflammatory responseHistamine H1 receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayHistamine H1 receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayHistamine H1 receptorHomo sapiens (human)
memoryHistamine H1 receptorHomo sapiens (human)
visual learningHistamine H1 receptorHomo sapiens (human)
regulation of vascular permeabilityHistamine H1 receptorHomo sapiens (human)
positive regulation of vasoconstrictionHistamine H1 receptorHomo sapiens (human)
regulation of synaptic plasticityHistamine H1 receptorHomo sapiens (human)
cellular response to histamineHistamine H1 receptorHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayHistamine H1 receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerHistamine H1 receptorHomo sapiens (human)
chemical synaptic transmissionHistamine H1 receptorHomo sapiens (human)
double-strand break repair via homologous recombinationMBT domain-containing protein 1Homo sapiens (human)
chromatin organizationMBT domain-containing protein 1Homo sapiens (human)
regulation of apoptotic processMBT domain-containing protein 1Homo sapiens (human)
positive regulation of DNA-templated transcriptionMBT domain-containing protein 1Homo sapiens (human)
embryonic skeletal system developmentMBT domain-containing protein 1Homo sapiens (human)
regulation of cell cycleMBT domain-containing protein 1Homo sapiens (human)
positive regulation of double-strand break repair via homologous recombinationMBT domain-containing protein 1Homo sapiens (human)
regulation of double-strand break repairMBT domain-containing protein 1Homo sapiens (human)
negative regulation of DNA-templated transcriptionMBT domain-containing protein 1Homo 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)
chromatin organizationLethal(3)malignant brain tumor-like protein 4Homo sapiens (human)
negative regulation of DNA-templated transcriptionLethal(3)malignant brain tumor-like protein 4Homo sapiens (human)
xenobiotic metabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
negative regulation of gene expressionCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bile acid and bile salt transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
heme catabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic export from cellCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transepithelial transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
leukotriene transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
monoatomic anion transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
chromatin organizationLethal(3)malignant brain tumor-like protein 3Homo sapiens (human)
macrophage differentiationLethal(3)malignant brain tumor-like protein 3Homo sapiens (human)
granulocyte differentiationLethal(3)malignant brain tumor-like protein 3Homo sapiens (human)
erythrocyte maturationLethal(3)malignant brain tumor-like protein 3Homo sapiens (human)
negative regulation of DNA-templated transcriptionLethal(3)malignant brain tumor-like protein 3Homo sapiens (human)
regulation of DNA methylation-dependent heterochromatin formationLethal(3)malignant brain tumor-like protein 3Homo sapiens (human)
positive regulation of ubiquitin-dependent protein catabolic processLethal(3)malignant brain tumor-like protein 3Homo 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)
chromatin organizationLethal(3)malignant brain tumor-like protein 1Homo sapiens (human)
regulation of mitotic nuclear divisionLethal(3)malignant brain tumor-like protein 1Homo sapiens (human)
hemopoiesisLethal(3)malignant brain tumor-like protein 1Homo sapiens (human)
heterochromatin formationLethal(3)malignant brain tumor-like protein 1Homo sapiens (human)
regulation of megakaryocyte differentiationLethal(3)malignant brain tumor-like protein 1Homo sapiens (human)
negative regulation of DNA-templated transcriptionLethal(3)malignant brain tumor-like protein 1Homo sapiens (human)
regulation of cell cycleLethal(3)malignant brain tumor-like protein 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (49)

Processvia Protein(s)Taxonomy
ATP bindingATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type bile acid transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATP hydrolysis activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
icosanoid transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
guanine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ATP bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type xenobiotic transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
urate transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
purine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type bile acid transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
efflux transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
15-hydroxyprostaglandin dehydrogenase (NAD+) activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATP hydrolysis activityMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
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)
histamine receptor activityHistamine H1 receptorHomo sapiens (human)
G protein-coupled serotonin receptor activityHistamine H1 receptorHomo sapiens (human)
neurotransmitter receptor activityHistamine H1 receptorHomo sapiens (human)
protein bindingMBT domain-containing protein 1Homo sapiens (human)
zinc ion bindingMBT domain-containing protein 1Homo sapiens (human)
methylated histone bindingMBT domain-containing protein 1Homo sapiens (human)
NuA4 histone acetyltransferase complex bindingMBT domain-containing protein 1Homo sapiens (human)
chromatin bindingMBT domain-containing protein 1Homo 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)
protein bindingLethal(3)malignant brain tumor-like protein 4Homo sapiens (human)
zinc ion bindingLethal(3)malignant brain tumor-like protein 4Homo sapiens (human)
histone bindingLethal(3)malignant brain tumor-like protein 4Homo sapiens (human)
chromatin bindingLethal(3)malignant brain tumor-like protein 4Homo sapiens (human)
protein bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
organic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type xenobiotic transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP hydrolysis activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
chromatin bindingLethal(3)malignant brain tumor-like protein 3Homo sapiens (human)
protein bindingLethal(3)malignant brain tumor-like protein 3Homo sapiens (human)
zinc ion bindingLethal(3)malignant brain tumor-like protein 3Homo sapiens (human)
identical protein bindingLethal(3)malignant brain tumor-like protein 3Homo sapiens (human)
methylation-dependent protein bindingLethal(3)malignant brain tumor-like protein 3Homo sapiens (human)
histone bindingLethal(3)malignant brain tumor-like protein 3Homo 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)
chromatin bindingLethal(3)malignant brain tumor-like protein 1Homo sapiens (human)
protein bindingLethal(3)malignant brain tumor-like protein 1Homo sapiens (human)
zinc ion bindingLethal(3)malignant brain tumor-like protein 1Homo sapiens (human)
nucleosome bindingLethal(3)malignant brain tumor-like protein 1Homo sapiens (human)
SAM domain bindingLethal(3)malignant brain tumor-like protein 1Homo sapiens (human)
methylated histone bindingLethal(3)malignant brain tumor-like protein 1Homo sapiens (human)
histone bindingLethal(3)malignant brain tumor-like protein 1Homo sapiens (human)
identical protein bindingLethal(3)malignant brain tumor-like protein 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (35)

Processvia Protein(s)Taxonomy
plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basal plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basolateral plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
nucleolusMultidrug resistance-associated protein 4Homo sapiens (human)
Golgi apparatusMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
platelet dense granule membraneMultidrug resistance-associated protein 4Homo sapiens (human)
external side of apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
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)
cytosolHistamine H1 receptorHomo sapiens (human)
plasma membraneHistamine H1 receptorHomo sapiens (human)
synapseHistamine H1 receptorHomo sapiens (human)
dendriteHistamine H1 receptorHomo sapiens (human)
plasma membraneHistamine H1 receptorHomo sapiens (human)
site of double-strand breakMBT domain-containing protein 1Homo sapiens (human)
nucleosomeMBT domain-containing protein 1Homo sapiens (human)
NuA4 histone acetyltransferase complexMBT domain-containing protein 1Homo sapiens (human)
nucleusMBT domain-containing protein 1Homo sapiens (human)
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)
nucleusLethal(3)malignant brain tumor-like protein 4Homo sapiens (human)
plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
cell surfaceCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
intercellular canaliculusCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
nucleusLethal(3)malignant brain tumor-like protein 3Homo sapiens (human)
nucleoplasmLethal(3)malignant brain tumor-like protein 3Homo sapiens (human)
nucleolusLethal(3)malignant brain tumor-like protein 3Homo 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)
nucleolusLethal(3)malignant brain tumor-like protein 1Homo sapiens (human)
condensed chromosomeLethal(3)malignant brain tumor-like protein 1Homo sapiens (human)
nucleusLethal(3)malignant brain tumor-like protein 1Homo sapiens (human)
nucleoplasmLethal(3)malignant brain tumor-like protein 1Homo sapiens (human)
chromatin lock complexLethal(3)malignant brain tumor-like protein 1Homo sapiens (human)
chromatinLethal(3)malignant brain tumor-like protein 1Homo sapiens (human)
nucleusLethal(3)malignant brain tumor-like protein 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (177)

Assay IDTitleYearJournalArticle
AID351895Displacement of [3H]pyrilamine from human histamine receptor subtype 1 expressed in CHO cells2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Design, synthesis, and evaluation of 10-N-substituted acridones as novel chemosensitizers in Plasmodium falciparum.
AID1636475Drug activation in human Hep3B cells assessed as human CYP2D6-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 8.9 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.
AID351891Cytotoxicity against C57BL/6J mouse splenocytes after 72 hrs by alamar blue assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Design, synthesis, and evaluation of 10-N-substituted acridones as novel chemosensitizers in Plasmodium falciparum.
AID173540Percentage decrease in antiallergic activity against cutaneous reaction to histamine in rat, by oral administration at a dose of 10 mg/kg1985Journal of medicinal chemistry, May, Volume: 28, Issue:5
New antihistaminic theophylline or theobromine derivatives.
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).
AID29337Ionisation constant (pKa)2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID1443980Inhibition of human BSEP expressed in fall armyworm sf9 cell plasma membrane vesicles assessed as reduction in vesicle-associated [3H]-taurocholate transport preincubated for 10 mins prior to ATP addition measured after 15 mins in presence of [3H]-tauroch2010Toxicological sciences : an official journal of the Society of Toxicology, Dec, Volume: 118, Issue:2
Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development.
AID26516Partition coefficient (logD) (HPLC)1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID537069Inhibition of L3MBTL4 by alpha-screening2010Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21
Identification of non-peptide malignant brain tumor (MBT) repeat antagonists by virtual screening of commercially available compounds.
AID74209Compound is evaluated for the inhibition of H1-receptor antagonists of histamine-induced skin wheal formation in the guinea pig with a pretreatment interval prior to histamine challenge at 18 h1995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
New antihistamines: substituted piperazine and piperidine derivatives as novel H1-antagonists.
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).
AID444052Hepatic clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1155077Inhibition of CTR in Plasmodium falciparum C67G8 expressing chloroquine-resistance-conferring pfcrt alleles assessed as increase of accumulation of [3H]-chloroquine level at 1 uM after 1 hr relative to control2014ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
Chlorpheniramine Analogues Reverse Chloroquine Resistance in Plasmodium falciparum by Inhibiting PfCRT.
AID351893Antimalarial activity after 72 hrs against chloroquine-sensitive Plasmodium falciparum D6 infected human erythrocytes by SYBR green assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Design, synthesis, and evaluation of 10-N-substituted acridones as novel chemosensitizers in Plasmodium falciparum.
AID28235Unbound fraction (plasma)2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID234883Potency relative to 7-[3-(4-Benzhydryl-piperidine-1-yl)-propyl]-1,3-dimethyl-3,7-dihydro-purine-2,6-dione1995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
New antihistamines: substituted piperazine and piperidine derivatives as novel H1-antagonists.
AID609562Inhibition of histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced muscle spasms at 2 x 10 '-3 mg/ml after 5 mins (Rvb = 0.31 %)2011Bioorganic & medicinal chemistry letters, Aug-01, Volume: 21, Issue:15
Synthesis and antihistamine evaluations of novel loratadine analogues.
AID1155070Antiplasmodial activity against Plasmodium falciparum C4Dd2 expressing chloroquine-resistance-conferring pfcrt alleles assessed as parasite growth at 800 nM after 72 hrs by SYBR Green I-based fluorescence assay relative to control2014ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
Chlorpheniramine Analogues Reverse Chloroquine Resistance in Plasmodium falciparum by Inhibiting PfCRT.
AID1155074Response modification index, ratio of IC50 for Plasmodium falciparum C67G8 expressing chloroquine-resistance-conferring pfcrt alleles in presence of drug to IC50 for Plasmodium falciparum C67G8 expressing chloroquine-resistance-conferring pfcrt alleles in2014ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
Chlorpheniramine Analogues Reverse Chloroquine Resistance in Plasmodium falciparum by Inhibiting PfCRT.
AID540209Volume of distribution at steady state in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
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.
AID1611423In vivo antiallergic activity in guinea pig assessed as protection against histamine-induced bronchospasm at 25 mg/kg by Van Arman method relative to control2019Bioorganic & medicinal chemistry, 12-15, Volume: 27, Issue:24
Design, synthesis and biological activity of a novel ethylenediamine derivatives as H
AID26362Ionization constant (pKa)2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics.
AID1611421In vivo antiallergic activity in histamine-induced bronchospasm guinea pig model assessed as duration of convulsions at 25 mg/kg by Van Arman method2019Bioorganic & medicinal chemistry, 12-15, Volume: 27, Issue:24
Design, synthesis and biological activity of a novel ethylenediamine derivatives as H
AID29359Ionization constant (pKa)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
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.
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.
AID26295Partition coefficient (logD) (HPLC)1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID467611Dissociation constant, pKa of the compound2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Prediction of volume of distribution values in human using immobilized artificial membrane partitioning coefficients, the fraction of compound ionized and plasma protein binding data.
AID27167Delta logD (logD6.5 - logD7.4)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID681345TP_TRANSPORTER: inhibition of TEA uptake (TEA: 50 uM) in OCT2-expressing MDCK cells2001Pharmaceutical research, Nov, Volume: 18, Issue:11
Distinct characteristics of organic cation transporters, OCT1 and OCT2, in the basolateral membrane of renal tubules.
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.
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.
AID26296Partition coefficient (logD7.4)1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
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.
AID8002Observed volume of distribution2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics.
AID29813Oral bioavailability in human2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID26522Partition coefficient (logD) (HPLC)1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID540211Fraction unbound in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID177710In vivo protection from compound 48/80 induced lethality test in rats 1 hour after subcutaneous administration.1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
New antihistaminic N-heterocyclic 4-piperidinamines. 1. Synthesis and antihistaminic activity of N-(4-piperidinyl)-1H-benzimidazol-2-amines.
AID17268Dissociation constant (KD) of the compound1995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
New antihistamines: substituted piperazine and piperidine derivatives as novel H1-antagonists.
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).
AID444053Renal clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID444057Fraction escaping hepatic elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID28681Partition coefficient (logD6.5)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID1232308Distribution coefficient, log D of the compound2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Volume of Distribution in Drug Design.
AID89260Concentration required to cause 50% inhibition of platelet activating factor (PAF)-induced platelet aggregation of human platelet rich plasma when challenged with 25 nM PAF.1991Journal of medicinal chemistry, Jan, Volume: 34, Issue:1
Dual antagonists of platelet activating factor and histamine. Identification of structural requirements for dual activity of N-Acyl-4-(5,6-dihydro-11H-benzo [5,6]cyclohepta-[1,2-b]pyridin-11-ylidene)piperidines.
AID1636357Drug activation in human Hep3B cells assessed as human CYP3A4-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.
AID28236Unbound fraction (tissues)2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID87519Binding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranes1998Bioorganic & medicinal chemistry letters, Dec-15, Volume: 8, Issue:24
Dual antagonists of platelet activating factor and histamine. 3. Synthesis, biological activity and conformational implications of substituted N-acyl-bis-arylcycloheptapiperazines.
AID1063784Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)2014Bioorganic & medicinal chemistry letters, Jan-15, Volume: 24, Issue:2
The synthesis and comparative receptor binding affinities of novel, isomeric pyridoindolobenzazepine scaffolds.
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).
AID7783Unbound fraction (plasma)2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics.
AID425653Renal clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID1473738Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1611424Acute toxicity in ip dosed histamine-induced bronchospasm guinea pig model2019Bioorganic & medicinal chemistry, 12-15, Volume: 27, Issue:24
Design, synthesis and biological activity of a novel ethylenediamine derivatives as H
AID1155069Antiplasmodial activity against Plasmodium falciparum C2GC03 expressing wild-type pfcrt allele assessed as parasite growth at 800 nM after 72 hrs by SYBR Green I-based fluorescence assay relative to control2014ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
Chlorpheniramine Analogues Reverse Chloroquine Resistance in Plasmodium falciparum by Inhibiting PfCRT.
AID1537240Antiallergic activity in CD-1 mouse model of IgE/DNP-BSA-stimulated passive cutaneous anaphylaxis assessed as inhibition of vascular permeability at 1% administered topically immediately after sensitization by Evans blue extravasation assay relative to co2019Journal of natural products, 02-22, Volume: 82, Issue:2
In Vivo Anti-inflammatory and Antiallergic Activity of Pure Naringenin, Naringenin Chalcone, and Quercetin in Mice.
AID92393In vitro antagonist activity, determined by 50% inhibition of PAF-induced platelet aggregation of human platelet rich plasma when challenged with PAF1998Bioorganic & medicinal chemistry letters, Dec-15, Volume: 8, Issue:24
Dual antagonists of platelet activating factor and histamine. 3. Synthesis, biological activity and conformational implications of substituted N-acyl-bis-arylcycloheptapiperazines.
AID1232306Dissociation constant of the compound2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Volume of Distribution in Drug Design.
AID1473739Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
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).
AID1611418Antiallergic activity in IgE/Ag-stimulated rat RBL2H3 cells assessed as inhibition of HSA-induced beta-hexosaminidase release preincubated with compound for 30 mins and then stimulated with HSA for 15 mins followed by incubation with P-nitrophenyl-N-acety2019Bioorganic & medicinal chemistry, 12-15, Volume: 27, Issue:24
Design, synthesis and biological activity of a novel ethylenediamine derivatives as H
AID177713In vivo anti-histaminic protection from 48/80 induced lethality in rats 2 hours after oral administration1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
New antihistaminic N-heterocyclic 4-piperidinamines. 1. Synthesis and antihistaminic activity of N-(4-piperidinyl)-1H-benzimidazol-2-amines.
AID444058Volume of distribution at steady state in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID408340Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique2008Bioorganic & medicinal chemistry, Jun-01, Volume: 16, Issue:11
Support vector machines classification of hERG liabilities based on atom types.
AID1611425Antiallergic activity in mouse assessed as inhibition of histamine-induced increase in capillary permeability by measuring Evans blue dye concentration at 20 mg/kg administered via gavage for 1 week followed by Evans blue dye injection immediately after s2019Bioorganic & medicinal chemistry, 12-15, Volume: 27, Issue:24
Design, synthesis and biological activity of a novel ethylenediamine derivatives as H
AID624623Apparent permeability (Papp) from basolateral to apical side determined in MDR1-MDCKII cells2001The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2
Rational use of in vitro P-glycoprotein assays in drug discovery.
AID395325Lipophilicity, log P by microemulsion electrokinetic chromatography2009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs.
AID624608Specific activity of expressed human recombinant UGT1A42000Annual review of pharmacology and toxicology, , Volume: 40Human UDP-glucuronosyltransferases: metabolism, expression, and disease.
AID425652Total body clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID29925Volume of distribution in man (IV dose)2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID1155072Response modification index, ratio of IC50 for Plasmodium falciparum C2GC03 expressing wild-type pfcrt allele in presence of drug to IC50 for Plasmodium falciparum C2GC03 expressing wild-type pfcrt allele in absence of 800 nM of drug2014ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
Chlorpheniramine Analogues Reverse Chloroquine Resistance in Plasmodium falciparum by Inhibiting PfCRT.
AID609561Antiasthmatic activity in guinea pig assessed as inhibition of histamine phosphate solution-induced asthmatic reaction measured as increase in asthmogenic latency period at 0.2 mg/kg administered as intragastric (Rvb = 95.50 +/- 18.98 sec)2011Bioorganic & medicinal chemistry letters, Aug-01, Volume: 21, Issue:15
Synthesis and antihistamine evaluations of novel loratadine analogues.
AID1155066Inhibition of chloroquine-resistant Plasmodium falciparum Dd2 CRT expressed in Xenopus laevis oocytes plasma membrane assessed as reduction of [3H]-chloroquine transportation at 100 uM after 1 to 2 hrs2014ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
Chlorpheniramine Analogues Reverse Chloroquine Resistance in Plasmodium falciparum by Inhibiting PfCRT.
AID1232311Unbound volume of distribution at steady state in human2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Volume of Distribution in Drug Design.
AID1611416Antiallergic activity in rat RBL2H3 cells assessed as inhibition of C48/80-induced mast cell degranulation preincubated with compound for 30 mins and then treated with C48/80 for 1 hr by neutral red dye based method2019Bioorganic & medicinal chemistry, 12-15, Volume: 27, Issue:24
Design, synthesis and biological activity of a novel ethylenediamine derivatives as H
AID87521Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand1991Journal of medicinal chemistry, Jan, Volume: 34, Issue:1
Dual antagonists of platelet activating factor and histamine. Identification of structural requirements for dual activity of N-Acyl-4-(5,6-dihydro-11H-benzo [5,6]cyclohepta-[1,2-b]pyridin-11-ylidene)piperidines.
AID29423HPLC capacity factor (k')2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
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).
AID23961logD (measured by HPLC) (as log k')1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID624628Drug-stimulated Pgp ATPase activity ratio determined in MDR1-Sf9 cell membranes with test compound at a concentration of 20uM2001The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2
Rational use of in vitro P-glycoprotein assays in drug discovery.
AID1155075Inhibition of CTR in Plasmodium falciparum C2GC03 expressing wild-type pfcrt allele assessed as increase of accumulation of [3H]-chloroquine level at 1 uM after 1 hr2014ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
Chlorpheniramine Analogues Reverse Chloroquine Resistance in Plasmodium falciparum by Inhibiting PfCRT.
AID624622Apparent permeability (Papp) from apical to basolateral side determined in MDR1-MDCKII cells2001The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2
Rational use of in vitro P-glycoprotein assays in drug discovery.
AID481439Absolute bioavailability in human2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
How well can the Caco-2/Madin-Darby canine kidney models predict effective human jejunal permeability?
AID1769487Aqueous solubility of the compound
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.
AID26294Partition coefficient (logD) (HPLC)1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID1232307Lipophilicity, log P of the compound2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Volume of Distribution in Drug Design.
AID588213Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID444050Fraction unbound in human plasma2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
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).
AID351890Antimalarial activity after 72 hrs against chloroquine-resistant Plasmodium falciparum Dd2 infected human erythrocytes by SYBR green assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Design, synthesis, and evaluation of 10-N-substituted acridones as novel chemosensitizers in Plasmodium falciparum.
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.
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.
AID481442Transcellular permeability at pH 6.5 calculated from in vitro P app values in Caco-2 and/or MDCK cells2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
How well can the Caco-2/Madin-Darby canine kidney models predict effective human jejunal permeability?
AID540210Clearance in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID161281Inhibition of human Potassium channel HERG expressed in mammalian cells2003Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16
Prediction of hERG potassium channel affinity by traditional and hologram qSAR methods.
AID1473741Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
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).
AID240820Inhibitory concentration against IKr potassium channel2004Bioorganic & medicinal chemistry letters, Sep-20, Volume: 14, Issue:18
The pharmacophore hypotheses of I(Kr) potassium channel blockers: novel class III antiarrhythmic agents.
AID609560Antiasthmatic activity in guinea pig assessed as inhibition of histamine phosphate solution-induced asthmatic reaction measured as increase in asthmogenic latency period at 0.5 mg/kg administered as intragastric (Rvb = 99.30 +/- 30.06 sec)2011Bioorganic & medicinal chemistry letters, Aug-01, Volume: 21, Issue:15
Synthesis and antihistamine evaluations of novel loratadine analogues.
AID74208Compound is evaluated for the inhibition of H1-receptor antagonists of histamine-induced skin wheal formation in the guinea pig with a pretreatment interval prior to histamine challenge at 1 h1995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
New antihistamines: substituted piperazine and piperidine derivatives as novel H1-antagonists.
AID87525Ability to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranes2003Bioorganic & medicinal chemistry letters, Jun-16, Volume: 13, Issue:12
Identification of a dual histamine H1/H3 receptor ligand based on the H1 antagonist chlorpheniramine.
AID1473740Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID624629Inhibition of Pgp expressed in MDR1-MDCKII cells measured by calcein-AM assay2001The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2
Rational use of in vitro P-glycoprotein assays in drug discovery.
AID624609Specific activity of expressed human recombinant UGT1A62000Annual review of pharmacology and toxicology, , Volume: 40Human UDP-glucuronosyltransferases: metabolism, expression, and disease.
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).
AID351897Chemosensitizing activity after 72 hrs against chloroquine-resistant Plasmodium falciparum Dd2 infected human erythrocytes as IC50 ratio chloroquine +/- 500 nM by SYBR green assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Design, synthesis, and evaluation of 10-N-substituted acridones as novel chemosensitizers in Plasmodium falciparum.
AID537067Inhibition of L3MBTL1 by alpha-screening2010Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21
Identification of non-peptide malignant brain tumor (MBT) repeat antagonists by virtual screening of commercially available compounds.
AID624626Ratio of apparent permeability from basolateral to apical side over apical to basolateral side determined in MDR1-MDCKII cells2001The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2
Rational use of in vitro P-glycoprotein assays in drug discovery.
AID540212Mean residence time in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID28233Fraction ionized (pH 7.4)2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID467612Fraction unbound in human plasma2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Prediction of volume of distribution values in human using immobilized artificial membrane partitioning coefficients, the fraction of compound ionized and plasma protein binding data.
AID361986Lipophilicity, log D of compound at pH 7.4 by shake flask method2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
Determination of log D via automated microfluidic liquid-liquid extraction.
AID1155076Inhibition of CTR in Plasmodium falciparum C4Dd2 expressing chloroquine-resistance-conferring pfcrt alleles assessed as increase of accumulation of [3H]-chloroquine level at 1 uM after 1 hr relative to control2014ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
Chlorpheniramine Analogues Reverse Chloroquine Resistance in Plasmodium falciparum by Inhibiting PfCRT.
AID591511Binding affinity to histamine H1 receptor2011Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis.
AID781328pKa (acid-base dissociation constant) as determined by Luan ref: Pharm. Res. 20052014Pharmaceutical research, Apr, Volume: 31, Issue:4
Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds.
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).
AID395328Lipophilicity, log P of the compound2009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs.
AID23971logD (measured by HPLC) (as log k')1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
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).
AID1155068Inhibition of chloroquine-resistant Plasmodium falciparum Dd2 CRT expressed in Xenopus laevis oocytes plasma membrane assessed as reduction of [3H]-chloroquine transportation after 1 to 2 hrs2014ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
Chlorpheniramine Analogues Reverse Chloroquine Resistance in Plasmodium falciparum by Inhibiting PfCRT.
AID515780Intrinsic solubility of the compound in water2010Bioorganic & medicinal chemistry, Oct-01, Volume: 18, Issue:19
QSAR-based solubility model for drug-like compounds.
AID624612Specific activity of expressed human recombinant UGT1A92000Annual review of pharmacology and toxicology, , Volume: 40Human UDP-glucuronosyltransferases: metabolism, expression, and disease.
AID537068Inhibition of L3MBTL3 by alpha-screening2010Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21
Identification of non-peptide malignant brain tumor (MBT) repeat antagonists by virtual screening of commercially available compounds.
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).
AID1155071Antiplasmodial activity against Plasmodium falciparum C67G8 expressing chloroquine-resistance-conferring pfcrt alleles assessed as parasite growth at 800 nM after 72 hrs by SYBR Green I-based fluorescence assay relative to control2014ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
Chlorpheniramine Analogues Reverse Chloroquine Resistance in Plasmodium falciparum by Inhibiting PfCRT.
AID311367Permeability coefficient in human skin2007Bioorganic & medicinal chemistry, Nov-15, Volume: 15, Issue:22
Transdermal penetration behaviour of drugs: CART-clustering, QSPR and selection of model compounds.
AID444051Total clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID361985Lipophilicity, log D of compound at pH 7.4 by microfluidic liquid-liquid extraction method2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
Determination of log D via automated microfluidic liquid-liquid extraction.
AID243151Inhibitory concentration against potassium channel HERG2005Bioorganic & medicinal chemistry letters, Jun-02, Volume: 15, Issue:11
A discriminant model constructed by the support vector machine method for HERG potassium channel inhibitors.
AID1155073Response modification index, ratio of IC50 for Plasmodium falciparum C4Dd2 expressing chloroquine-resistance-conferring pfcrt alleles in presence of drug to IC50 for Plasmodium falciparum C4Dd2 expressing chloroquine-resistance-conferring pfcrt alleles in2014ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
Chlorpheniramine Analogues Reverse Chloroquine Resistance in Plasmodium falciparum by Inhibiting PfCRT.
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).
AID237685Lipophilicity determined as logarithm of the partition coefficient in the alkane/water system2005Journal of medicinal chemistry, May-05, Volume: 48, Issue:9
Calculating virtual log P in the alkane/water system (log P(N)(alk)) and its derived parameters deltalog P(N)(oct-alk) and log D(pH)(alk).
AID351896Chemosensitizing activity after 72 hrs against chloroquine-sensitive Plasmodium falciparum D6 infected human erythrocytes as IC50 ratio chloroquine +/- 500nM by SYBR green assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Design, synthesis, and evaluation of 10-N-substituted acridones as novel chemosensitizers in Plasmodium falciparum.
AID1232310Volume of distribution at steady state in human2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Volume of Distribution in Drug Design.
AID23965logD (measured by HPLC) (as log k')1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
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.
AID540213Half life in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID681348TP_TRANSPORTER: inhibition of TEA uptake (TEA: 50 uM) in OCT1-expressing MDCK cells2001Pharmaceutical research, Nov, Volume: 18, Issue:11
Distinct characteristics of organic cation transporters, OCT1 and OCT2, in the basolateral membrane of renal tubules.
AID75529Percentage decrease in bronchodilator activity against serotonin-induced bronchospasm reaction in guinea pig by intraveneous administration at dose 250 ug/kg1985Journal of medicinal chemistry, May, Volume: 28, Issue:5
New antihistaminic theophylline or theobromine derivatives.
AID537066Activity at L3MBTL1 at 100 uM2010Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21
Identification of non-peptide malignant brain tumor (MBT) repeat antagonists by virtual screening of commercially available compounds.
AID77385Protection against histamine-induced lethality in guinea pig at 1 hr pretreatment time upon peroral administration.1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
Optical isomers of rocastine and close analogues: synthesis and H1 antihistaminic activity of its enantiomers and their structural relationship to the classical antihistamines.
AID444056Fraction escaping gut-wall elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID444054Oral bioavailability in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID24863pA2 value is determined compared to standard H1-antagonists1995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
New antihistamines: substituted piperazine and piperidine derivatives as novel H1-antagonists.
AID1232309Unbound fraction in human plasma2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Volume of Distribution in Drug Design.
AID1611417Antiallergic activity in rat RBL2H3 cells assessed as inhibition of C48/80-induced histamine release preincubated with compound for 30 mins followed by C48/80 stimulation for 1 hr2019Bioorganic & medicinal chemistry, 12-15, Volume: 27, Issue:24
Design, synthesis and biological activity of a novel ethylenediamine derivatives as H
AID467613Volume of distribution at steady state in human2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Prediction of volume of distribution values in human using immobilized artificial membrane partitioning coefficients, the fraction of compound ionized and plasma protein binding data.
AID537070Inhibition of MBTD1 by alpha-screening2010Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21
Identification of non-peptide malignant brain tumor (MBT) repeat antagonists by virtual screening of commercially available compounds.
AID588212Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID86586Inhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortex1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
Optical isomers of rocastine and close analogues: synthesis and H1 antihistaminic activity of its enantiomers and their structural relationship to the classical antihistamines.
AID75528Percent decrease in bronchodilator activity against histamine-induced bronchospasm reaction in guinea pig by intraveneous administration at dose 250 ug/kg1985Journal of medicinal chemistry, May, Volume: 28, Issue:5
New antihistaminic theophylline or theobromine derivatives.
AID19424Partition coefficient (logD7.4)2001Journal of medicinal chemistry, Jul-19, Volume: 44, Issue:15
ElogD(oct): a tool for lipophilicity determination in drug discovery. 2. Basic and neutral compounds.
AID23963logD (measured by HPLC) (as log k')1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID1769488Binding affinity to salmon DNA assessed as DNA intercalation measured after 30 mins by UV based spectroscopic method
AID588211Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID444055Fraction absorbed in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID23970logD (measured by HPLC) (as log k')1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID173539Percent decrease in antiallergic activity by antigen/antibody reaction assay in rat by oral administration at a dose of 10 mg/kg1985Journal of medicinal chemistry, May, Volume: 28, Issue:5
New antihistaminic theophylline or theobromine derivatives.
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).
AID23968logD (measured by HPLC) (as log k')1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID1346037Human H1 receptor (Histamine receptors)2011Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (1,884)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990906 (48.09)18.7374
1990's338 (17.94)18.2507
2000's360 (19.11)29.6817
2010's229 (12.15)24.3611
2020's51 (2.71)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 113.75

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 Index113.75 (24.57)
Research Supply Index7.75 (2.92)
Research Growth Index4.33 (4.65)
Search Engine Demand Index227.19 (26.88)
Search Engine Supply Index2.13 (0.95)

This Compound (113.75)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials287 (14.07%)5.53%
Reviews39 (1.91%)6.00%
Case Studies204 (10.00%)4.05%
Observational0 (0.00%)0.25%
Other1,510 (74.02%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (25)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Anti-histamines Promote Electroacupuncture Analgesia: Basic and Clinical Research [NCT03805035]40 participants (Actual)Interventional2019-01-24Completed
A Prospective, Randomized, Double-blind Controlled Trial of Chlorpheniramine Pretransfusion Medication for Allergic Transfusion Reactions [NCT04688736]Phase 26,642 participants (Anticipated)Interventional2021-01-01Recruiting
A Multicentric, Randomized, Double-Blind, Comparative, Prospective, Placebo-controlled, Phase-II/III Clinical Trial (ACCROS-I) [NCT05449405]Phase 2/Phase 3101 participants (Actual)Interventional2021-12-07Completed
Comparison Between Dexchlorpheniramine and Dexchlorpheniramine/Pseudoephedrine/Guaifenesin in the Relief of Allergic Symptoms in Rhinitic Patients With Viral Upper Respiratory Tract Infections and Productive Cough [NCT01085721]Phase 3170 participants (Anticipated)InterventionalNot yet recruiting
A Phase 2, Double-Blind, Parallel-Group, Dose-Ranging Study Evaluating Safety/ Efficacy Atropine Doses With Pseudoephedrine and Chlorpheniramine in SAR Patients 12 Years of Age and Older [NCT02082054]Phase 2125 participants (Anticipated)Interventional2014-03-31Active, not recruiting
[NCT01233934]Phase 390 participants (Anticipated)Interventional2011-02-28Not yet recruiting
Mechanisms of N-acetylcysteine Mediated Vascular Adverse Effects [NCT01209455]24 participants (Anticipated)Interventional2011-01-31Recruiting
Effect of an Adjunctive Sedative for the Patients With Histories of Paradoxical Reaction to Midazolam During Sedative Endoscopy [NCT03940391]220 participants (Anticipated)Interventional2019-05-01Enrolling by invitation
Non-inferiority, Monocentric Comparative Open Study of Two Topical Pharmaceutical Preparations (Cream and Gel) of Dexchlorpheniramine Maleate in the Evaluation of Safety and Efficacy for the Relief of Mild to Moderate Sunburn Related Symptoms [NCT01237925]Phase 3124 participants (Anticipated)InterventionalNot yet recruiting
Phase II Multicenter, Double-blinded Clinical Trial of SP160412 in the Temporary Relief of Mild to Moderate (i.e,First Degree) Sunburn [NCT03332524]Phase 280 participants (Actual)Interventional2018-01-15Terminated(stopped due to Sponsor decided to stop for lack of efficacy)
Accelerating COVID-19 Clinical Recovery in the Outpatient Setting: Retrospective Data Collection and Analysis of COVID-19 Patients Treated With ClorNovir® (Chlorpheniramine Maleate (0.4% Nasal Spray) [NCT05520944]1,000 participants (Anticipated)Observational2021-08-26Active, not recruiting
Phase III Clinical Trial - Efficacy and Safety Assessment of a Compound Acetaminophen, Chlorpheniramine and Phenylephrine Combination in the Symptomatic Treatment of Common Cold and Flu-Like Syndrome in Adults [NCT00940836]Phase 3146 participants (Anticipated)Interventional2009-06-30Recruiting
Non-inferiority, Monocentric Comparative Open Study of Two Topical Pharmaceutical Preparations (Cream and Lotion) of Dexchlorpheniramine Maleate in the Evaluation of Safety and Efficacy for the Relief of Sunburn Related Symptoms [NCT01085851]Phase 330 participants (Anticipated)InterventionalNot yet recruiting
An Open-Label, Randomized, Two-Period, Crossover Study to Evaluate the Bioequivalence of an Extended Release Test Capsule Formulation of Chlorpheniramine Polistirex and Hydrocodone Polistirex Compared to an Equivalent Dose of a Commercially Available Refe [NCT00853294]Phase 142 participants (Actual)Interventional2003-09-30Completed
A Single-Dose, Open-Label, Pharmacokinetic Study of Chlorpheniramine Maleate Liquid in Children and Adolescents [NCT00837837]Phase 136 participants (Actual)Interventional2008-12-21Completed
A Single-blind, Randomized, Placebo Controlled, Crossover Pilot Study to Evaluate the Onset of Action of an Antihistamine in Subjects Following Allergen Exposure in an Allergen Chamber [NCT02722083]Phase 21 participants (Actual)Interventional2016-05-07Terminated
Dose-Ranging Study of Mometasone Furoate Nasal Spray (SCH 32088) in the Treatment of Children (Ages 6-11) With Seasonal Allergic Rhinitis (Protocol C95-161) [NCT03879772]Phase 3679 participants (Actual)Interventional1996-03-12Completed
An Open-Label, Randomized, Two-Period, Crossover Study to Evaluate the Bioequivalence of an Extended Release Test Capsule Formulation of Chlorpheniramine Polistirex and Hydrocodone Polistirex Compared to an Equivalent Dose of a Commercially Available Refe [NCT00853190]Phase 143 participants (Actual)Interventional2003-09-30Completed
Non-inferiority, Monocentric Comparative Open Study of Two Topical Pharmaceutical Preparations (Cream and Lotion) of Dexchlorpheniramine Maleate in the Evaluation of Safety and Efficacy for the Relief of Insect Bite Related-symptoms [NCT00995397]Phase 330 participants (Anticipated)InterventionalNot yet recruiting
A Randomized Placebo Control Trial to Evaluate the Efficacy of Chlorpheniramine Maleate Nasal Spray vs. Placebo for Acute or Chronic Rhinitis [NCT04790487]Phase 2/Phase 30 participants (Actual)Interventional2019-07-30Withdrawn(stopped due to Study Period Ended/Not Completed)
First-generation OTC Antihistamine Use and Voice Function: A Preliminary Study [NCT05858216]Early Phase 110 participants (Anticipated)Interventional2023-05-15Not yet recruiting
Human Subject Research Ethics Committee, 2 nd Affiliated Hospital, School of Medicine, Zhejiang University, China [NCT04937101]78 participants (Anticipated)Interventional2021-01-01Recruiting
A Multicenter, Randomized, Double-blind, Placebo-controlled, Dose-escalation Study to Determine the Depth and Duration of Hepatitis B Surface Antigen (HBsAg) Reduction After a Single Intravenous Dose of ARC-520 in Combination With Entecavir in Patients Wi [NCT02065336]Phase 258 participants (Actual)Interventional2014-03-31Terminated(stopped due to Company decision to discontinue trial)
A Randomized Controlled Study Comparing the Prophylactic Effect of histamine1 and Histamine 2 Receptor Blocker in Prevention Systolic Hypotension After Protamine Administration in Cardiac Patient Having Cardiopulmonary Bypass [NCT03583567]Phase 440 participants (Actual)Interventional2018-09-05Completed
A Multicentric, Randomized, Double-Blind, Comparative, Prospective, Placebo-controlled, Phase-II/III Clinical Trial (ACCROS-III) [NCT05886829]Phase 2/Phase 3157 participants (Actual)Interventional2022-07-27Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT02065336 (16) [back to overview]Change From Baseline in Entecavir Plasma Trough Concentration, Cohorts 1-7
NCT02065336 (16) [back to overview]Change From Baseline Over Time in Quantitative Hepatitis B Surface Antigen (HBsAG)
NCT02065336 (16) [back to overview]Change From Baseline Over Time in Quantitative Hepatitis B Surface Antigen (HBsAG)
NCT02065336 (16) [back to overview]Change From Baseline Over Time in Quantitative Hepatitis B Surface Antigen (HBsAG)
NCT02065336 (16) [back to overview]Change From Baseline Over Time in Quantitative Hepatitis B Surface Antigen (HBsAG)
NCT02065336 (16) [back to overview]Number of Participants With Negative Bee Venom Allergy Test Results at Baseline, Day 29, and Day 85
NCT02065336 (16) [back to overview]Number of Participants With Treatment-Emergent Adverse Events (TEAEs) and Serious Adverse Events (SAEs)
NCT02065336 (16) [back to overview]Pharmacokinetics of ARC-520 of ARC-520 Product Constituents AD0009 and AD0010: Area Under the Plasma Concentration-Time Curve From Time 0 to the Last Quantifiable Plasma Concentration (AUClast), Cohorts 1-5
NCT02065336 (16) [back to overview]Pharmacokinetics of ARC-520 Product Constituents AD0009 and AD0010: Apparent Volume of Distribution During the Terminal Phase (Vz), Cohorts 1-5
NCT02065336 (16) [back to overview]Pharmacokinetics of ARC-520 Product Constituents AD0009 and AD0010: Area Under the Plasma Concentration-Time Curve From Time 0 Extrapolated to Infinity (AUCinf), Cohorts 1-5 Only
NCT02065336 (16) [back to overview]Pharmacokinetics of ARC-520 Product Constituents AD0009 and AD0010: Area Under the Plasma Concentration-Time Curve From Time 0 to 24 Hours (AUC0-24), Cohorts 1-5
NCT02065336 (16) [back to overview]Pharmacokinetics of ARC-520 Product Constituents AD0009 and AD0010: Clearance (CL), Cohorts 1-5
NCT02065336 (16) [back to overview]Pharmacokinetics of ARC-520 Product Constituents AD0009 and AD0010: Maximum Observed Plasma Concentration (Cmax), Cohorts 1-5
NCT02065336 (16) [back to overview]Pharmacokinetics of ARC-520 Product Constituents AD0009 and AD0010: Terminal Elimination Half-Life (t1/2), Cohorts 1-5
NCT02065336 (16) [back to overview]Pharmacokinetics of ARC-520 Product Constituents AD0009 and AD0010: Terminal Elimination Rate Constant (Kel), Cohorts 1-5
NCT02065336 (16) [back to overview]Pharmacokinetics of ARC-520 Product Constituents AD0009 and AD0010: Volume in Steady State (Vss), Cohorts 1-5
NCT03879772 (6) [back to overview]Change From Baseline in the Total Nasal Symptom Score (TNSS) [Average of Morning (AM), Evening (PM) Score] Averaged Over Days 1 to 15 as Assessed by Participant
NCT03879772 (6) [back to overview]Change From Baseline in the Total Nasal Symptom Score (TNSS) [Average of Morning (AM)/Evening (PM) Score] Averaged Over Days 16 to 29 as Assessed by Participant
NCT03879772 (6) [back to overview]Change From Baseline in the Total Nasal Symptom Score (TNSS) at Day 8 as Assessed by Investigator
NCT03879772 (6) [back to overview]Change From Baseline in the Total Nasal Symptom Score (TNSS) on Day 15 as Assessed by Investigator
NCT03879772 (6) [back to overview]Change From Baseline in the Total Nasal Symptom Score (TNSS) on Day 29 as Assessed by Investigator
NCT03879772 (6) [back to overview]Change From Baseline in the Total Nasal Symptom Score (TNSS) on Day 4 as Assessed by Investigator

Change From Baseline in Entecavir Plasma Trough Concentration, Cohorts 1-7

(NCT02065336)
Timeframe: Baseline, Days 1, 2, 3, 8, 15, 22, 29

,,,,,,
Interventionng/mL (Mean)
Day 1Day 2Day 3Day 8Day 15Day 22Day 29
ARC-520 Cohort 100.06-0.02-0.010.010.040.00
ARC-520 Cohort 200.06-0.06-0.09-0.03-0.02-0.01
ARC-520 Cohort 300.13-0.06-0.09-0.03-0.030.01
ARC-520 Cohort 60-0.91-1.04-1.01-1.01-1.00-1.00
ARC-520 Cohort 700.160.150.450.320.330.36
ARC-520 Cohorts 4 and 500.120.12-0.030.000.000.00
Placebo Normal Saline Cohorts 1-50-0.31-0.29-0.30-0.10-0.30-0.30

[back to top]

Change From Baseline Over Time in Quantitative Hepatitis B Surface Antigen (HBsAG)

(NCT02065336)
Timeframe: Baseline, through Day 85 (Cohorts 1-7) and through 24 weeks post-last dose (last dose: Day 85 Cohort 9; Day 253 Cohort 10)

InterventionIU/mL (Mean)
Day 1Day 29Day 57Day 85Day 113Day 141Day 169Day 197Day 225Day 253
ARC-520 Cohort 10-19222-22617-22840-23305-23205-23182-26481-30234-1249-643

[back to top]

Change From Baseline Over Time in Quantitative Hepatitis B Surface Antigen (HBsAG)

(NCT02065336)
Timeframe: Baseline, through Day 85 (Cohorts 1-7) and through 24 weeks post-last dose (last dose: Day 85 Cohort 9; Day 253 Cohort 10)

InterventionIU/mL (Mean)
Day 3Day 8Day 15Day 22Day 29Day 43Day 85
ARC-520 Cohort 1-554.8-928.1-1055.1-1225.4-579.1-1020.1-670.1

[back to top]

Change From Baseline Over Time in Quantitative Hepatitis B Surface Antigen (HBsAG)

(NCT02065336)
Timeframe: Baseline, through Day 85 (Cohorts 1-7) and through 24 weeks post-last dose (last dose: Day 85 Cohort 9; Day 253 Cohort 10)

InterventionIU/mL (Mean)
Day 3Day 8Day 22Day 29Day 43Day 57Day 85
ARC-520 Cohort 6-948.0-1344.0-1553.7-1532.3-1566.8-1370.7-791.0

[back to top]

Change From Baseline Over Time in Quantitative Hepatitis B Surface Antigen (HBsAG)

(NCT02065336)
Timeframe: Baseline, through Day 85 (Cohorts 1-7) and through 24 weeks post-last dose (last dose: Day 85 Cohort 9; Day 253 Cohort 10)

,,,,,
InterventionIU/mL (Mean)
Day 3Day 8Day 15Day 22Day 29Day 43Day 57Day 85
ARC-520 Cohort 3-1003.6-884.3-470.8-204.393.3-1471.8-2330.1-2119.3
ARC-520 Cohort 4-1501.0-2591.2-3069.0-2978.8-2972.8-3219.8-2813.0-926.3
ARC-520 Cohort 5-1664.7-1789.8-1672.8-1951.7-1964.3-1939.7-1536.0-537.5
ARC-520 Cohort 2-1194.0-2179.2-2260.8-2266.2-1826.3-1288.8-1056.7-542.8
ARC-520 Cohort 7-12401.1-20123.8-22915.6-23872.7-24148.3-23932.0-22658.4-20827.2
Placebo Normal Saline Cohorts 1-543.342.2236.6115.1168.858.3156.1225.4

[back to top]

Number of Participants With Negative Bee Venom Allergy Test Results at Baseline, Day 29, and Day 85

Bee venom allergy tests were used to assess immunoglobulin E (IgE) in Cohorts 1-7. Analysis values less than 0.35 kU/L were taken as negative. (NCT02065336)
Timeframe: Baseline, Day 29, Day 85

,,,,,,,
InterventionParticipants (Count of Participants)
BaselineDay 29Day 85
ARC-520 Cohort 1666
ARC-520 Cohort 2666
ARC-520 Cohort 3666
ARC-520 Cohort 4666
ARC-520 Cohort 5666
ARC-520 Cohort 6666
ARC-520 Cohort 7121111
Placebo Normal Saline Cohorts 1-5101010

[back to top]

Number of Participants With Treatment-Emergent Adverse Events (TEAEs) and Serious Adverse Events (SAEs)

An adverse event (AE) is any untoward medical occurrence which does not necessarily have a causal relationship with this treatment. An SAE is any AE that: results in death; is life-threatening; requires inpatient hospitalization or prolongation of an existing hospitalization; results in persistent or significant disability/incapacity; is a congenital anomaly/birth defect; or is a medically important event or reaction.Events were categorized as mild, moderate or severe. TEAEs were defined as all AEs starting or worsening after commencement of treatment with investigational product. A treatment-related TEAE was one whose relationship to treatment was noted as unlikely, possibly, or probably related. (NCT02065336)
Timeframe: through Day 85 (Cohorts 1-7) and through 24 weeks post-last dose (last dose: Day 85 Cohort 9; Day 225 Cohort 10)

,,,,,,,,,
InterventionParticipants (Count of Participants)
Any TEAEAny mild TEAEAny moderate TEAEAny severe TEAEAny TEAE related to study drugAny TEAE leading to discontinuation of treatmentAny SAEAny SAE related to study drugAny life-threatening SAEAny SAE leading to death
ARC-520 Cohort 11100000000
ARC-520 Cohort 107700400000
ARC-520 Cohort 24310000000
ARC-520 Cohort 31100000000
ARC-520 Cohort 40000000000
ARC-520 Cohort 51100000000
ARC-520 Cohort 61100000000
ARC-520 Cohort 71100000000
ARC-520 Cohort 91100000000
Placebo Normal Saline Cohorts 1-50000000000

[back to top]

Pharmacokinetics of ARC-520 of ARC-520 Product Constituents AD0009 and AD0010: Area Under the Plasma Concentration-Time Curve From Time 0 to the Last Quantifiable Plasma Concentration (AUClast), Cohorts 1-5

(NCT02065336)
Timeframe: Day 1 predose, immediately prior to the end of infusion, 0.5, 1, 3, 6, 24, and 48 hours postdose

,,,,
Interventionµg*hr/mL (Mean)
AD0009AD0010
ARC-520 Cohort 181.497.6
ARC-520 Cohort 2196205
ARC-520 Cohort 3218317
ARC-520 Cohort 4326385
ARC-520 Cohort 5356434

[back to top]

Pharmacokinetics of ARC-520 Product Constituents AD0009 and AD0010: Apparent Volume of Distribution During the Terminal Phase (Vz), Cohorts 1-5

(NCT02065336)
Timeframe: Day 1 predose, immediately prior to the end of infusion, 0.5, 1, 3, 6, 24, and 48 hours postdose

,,,,
InterventionmL/kg (Mean)
AD0009AD0010
ARC-520 Cohort 139.539.4
ARC-520 Cohort 243.246.1
ARC-520 Cohort 345.737.1
ARC-520 Cohort 439.037.9
ARC-520 Cohort 535.436.9

[back to top]

Pharmacokinetics of ARC-520 Product Constituents AD0009 and AD0010: Area Under the Plasma Concentration-Time Curve From Time 0 Extrapolated to Infinity (AUCinf), Cohorts 1-5 Only

(NCT02065336)
Timeframe: Day 1 predose, immediately prior to the end of infusion, 0.5, 1, 3, 6, 24, and 48 hours postdose

,,,,
Interventionµg*hr/mL (Mean)
AD0009AD0010
ARC-520 Cohort 181.497.8
ARC-520 Cohort 2196207
ARC-520 Cohort 3218318
ARC-520 Cohort 4326386
ARC-520 Cohort 5356435

[back to top]

Pharmacokinetics of ARC-520 Product Constituents AD0009 and AD0010: Area Under the Plasma Concentration-Time Curve From Time 0 to 24 Hours (AUC0-24), Cohorts 1-5

(NCT02065336)
Timeframe: Day 1 predose, immediately prior to the end of infusion, 0.5, 1, 3, 6, 24, and 48 hours postdose

,,,,
Interventionµg*hr/mL (Mean)
AD0009AD0010
ARC-520 Cohort 179.193.0
ARC-520 Cohort 2185190
ARC-520 Cohort 3212301
ARC-520 Cohort 4318370
ARC-520 Cohort 5349412

[back to top]

Pharmacokinetics of ARC-520 Product Constituents AD0009 and AD0010: Clearance (CL), Cohorts 1-5

(NCT02065336)
Timeframe: Day 1 predose, immediately prior to the end of infusion, 0.5, 1, 3, 6, 24, and 48 hours postdose

,,,,
InterventionmL/hr/kg (Mean)
AD0009AD0010
ARC-520 Cohort 16.215.16
ARC-520 Cohort 25.585.08
ARC-520 Cohort 37.114.84
ARC-520 Cohort 46.475.41
ARC-520 Cohort 55.704.65

[back to top]

Pharmacokinetics of ARC-520 Product Constituents AD0009 and AD0010: Maximum Observed Plasma Concentration (Cmax), Cohorts 1-5

(NCT02065336)
Timeframe: Day 1 predose, immediately prior to the end of infusion, 0.5, 1, 3, 6, 24, and 48 hours postdose

,,,,
Interventionµg/mL (Mean)
AD0009AD0010
ARC-520 Cohort 113.712.7
ARC-520 Cohort 226.422.5
ARC-520 Cohort 333.539.7
ARC-520 Cohort 454.850.5
ARC-520 Cohort 558.252.4

[back to top]

Pharmacokinetics of ARC-520 Product Constituents AD0009 and AD0010: Terminal Elimination Half-Life (t1/2), Cohorts 1-5

(NCT02065336)
Timeframe: Day 1 predose, immediately prior to the end of infusion, 0.5, 1, 3, 6, 24, and 48 hours postdose

,,,,
Interventionhours (Median)
AD0009AD0010
ARC-520 Cohort 14.385.29
ARC-520 Cohort 25.366.32
ARC-520 Cohort 34.645.48
ARC-520 Cohort 44.184.79
ARC-520 Cohort 54.325.36

[back to top]

Pharmacokinetics of ARC-520 Product Constituents AD0009 and AD0010: Terminal Elimination Rate Constant (Kel), Cohorts 1-5

(NCT02065336)
Timeframe: Day 1 predose, immediately prior to the end of infusion, 0.5, 1, 3, 6, 24, and 48 hours postdose

,,,,
Intervention1/hr (Mean)
AD0009AD0010
ARC-520 Cohort 10.1570.132
ARC-520 Cohort 20.1320.111
ARC-520 Cohort 30.1540.130
ARC-520 Cohort 40.1650.142
ARC-520 Cohort 50.1610.126

[back to top]

Pharmacokinetics of ARC-520 Product Constituents AD0009 and AD0010: Volume in Steady State (Vss), Cohorts 1-5

(NCT02065336)
Timeframe: Day 1 predose, immediately prior to the end of infusion, 0.5, 1, 3, 6, 24, and 48 hours postdose

,,,,
InterventionmL/kg (Mean)
AD0009AD0010
ARC-520 Cohort 139.640.7
ARC-520 Cohort 245.846.7
ARC-520 Cohort 345.338.1
ARC-520 Cohort 439.639.8
ARC-520 Cohort 535.338.5

[back to top]

Change From Baseline in the Total Nasal Symptom Score (TNSS) [Average of Morning (AM), Evening (PM) Score] Averaged Over Days 1 to 15 as Assessed by Participant

Mean change from baseline (CFB) averaged over study days 1-15 was calculated for TNSS assessed by participants (with assistance from caregiver). Participants scored 4 symptoms (rhinorrhea, stuffiness, itching, sneezing) in diaries using the scale 0=none, 1=mild, 2=moderate, 3=severe. TNSS was the sum of the 4 individual scores (range=0-12; higher score indicating more frequent/severe nasal symptoms.) CFD=the 15-day average score-baseline score. Scores were recorded twice daily, in the morning (AM) and evening (PM). Average AM/PM scores were first calculated separately, then averaged together to obtain the 15-day average score. If diary entries were missing, an average AM or PM score was not calculated. If neither average AM nor PM score were calculated, the total 15-day average score was not calculated. Baseline score=Mean of the Baseline AM (day of visit plus 3 preceding days) and the Baseline PM (3 preceding days) scores. Negative change indicated a decrease in symptom severity. (NCT03879772)
Timeframe: Baseline and Days 1 through 15 (average over 15 days)

,,,,
InterventionScores on a scale (Mean)
BaselineChange From Baseline Days 1 to 15
BDP 84 mcg BID6.6-1.9
MFNS 100 mcg QD6.9-1.9
MFNS 200 mcg QD6.9-1.8
MFNS 25 mcg QD6.3-1.5
Placebo6.8-1.2

[back to top]

Change From Baseline in the Total Nasal Symptom Score (TNSS) [Average of Morning (AM)/Evening (PM) Score] Averaged Over Days 16 to 29 as Assessed by Participant

Mean change from baseline (CFB) averaged over study days 1-15 was calculated for TNSS assessed by participants (with assistance from caregiver). Participants scored 4 symptoms (rhinorrhea, stuffiness, itching, sneezing) in diaries using the scale 0=none, 1=mild, 2=moderate, 3=severe. TNSS was the sum of the 4 individual scores (range=0-12; higher score indicating more frequent/severe nasal symptoms.) CFD=the 15-day average score-baseline score. Scores were recorded twice daily, in the morning (AM) and evening (PM). Average AM/PM scores were first calculated separately, then averaged together to obtain the 15-day average score. If diary entries were missing, an average AM or PM score was not calculated. If neither average AM nor PM score were calculated, the total 15-day average score was not calculated. Baseline score=Mean of the Baseline AM (day of visit plus 3 preceding days) and the Baseline PM (3 preceding days) scores. Negative change indicated a decrease in symptom severity. (NCT03879772)
Timeframe: Baseline and Days 16 through 29 (average over 15 days)

,,,,
InterventionScores on a scale (Mean)
BaselineChange From Baseline Days 16 to 29
BDP 84 mcg BID6.6-2.6
MFNS 100 mcg QD6.9-2.8
MFNS 200 mcg QD6.9-2.7
MFNS 25 mcg QD6.3-2.1
Placebo6.8-1.7

[back to top]

Change From Baseline in the Total Nasal Symptom Score (TNSS) at Day 8 as Assessed by Investigator

The mean change from baseline at study day 8 was calculated for TNSS as assessed by the investigator. TNSS was a composite of the individual nasal symptom scores of discharge (rhinorrhea), stuffiness, sneezing, and itching. The 4 individual nasal symptom scores were rated by the investigator at the visit as follows: 0=none, 1=mild, 2=moderate, 3=severe. TNSS was the sum of the 4 individual nasal symptom scores (range= 0-12; higher score indicating more frequent/severe nasal symptoms). For each participant, individual scores were totaled and used to calculate the change from Baseline in TNSS at the visit. Participant changes were then used to calculate the mean change for each treatment group at that visit. Change from Baseline = visit score - Baseline score (Day 1 visit). Negative changes indicate a decrease in symptom severity. (NCT03879772)
Timeframe: Baseline (Day 1) and Day 8

,,,,
InterventionScores on a scale (Mean)
BaselineChange From Baseline Day 8
BDP 84 mcg BID8.0-2.8
MFNS 100 mcg QD8.1-2.8
MFNS 200 mcg QD7.9-2.8
MFNS 25 mcg QD7.8-2.8
Placebo8.0-1.9

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Change From Baseline in the Total Nasal Symptom Score (TNSS) on Day 15 as Assessed by Investigator

The mean change from baseline at study day 15 was calculated for TNSS as assessed by the investigator. TNSS was a composite of the individual nasal symptom scores of discharge (rhinorrhea), stuffiness, sneezing, and itching. The 4 individual nasal symptom scores were rated by the investigator at the visit as follows: 0=none, 1=mild, 2=moderate, 3=severe. TNSS was the sum of the 4 individual nasal symptom scores (range= 0-12; higher score indicating more frequent/severe nasal symptoms). For each participant, individual scores were totaled and used to calculate the change from Baseline in TNSS at the visit. Participant changes were then used to calculate the mean change for each treatment group at that visit. Change from Baseline = visit score - Baseline score (Day 1 visit). Negative changes indicate a decrease in symptom severity. (NCT03879772)
Timeframe: Baseline (Day 1) and Day 15

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InterventionScores on a scale (Mean)
BaselineChange From Baseline Day 15
BDP 84 mcg BID8.0-3.5
MFNS 100 mcg QD8.1-3.0
MFNS 200 mcg QD7.9-3.1
MFNS 25 mcg QD7.8-2.9
Placebo8.0-2.4

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Change From Baseline in the Total Nasal Symptom Score (TNSS) on Day 29 as Assessed by Investigator

The mean change from baseline at study day 29 was calculated for TNSS as assessed by the investigator. TNSS was a composite of the individual nasal symptom scores of discharge (rhinorrhea), stuffiness, sneezing, and itching. The 4 individual nasal symptom scores were rated by the investigator at the visit as follows: 0=none, 1=mild, 2=moderate, 3=severe. TNSS was the sum of the 4 individual nasal symptom scores (range= 0-12; higher score indicating more frequent/severe nasal symptoms). For each participant, individual scores were totaled and used to calculate the change from Baseline in TNSS at the visit. Participant changes were then used to calculate the mean change for each treatment group at that visit. Change from Baseline = visit score - Baseline score (Day 1 visit). Negative changes indicate a decrease in symptom severity. (NCT03879772)
Timeframe: Baseline (Day 1) and Day 29

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InterventionScores on a scale (Mean)
BaselineChange From Baseline Day 29
BDP 84 mcg BID8.0-3.7
MFNS 100 mcg QD8.1-3.7
MFNS 200 mcg QD7.9-3.8
MFNS 25 mcg QD7.8-3.1
Placebo8.0-2.5

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Change From Baseline in the Total Nasal Symptom Score (TNSS) on Day 4 as Assessed by Investigator

The mean change from baseline at study day 4 was calculated for TNSS as assessed by the investigator. TNSS was a composite of the individual nasal symptom scores of discharge (rhinorrhea), stuffiness, sneezing, and itching. The 4 individual nasal symptom scores were rated by the investigator at the visit as follows: 0=none, 1=mild, 2=moderate, 3=severe. TNSS was the sum of the 4 individual nasal symptom scores (range= 0-12; higher score indicating more frequent/severe nasal symptoms). For each participant, individual scores were totaled and used to calculate the change from Baseline in TNSS at the visit. Participant changes were then used to calculate the mean change for each treatment group at that visit. Change from Baseline = visit score - Baseline score (Day 1 visit). Negative changes indicate a decrease in symptom severity. (NCT03879772)
Timeframe: Baseline (Day 1) and Day 4

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InterventionScores on a scale (Mean)
BaselineChange From Baseline Day 4
BDP 84 mcg BID8.0-2.4
MFNS 100 mcg QD8.1-2.0
MFNS 200 mcg QD7.9-2.0
MFNS 25 mcg QD7.8-2.2
Placebo8.0-1.3

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