Page last updated: 2024-11-04

hydroxyzine

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Description

Hydroxyzine is an antihistamine that is used to treat anxiety, itching, and allergies. It works by blocking the action of histamine, a chemical that is released in the body during allergic reactions. Hydroxyzine is available as a tablet, capsule, syrup, and injection. The synthesis of hydroxyzine involves several steps, including the reaction of a chlorophenylacetic acid with a piperazine derivative. Hydroxyzine has a sedative effect and can cause drowsiness, dizziness, and dry mouth. It is also important to note that hydroxyzine can interact with other medications, so it is important to talk to your doctor before taking it. Hydroxyzine is studied because it is an effective treatment for anxiety, itching, and allergies. Research is ongoing to better understand the mechanism of action of hydroxyzine and its potential benefits and risks.'

Hydroxyzine: A histamine H1 receptor antagonist that is effective in the treatment of chronic urticaria, dermatitis, and histamine-mediated pruritus. Unlike its major metabolite CETIRIZINE, it does cause drowsiness. It is also effective as an antiemetic, for relief of anxiety and tension, and as a sedative. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

hydroxyzine : A N-alkylpiperazine that is piperzine in which the nitrogens atoms are substituted by 2-(2-hydroxyethoxy)ethyl and (4-chlorophenyl)(phenyl)methyl groups respectively. [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 CID3658
CHEMBL ID896
CHEBI ID5818
SCHEMBL ID4491
MeSH IDM0010792

Synonyms (170)

Synonym
BRD-A62428732-096-02-6
BRD-A62428732-300-03-0
np 212
ethanol, 2-[2-[4-(p-chloro-.alpha.-phenylbenzyl)-1-piperazinyl]ethoxy]-
atara
nevrolaks
u.c.b 4492
idrossizina
1-(p-chlorodiphenylmethyl)-4-[2-(2-hydroxyethoxy)ethyl]piperazine
atarazoid
hychotine
2-[2-[4-(p-chloro-.alpha.-phenylbenzyl)-1-piperazinyl]ethoxy]ethanol
paxistil
atarax base
plaxidol
tran-q
ucb 492
placidol
atazina
parenteral
nsc169188
ataraxoid
deinait
n-(4-chlorobenzhydryl)-n'-(hydroxyethoxyethyl)piperazine
wln: t6n dntj ayr&r d6& d2o2q
vistaril
aterax
nsc-169188
1-(p-chlorobenzhydryl)-4-[2-(2-hydroxyethoxy)ethyl]piperazine
atarox
vesparaz-wirkstoff
pamazone
ethanol, 2-[2-[4-[(4-chlorophenyl)phenylmethyl]-1-piperazinyl]ethoxy]-
1-(p-chloro-.alpha.-phenylbenzyl)-4-[2-[(2-hydroxyethoxy)ethyl]piperazine
hydroxyzin
hydroxine
traquizine
hydroxycine
neo-calma
neurozina
1-(p-chlorobenzhydryl)-4-[2-(2-hydroxyethoxy)ethyl]diethylenediamine
hydroxizine
PRESTWICK2_000133
2-[(2-{4-[(4-chlorophenyl)(phenyl)methyl]piperazin-1-yl}ethyl)oxy]ethanol
chembl896 ,
2-(2-{4-[(4-chlorophenyl)(phenyl)methyl]piperazin-1-yl}ethoxy)ethan-1-ol
bdbm22875
hydroxyzine, (r)
nsc 169188
hidroxizina [inn-spanish]
1-(p-chlorodiphenylmethyl)-4-(2-(2-hydroxyethoxy)ethyl)piperazine
einecs 200-693-1
hydroxyzine [inn:ban]
ucb 4492
tranquizine
hydroxyzinum [inn-latin]
1-(p-chlorobenzhydryl)-4-(2-(2-hydroxyethoxy)ethyl)diethylenediamine
2-(2-(4-((4-chlorophenyl)phenylmethyl)-1-piperazinyl)ethoxy)ethanol
brn 0321392
ethanol, 2-(2-(4-((4-chlorophenyl)phenylmethyl)-1-piperazinyl)ethoxy)-
hsdb 3098
2-(2-(4-(p-chloro-alpha-phenylbenzyl)-1-piperazinyl)ethoxy)ethanol
idrossizina [dcit]
1-(p-chlorobenzhydryl)-4-(2-(2-hydroxyethoxy)ethyl)piperazine
1-(p-chloro-alpha-phenylbenzyl)-4-(2-hydroxyethoxyethyl)piperazine
vistaril parenteral
u.cb 4492
1-(p-chloro-alpha-phenylbenzyl)-4-(2-(2-hydroxyethoxy)ethyl)piperazine
hydroksyzyny [polish]
n-(4-chlorobenzhydryl)-n'-(hydroxyethyloxyethyl)piperazine
ethanol, 2-(2-(4-(p-chloro-alpha-phenylbenzyl)-1-piperazinyl)ethoxy)-
PRESTWICK3_000133
BSPBIO_000206
2-(2-{4-[(4-chlorophenyl)(phenyl)methyl]piperazin-1-yl}ethoxy)ethanol
hidroxizina
CHEBI:5818 ,
hydroxyzinum
BPBIO1_000228
AB00053485
68-88-2
hydroxyzine
C07045
DB00557
hydroxizinum
PRESTWICK0_000133
SPBIO_002145
PRESTWICK1_000133
AKOS003334349
u.c.b-4492
L000930
D08054
hydroxyzine (inn)
marex (tn)
2-[2-[4-[(4-chlorophenyl)-phenylmethyl]piperazin-1-yl]ethoxy]ethanol
NCGC00089816-03
NCGC00018255-03
NCGC00018255-02
NCGC00018255-04
NCGC00018255-06
tox21_113569
dtxsid8023137 ,
cas-68-88-2
dtxcid203137
hydroxyzyne
hydroxyzine base
FT-0670239
5-23-01-00462 (beilstein handbook reference)
unii-30s50ym8og
30s50ym8og ,
hydroksyzyny
gtpl7199
hydroxyzine [mi]
147152-21-4
hydroxyzine [inn]
(+/-)-2-(2-(4-(p-chloro-.alpha.-phenylbenzyl)-1-piperazinyl)ethoxy)ethanol
2-(2-(4-(p-chloro-.alpha.-phenylbenzyl)-1-piperazinyl)ethoxy)ethanol
1-(p-chloro-.alpha.-phenylbenzyl)-4-(2-((2-hydroxyethoxy)ethyl))piperazine
ethanol, 2-(2-(4-(4-chloro-.alpha.-phenylbenzyl)-1-piperazinyl)ethoxy)-
hydroxyzine [mart.]
hydroxyzine [who-dd]
ethanol, 2-(2-(4-((4-chlorophenyl)phenylmethyl)-1-piperazinyl)ethoxy)-,(+/-)-
(+/-)-hydroxyzine
hydroxyzine [hsdb]
hydroxyzine [vandf]
HY-B0548
SCHEMBL4491
tox21_113569_1
NCGC00021152-06
2-[2-[4-[(4-chlorophenyl)-phenyl-methyl]piperazin-1-yl]ethoxy]ethanol
AKOS016843978
2-[2-[4-[(4-chlorophenyl)phenylmethyl]-1-piperazinyl]ethoxy]ethanol
BBL034752
STL417960
ucb-4492
atarax (salt/mix)
durrax (salt/mix)
1-(p-chloro-.alpha.-phenylbenzyl)-4-(2-((2-hydroxyethoxy)ethyl)piperazine
vistaril (salt/mix)
ZQDWXGKKHFNSQK-UHFFFAOYSA-N
2-(2-(4-[(4-chlorophenyl)(phenyl)methyl]-1-piperazinyl)ethoxy)ethanol #
disron (salt/mix)
2-(2-(4-((4-chlorophenyl)(phenyl)methyl)piperazin-1-yl)ethoxy)ethanol
HMS3604B10
AB00053485_25
AB00053485_24
2-(2-{4-[(4-chloro-phenyl)-phenyl-methyl]-piperazin-1-yl}-ethoxy)-ethanol
mfcd00242772
MRF-0000015
ethanol,2-[2-[4-[(4-chlorophenyl)phenylmethyl]-1-piperazinyl]ethoxy]-
Q421937
2-(2-(4-((4-chlorophenyl)(phenyl)methyl)-piperazin-1-yl)ethoxy)ethanol
W13117
hydroxyzine free base
68-88-2 (free base)
1-(p-chloro-?-phenylbenzyl)-4-[2-(2-hydroxyethoxy)ethyl)]piperazine
EN300-708786
AS-81900
ulgrax
1-(p-chloro-alpha-phenylbenzyl)-4-(2-((2-hydroxyethoxy)ethyl))piperazine
multipax
(+/-)-2-(2-(4-(p-chloro-alpha-phenylbenzyl)-1-piperazinyl)ethoxy)ethanol
1-(p-chlorodiphenylmethyl)-4-
hydroxyzine (mart.)
idroxizina
hydroxyzinum (inn-latin)
1-(p-chlorobenzhydryl)-4-
n05bb01
ethanol, 2-(2-(4-(4-chloro-alpha-phenylbenzyl)-1-piperazinyl)ethoxy)-
orgatax
hidroxizina (inn-spanish)

Research Excerpts

Overview

Hydroxyzine is a first generation antihistamine widely used in the paediatric population for a variety of conditions. Hydroxyzine was found to be a competitive inhibitor of MAO-B (Ki - 38 microM), whereas it had a low potency towards MAo-A (IC50 > 630 microM).

ExcerptReferenceRelevance
"Hydroxyzine HCL (HHCL) is an antihistamine, used for the treatment of allergic skin conditions. "( Formulation and assessment of hydroxyzine HCL solid lipid nanoparticles by dual emulsification technique for transdermal delivery.
Ahmed, KA; El-Feky, YA; El-Telbany, DFA; El-Telbany, RFA; Zakaria, S, 2021
)
2.35
"Hydroxyzine is an antihistamine drug used for symptomatic relief of anxiety and tension. "( Hydroxyzine for lowering patient's anxiety during prehospital morphine analgesia: A prospective randomized double blind study.
Balen, F; Battefort, F; Bounes, V; Houze-Cerfon, CH; Houze-Cerfon, V; Motuel, J, 2021
)
3.51
"Hydroxyzine is a first-generation antihistamine and cetirizine, a second-generation antihistamine and active metabolite of hydroxyzine. "( Pharmacokinetics of hydroxyzine and cetirizine following oral administration of hydroxyzine to exercised Thoroughbred horses.
Flynn, K; Knych, HK; McKemie, DS; Steinmetz, S; Weiner, D, 2019
)
2.28
"Hydroxyzine is an antihistaminic with sedative properties used in the control of anxiety and emesis. "( Hydroxyzine distribution in postmortem cases and potential for redistribution.
Mallett, P; McIntyre, IM; Morhaime, J; Trochta, A, 2013
)
3.28
"Hydroxyzine is an anti-histamine medication which has been used in the treatment of anxiety."( Hydroxyzine for generalised anxiety disorder.
Barbui, C; Cipriani, A; Guaiana, G, 2010
)
2.52
"Hydroxyzine is a first generation antihistamine widely used in the paediatric population for a variety of conditions. "( Hydroxyzine-induced supraventricular tachycardia in a nine-year-old child.
Rasool, AH; Wong, AR, 2004
)
3.21
"Hydroxyzine was found to be a competitive inhibitor of MAO-B (Ki - 38 microM), whereas it had a low potency towards MAO-A (IC50 > 630 microM)."( Inhibition of amine oxidases by the histamine-1 receptor antagonist hydroxyzine.
Davey, G; O'Sullivan, J; O'Sullivan, MI; Tipton, KE, 2006
)
1.29
"Hydroxyzine is an effective therapy."( Follicular dermographism.
Shelley, ED; Shelley, WB, 1983
)
0.99
"Hydroxyzine is a piperazine, tricyclic, H1-receptor antagonist with unique properties, especially the inhibition of mast cell and neuronal secretion. "( Hydroxyzine in the treatment of interstitial cystitis.
Theoharides, TC, 1994
)
3.17
"Hydroxyzine is a useful drug for the symptomatic treatment of IC, especially in patients with documented allergies and/or evidence of bladder mast cell activation."( Hydroxyzine therapy for interstitial cystitis.
Sant, GR; Theoharides, TC, 1997
)
3.18
"Hydroxyzine is a commonly prescribed H1-receptor antagonist in small animal practice. "( Coma and apnea in a dog with hydroxyzine toxicosis.
Puschner, B; Smarick, SD; Tegzes, JH, 2002
)
2.05

Effects

Hydroxyzine has a long t1/2 and a large volume of distribution in the elderly. It has been used for many years for the treatment of allergic symptoms.

ExcerptReferenceRelevance
"Hydroxyzine has a long t1/2 and a large volume of distribution in the elderly."( Pharmacokinetic and pharmacodynamic studies of the H1-receptor antagonist hydroxyzine in the elderly.
Chen, XY; Simons, FE; Simons, KJ; Watson, WT, 1989
)
1.23
"Hydroxyzine 25 mg/day has equal results compared to doxepine 10 mg once daily; but greater than cetirizine 10 mg once a day in controlling the symptoms of patients with chronic pruritus."( Cetirizine, doxepine, and hydroxyzine in the treatment of pruritus due to sulfur mustard: a randomized clinical trial.
Davoudi, SM; Keshavarz, S; Sadr, B; Shohrati, M; Tajik, A, 2007
)
1.36
"Hydroxyzine has been used for many years for the treatment of allergic symptoms. "( Prospective controlled study of hydroxyzine and cetirizine in pregnancy.
Bailey, B; Baillie, M; Einarson, A; Jung, G; Koren, G; Spizzirri, D, 1997
)
2.02
"Hydroxyzine has a long t1/2 and a large volume of distribution in the elderly."( Pharmacokinetic and pharmacodynamic studies of the H1-receptor antagonist hydroxyzine in the elderly.
Chen, XY; Simons, FE; Simons, KJ; Watson, WT, 1989
)
1.23

Treatment

Hydroxyzine treatment inhibited (p<0.05) the progression and severity of EAE by 50% and the extent of mast cell degranulation by 70%. Treatment with hydroxyZine combined with a histamine-restricted diet resulted in significant general improvement.

ExcerptReferenceRelevance
"Hydroxyzine treatment inhibited (p<0.05) the progression and severity of EAE by 50% and the extent of mast cell degranulation by 70% (p<0.05)."( Hydroxyzine inhibits experimental allergic encephalomyelitis (EAE) and associated brain mast cell activation.
Dimitriadou, V; Pang, X; Theoharides, TC, 2000
)
2.47
"Treatment with hydroxyzine combined with a histamine-restricted diet resulted in significant general improvement."( Adult male patient with severe intellectual disability caused by a homozygous mutation in the HNMT gene.
Egger, JIM; Janssen, PKC; van Haeringen, A; Verhoeven, WMA, 2020
)
0.9
"Treatment with hydroxyzine, 25 mg daily, was successful after a month follow-up in preventing wheals and erythema."( Aquagenic urticaria: report of a case.
Fiorenza, G; Frances, AM; Frances, RJ,
)
0.47
"Treatment with hydroxyzine significantly reduced the number of papillar and reticular mast cells/mm3 of affected skin."( Mast cell quantification in the skin of children with atopic dermatitis: its value in diagnosis and in assessing the effectiveness of therapy.
de Luca, IM; Guerra Júnior, G; Leonardo, MB; Vilela, MM,
)
0.47
"Treatment with hydroxyzine in patients with CU improved the clinical symptoms and modified the profile of HR; more histamine was recovered at 1 hour (p less than 0.05) and 2 hours (p less than 0.05), as compared with baseline."( Effects of H1-antihistamine drug regimen on histamine release by nonlesional skin mast cells of patients with chronic urticaria.
Bédard, PM; Brunet, C; Hébert, J, 1990
)
0.62

Toxicity

Loratadine was safe and well tolerated with sedation and dry mouth similar to placebo and significantly less than hydroxyzine.

ExcerptReferenceRelevance
" Loratadine was safe and well tolerated with sedation and dry mouth similar to placebo and significantly less than hydroxyzine."( Relative efficacy and safety of loratadine, hydroxyzine, and placebo in chronic idiopathic urticaria.
Bernstein, DI; Cuss, F; Danzig, MR; Fox, RW; Garvin, PR; Grabiec, SV; Honsinger, RW; Kalivas, JT; Katz, HI; Monroe, EW, 1992
)
0.75
"The purpose of this prospective study was to determine the frequency of adverse events associated with supplemented and unsupplemented chloral hydrate sedation in a select group of children undergoing CT or MR imaging using the revised American Academy of Pediatrics (AAP) monitoring and management guidelines for pediatric sedation."( Chloral hydrate sedation of children undergoing CT and MR imaging: safety as judged by American Academy of Pediatrics guidelines.
Dolenga, M; Habisohn-Schuck, C; Sukhani, R; Vade, A, 1995
)
0.29
"Use of supplemented and unsupplemented chloral hydrate sedation provides effective and safe sedation in children if the AAP guidelines for patient selection, monitoring, and management are followed."( Chloral hydrate sedation of children undergoing CT and MR imaging: safety as judged by American Academy of Pediatrics guidelines.
Dolenga, M; Habisohn-Schuck, C; Sukhani, R; Vade, A, 1995
)
0.29
"The authors report on adverse events and sedation outcomes for an oral sedation regimen of chloral hydrate, meperidine and hydroxyzine with 100 percent oxygen, or O2, supplementation."( Adverse events and outcomes of conscious sedation for pediatric patients: study of an oral sedation regimen.
Leelataweedwud, P; Vann, WF, 2001
)
0.52
" The authors analyzed age, sex, weight, methods of drug delivery, waiting time after drug administration, treatment rendered, treatment time, adverse events, sedation outcomes and the number of visits needed to complete treatment using descriptive statistics, chi 2 tests, t test and analysis of variance."( Adverse events and outcomes of conscious sedation for pediatric patients: study of an oral sedation regimen.
Leelataweedwud, P; Vann, WF, 2001
)
0.31
"Minimal minor adverse events occurred with this sedation regimen."( Adverse events and outcomes of conscious sedation for pediatric patients: study of an oral sedation regimen.
Leelataweedwud, P; Vann, WF, 2001
)
0.31
"This oral sedation regimen offers reasonable outcomes with minimal adverse events under a strict protocol and use of O2 supplementation."( Adverse events and outcomes of conscious sedation for pediatric patients: study of an oral sedation regimen.
Leelataweedwud, P; Vann, WF, 2001
)
0.31
"5 million adverse drug reaction (ADR) reports for 8620 drugs/biologics that are listed for 1191 Coding Symbols for Thesaurus of Adverse Reaction (COSTAR) terms of adverse effects."( Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
Benz, RD; Contrera, JF; Kruhlak, NL; Matthews, EJ; Weaver, JL, 2004
)
0.32
" No serious adverse events were observed."( Comparative efficacy and safety of topical permethrin, topical ivermectin, and oral ivermectin in patients of uncomplicated scabies.
Chhaiya, SB; Dave, JN; Mehta, DS; Patel, VJ; Shah, HA,
)
0.13
" The objective was to measure the rate of adverse pregnancy outcomes."( The fetal safety of cetirizine: an observational cohort study and meta-analysis.
Boskovic, R; Djokanovic, N; Etwel, F; Koren, G; Martinovic, J; Moretti, ME, 2014
)
0.4
"The study investigated patient discharge parameters and postdischarge adverse events after discharge among children who received oral conscious sedation for dental treatment."( Oral Sedation Postdischarge Adverse Events in Pediatric Dental Patients.
Huang, A; Tanbonliong, T, 2015
)
0.42
"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
" The most common adverse drug effect was dry mouth, although 4 of the 5 studies did not report safety outcomes."( Efficacy and safety of hydroxyzine for sleep in adults: Systematic review.
Brown, JN; Burgazli, CR; Rana, KB; Tillman, F, 2023
)
1.22

Pharmacokinetics

We have compared the pharmacokinetic properties of a slow-release theophylline-hydroxyzine combination. We studied the changes in serum half-life values and clearance rates in dogs who were administered hydroxyzine, 0.25mg. The mean serum eliminatio is calculated from the terminal linear portion of the serum hydroxyZine concentration.

ExcerptReferenceRelevance
" Following administration of 100-mg single oral doses to normal male volunteers, peak plasma concentrations of approximately 80 ng/ml were observed; the half-life of drug removal was approximately 3 hr."( Sensitive assay for determination of hydroxyzine in plasma and its human pharmacokinetics.
Fouda, HG; Hobbs, DC; Stambaugh, JE, 1979
)
0.53
"We present an approach to the analysis of pharmacodynamic (PD) data arising from non-steady-state experiments, meant to be used when only PD data, not pharmacokinetic (PK) data, are available."( Semiparametric analysis of non-steady-state pharmacodynamic data.
Sheiner, LB; Verotta, D, 1991
)
0.28
" The terminal disposition half-life of cetirizine in these patients was 19."( Effect of haemodialysis on the pharmacokinetics of cetirizine.
Awni, WM; Chung, M; Halstenson, CE; Matzke, GR; Opsahl, JA; Yeh, J, 1990
)
0.28
" The mean serum elimination half-life of hydroxyzine was 36."( The pharmacokinetics and pharmacodynamics of hydroxyzine in patients with primary biliary cirrhosis.
Chen, XY; Minuk, GY; Simons, FE; Simons, KJ; Watson, WT, 1989
)
0.8
" 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
" We found that the elimination half-life of cetirizine was prolonged in patients with mild and moderate renal insufficiency, compared with age-matched individuals with normal renal function (19."( Pharmacokinetics of cetirizine in the elderly and patients with renal insufficiency.
Awni, WM; Chung, M; Halstenson, CE; Matzke, GR; Yeh, J, 1987
)
0.27
" Cmax (362 ng/ml), Tmax (1."( Single dose pharmacokinetics of cetirizine in young and elderly volunteers.
Bernheim, J; Lefebvre, RA; Rosseel, MT, 1988
)
0.27
"We have compared the pharmacokinetic properties of a slow-release theophylline-hydroxyzine combination and a slow-release theophylline preparation both after a single dose administration and at steady state after the dosage of twice/day for four days in ten healthy volunteers."( Pharmacokinetic comparison of a slow-release theophylline-hydroxyzine combination and a plain slow-release theophylline preparation.
Karttunen, P; Kokkonen, P; Parviainen, M; Savolainen, K; Silvasti, M; Tukiainen, H, 1988
)
0.75
"A model-independent program for pharmacokinetic analyses based on statistical moment theory is presented and demonstrated."( A rapid, universal TI-59 model-independent pharmacokinetic analysis program based on statistical moment theory.
Lewin, HM; Love, SJ; Reitberg, DP; Schentag, JJ; Smith, IL, 1985
)
0.27
" The mean elimination half-life calculated from the terminal linear portion of the serum hydroxyzine concentration vs."( The pharmacokinetics and antihistaminic of the H1 receptor antagonist hydroxyzine.
Frith, EM; Simons, FE; Simons, KJ, 1984
)
0.72
" This synergism may be due, at least in part, to a pharmacokinetic effect."( Effect of the H2-antagonist cimetidine on the pharmacokinetics and pharmacodynamics of the H1-antagonists hydroxyzine and cetirizine in patients with chronic urticaria.
Simons, FE; Simons, KJ; Sussman, GL, 1995
)
0.5
" The hydroxyzine and cetirizine half-life and AUC0-->infinity values were significantly increased and the systemic clearance rates were significantly decreased in the presence of cimetidine."( Effect of the H2-receptor antagonist cimetidine, on the pharmacokinetics and pharmacodynamics of the H1-receptor antagonists hydroxyzine and cetirizine in rabbits.
Chen, X; Simons, FE; Simons, KJ, 1994
)
1.01
" 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
" Moreover, the described procedure was applied for evaluating the pharmacokinetic parameters of hydroxyzine in plasma of two healthy volunteers after administration of a single oral dose (Atarax)-25mg)."( Development of a voltammetric procedure for assay of the antihistamine drug hydroxyzine at a glassy carbon electrode: Quantification and pharmacokinetic studies.
Abdallah, OM; Beltagi, AM; Ghoneim, MM, 2008
)
0.79
" The recommended dose of levocetirizine is 5 mg once daily, while its pharmacokinetic half-life is about 7 h in humans."( Physicochemical, pharmacological and pharmacokinetic properties of the zwitterionic antihistamines cetirizine and levocetirizine.
Chen, C, 2008
)
0.35
" Pharmacodynamic studies evaluated the suppressive effect on histamine and anticanine IgE-mediated cutaneous wheal formation."( Hydroxyzine and cetirizine pharmacokinetics and pharmacodynamics after oral and intravenous administration of hydroxyzine to healthy dogs.
Bizikova, P; Olivry, T; Papich, MG, 2008
)
1.79
" Upon this basis, the conflicting literature data of cetirizine microspeciation were clarified, and the pharmacokinetic absorption-distribution properties could be interpreted."( Triprotic acid-base microequilibria and pharmacokinetic sequelae of cetirizine.
Béni, S; Kökösi, J; Kovács, Z; Marosi, A; Noszál, B, 2009
)
0.35
" The pharmacodynamic effect of the chosen preparation was tested on the shaved back of histamine sensitized rabbits."( Microencapsulation of hydroxyzine HCl by thermal phase separation: in vitro release enhancement and in vivo pharmacodynamic evaluation.
Ibrahim Soliman, I; latif Aziz, R; Zaki Rizkalla, CM, 2013
)
0.7
"This review aims to analyze pharmacokinetic profile, plasma level variations so as the metabolism, interactions and possible relation to clinical effect of several drugs which are used primarily as anxiolytics."( Understanding the pharmacokinetics of anxiolytic drugs.
Altamura, AC; Bareggi, S; Maffini, M; Mauri, MC; Moliterno, D; Paletta, S, 2013
)
0.39
"There is a need for a more balanced assessment of the benefits and risks associated with benzodiazepine use, particularly considering pharmacokinetic profile of the drugs to ensure that patients, who would truly benefit from these agents, are not denied appropriate treatment."( Understanding the pharmacokinetics of anxiolytic drugs.
Altamura, AC; Bareggi, S; Maffini, M; Mauri, MC; Moliterno, D; Paletta, S, 2013
)
0.39
" A joint parent/metabolite population 2-compartment pharmacokinetic model with first-order absorption and elimination was utilized to describe the pharmacokinetics of both compounds."( Pharmacokinetics of hydroxyzine and cetirizine following oral administration of hydroxyzine to exercised Thoroughbred horses.
Flynn, K; Knych, HK; McKemie, DS; Steinmetz, S; Weiner, D, 2019
)
0.84
" The aim of the research was to be able to provide detection times (DT) from pharmacokinetic studies in thoroughbred horses to better inform trainers, and their veterinary surgeons, prescribing these substances for treatment of Thoroughbred racehorses."( Plasma and urine pharmacokinetics of hydroxyzine and cetirizine following repeated oral administrations to exercised horses.
Aldurdunji, M; Garth-Greeves, A; Hincks, PR; Muir, T; Paine, SW, 2022
)
0.99

Compound-Compound Interactions

ExcerptReferenceRelevance
"The purpose of this study was to compare the effectiveness of a chloral hydrate/hydroxyzine combination with and without meperidine in the sedation of pediatric dental patients."( Comparison of a chloral hydrate/hydroxyzine combination with and without meperidine in the sedation of pediatric dental patients.
Farrington, FH; Mourino, AP; Poorman, TL,
)
0.64
"Present results showed that single oral doses of rupatadine 10 mg in combination with alcohol do not produce more cognitive and psychomotor impairment than alcohol alone."( Evaluation of the cognitive, psychomotor and pharmacokinetic profiles of rupatadine, hydroxyzine and cetirizine, in combination with alcohol, in healthy volunteers.
Antonijoan, R; Barbanoj, MJ; Donado, E; García-Gea, C; Izquierdo, I; Jané, F; Pérez, I; Solans, A, 2006
)
0.56

Bioavailability

ExcerptReferenceRelevance
" 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
" 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
" Cetirizine exhibits high intestinal absorption in humans and its oral bioavailability is estimated to be greater than 70%."( Physicochemical, pharmacological and pharmacokinetic properties of the zwitterionic antihistamines cetirizine and levocetirizine.
Chen, C, 2008
)
0.35
"Cell membrane permeability is an important determinant for oral absorption and bioavailability of a drug molecule."( Highly predictive and interpretable models for PAMPA permeability.
Jadhav, A; Kerns, E; Nguyen, K; Shah, P; Sun, H; Xu, X; Yan, Z; Yu, KR, 2017
)
0.46
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

Cetirizine and hydroxyzine enter the skin readily. Their sustained high concentrations in skin after single or multiple dosing may contribute to their well-known efficacy in symptomatic treatment of urticaria and other skin disorders.

ExcerptRelevanceReference
" Intradermal histamine dose-response thresholds of pruritus were obtained before and after pretreatment with the three antihistamines and placebo in each subject."( Suppression of histamine-induced pruritus by three antihistaminic drugs.
Cohan, R; Leifer, KN; Rhoades, RB; Wittig, HJ, 1975
)
0.25
" The dosage of analgesic compound required to control each episode of tension headache was smaller than that of acetaminophen."( Study of a new analgesic compound in the treatment of tension headache.
Borges, J; Zavaleta, C, 1976
)
0.26
" Using a daily dosage of up to 16 mg/kg bodyweight more than 80% of children showed definite improvement leading to prevention or significant reduction of acute attacks and clearly reduced dyspnoeic states between attacks."( [Long-term out-patient treatment of children with asthma with a theophylline-ephedrine-hydroxyzine combination (author's transl)].
Götz, M, 1975
)
0.48
" In cases with heart disease and elderly subjects, a lower dosage or omission of atropine was common."( [Manipulation, premedication, and chemoprophylaxis for fiberoptic bronchoscopy].
Hasegawa, Y; Ogasawara, T; Saka, H; Shimokata, K; Watanabe, A, 1992
)
0.28
" Spectral analysis of the EEG did not distinguish between the multi and single dosage schedules regarding the respective drugs in the low doses administered."( The comparison of the effects of multi and single doses of buspirone, chlordiazepoxide and hydroxyzine on psychomotor function and EEG.
Bartel, PR; Becker, PJ; Blom, MW; Sommers, DK; Van der Meyden, CH, 1992
)
0.5
" A dose-response relationship was evident for selected symptoms, and the once daily 5-mg dose was found to be an effective minimum dose."( Double-blind comparison of cetirizine and placebo in the treatment of seasonal rhinitis.
Altman, R; Brandon, ML; Buchman, E; Connell, JT; Dockhorn, R; Falliers, CJ; Leese, PT; Miller, J; Wasserman, SI; Zeterberg, JM, 1991
)
0.28
" These properties, combined with a once-daily dosage regimen, should help improve patient compliance and optimize antihistamine therapy."( Cetirizine: a unique second-generation antihistamine for treatment of rhinitis and chronic urticaria.
Pierson, WE,
)
0.13
" Bedtime dosing of hydroxyzine was investigated as a dosing strategy to minimize reaction time degradation and adverse subjective symptoms previously documented for hydroxyzine in divided doses."( Objective antihistamine side effects are mitigated by evening dosing of hydroxyzine.
Apaliski, SJ; Goetz, DW; Jacobson, JM; Martin, ME; Repperger, DW, 1991
)
0.84
" At the dosage used, cetirizine therapy appears to be no more effective than terfenadine."( A comparison of cetirizine and terfenadine in the management of solar urticaria.
Bilsland, D; Ferguson, J, 1991
)
0.28
"A double-blind, placebo-controlled clinical trial was undertaken for two weeks to evaluate three dosing schedules for administration of cetirizine in patients with seasonal allergic rhinitis."( Cetirizine therapy for seasonal allergic rhinitis: alternative dosage schedules.
Broide, DH; Marquardt, DL; Wasserman, SI,
)
0.13
" One subject developed moderate drowsiness during multiple dosing with cetirizine."( Effects of oral cetirizine, a selective H1 antagonist, on allergen- and exercise-induced bronchoconstriction in subjects with asthma.
Dauphinee, B; Djahed, B; Gong, H; Tashkin, DP; Wu, TC, 1990
)
0.28
" Further, astemizole has the longest time to relief of symptoms in this class; histamine wheal inhibition is not apparent until the second day of 10 mg dosing and does not peak for 9 to 12 days."( Pharmacology of antihistamines.
Woodward, JK, 1990
)
0.28
" The present study investigated the nature of desaturations in relation to patient activity as a function of a drug combination, single drug dose-response design, and placebo conditions."( Conscious sedation and pulse oximetry: false alarms?
Wilson, S,
)
0.13
" Patients number 8 through 16 gave higher ratings probably because a more idealized dosage regimen was being used by that time in the study."( Patient-controlled analgesia in patients with sickle cell vaso-occlusive crisis.
Castro, O; Finke, H; McPherson, E; Perlin, E; Pittman, J, 1990
)
0.28
" It is concluded that when a healthy child receives a sedative agent for dental treatment, the type of drug and drug dosage depend more on the biases of the individual practitioner, than on the requirements of the patient."( Report of project USAP: the use of sedative agents in pediatric dentistry.
Houpt, M,
)
0.13
" During daily dosing with cetirizine, 5 mg or 10 mg at bedtime for 35 days, serum cetirizine concentrations and suppression of histamine-induced wheals and flares were monitored every 7 days, 12 hours after the cetirizine dose."( Cetirizine: a pharmacokinetic and pharmacodynamic evaluation in children with seasonal allergic rhinitis.
Chen, XY; Simons, FE; Simons, KJ; Watson, WT, 1989
)
0.28
" 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
)
0.27
" The purpose of the evaluation was to determine whether dosage schedules of cetirizine will require modification in the elderly or patients with renal insufficiency."( Pharmacokinetics of cetirizine in the elderly and patients with renal insufficiency.
Awni, WM; Chung, M; Halstenson, CE; Matzke, GR; Yeh, J, 1987
)
0.27
"We have compared the pharmacokinetic properties of a slow-release theophylline-hydroxyzine combination and a slow-release theophylline preparation both after a single dose administration and at steady state after the dosage of twice/day for four days in ten healthy volunteers."( Pharmacokinetic comparison of a slow-release theophylline-hydroxyzine combination and a plain slow-release theophylline preparation.
Karttunen, P; Kokkonen, P; Parviainen, M; Savolainen, K; Silvasti, M; Tukiainen, H, 1988
)
0.75
" In four patients, including two of the patients in whom rapid test dosing of a sulfonamide had been unsuccessful, treatment of the sulfa reaction with corticosteroids and antihistamines permitted continued sulfa administration."( The management of patients with sulfonamide allergy.
Boxer, MB; Dykewicz, MS; Greenberger, PA; Kelly, JF; Patterson, R,
)
0.13
" Clinicians should consider giving patients with a tendency to abuse drugs nonidentifiable dosage forms."( Effect of patient recognition of tranquilizers on their use in alcohol detoxification.
Francis, DA; Nelson, AA, 1984
)
0.27
"Cetirizine and hydroxyzine enter the skin readily, and their sustained high concentrations in skin after single or multiple dosing may contribute to their well-known efficacy in symptomatic treatment of urticaria and other skin disorders in which histamine plays a role."( Quantitation of H1-receptor antagonists in skin and serum.
Murray, HE; Simons, FE; Simons, KJ, 1995
)
0.64
"The assessment model compares the official United States Pharmacopeia disintegration approach for dissolution analysis with that of the Food and Drug Administration's recommended rotating paddle technique for inducing aqueous disruption of the solid oral dosage form."( Comparative studies on the in vitro drug dissolution profiles for hydroxyzine hydrochloride tablets.
Loucas, SP; Maager, P; Mehl, B, 1993
)
0.52
" The most common adverse effect reported after therapeutic dosing is mild sedation; severe reactions resulting in coma have occasionally been reported in children."( Coma and apnea in a dog with hydroxyzine toxicosis.
Puschner, B; Smarick, SD; Tegzes, JH, 2002
)
0.61
" The only side reaction in this series was temporary drowsiness which, in the majority of patients, ceased after therapy was steadily continued on the same dosage level."( Management of emotional disturbances; use of hydroxyzine (atarax) in general practice.
DOLAN, CM, 1958
)
0.5
" Depending on the intended indication and dosing regimen, PPL can delay or stop development of a compound in the drug discovery process."( Evaluation of a published in silico model and construction of a novel Bayesian model for predicting phospholipidosis inducing potential.
Gehlhaar, D; Greene, N; Johnson, TO; Pelletier, DJ; Tilloy-Ellul, A,
)
0.13
"12% (n=5) were achieved for assay of hydroxyzine in Atarax 10 and 25mg dosage forms, respectively."( Development of a voltammetric procedure for assay of the antihistamine drug hydroxyzine at a glassy carbon electrode: Quantification and pharmacokinetic studies.
Abdallah, OM; Beltagi, AM; Ghoneim, MM, 2008
)
0.85
" We proposed a systematic classification scheme using FDA-approved drug labeling to assess the DILI potential of drugs, which yielded a benchmark dataset with 287 drugs representing a wide range of therapeutic categories and daily dosage amounts."( FDA-approved drug labeling for the study of drug-induced liver injury.
Chen, M; Fang, H; Liu, Z; Shi, Q; Tong, W; Vijay, V, 2011
)
0.37
" Therefore, the aim of the present study was to produce an effective drug-loaded dosage form that is able to control the release of hydroxyzine hydrochloride into the skin."( In vitro and in vivo evaluation of hydroxyzine hydrochloride microsponges for topical delivery.
latif Aziz, R; Soliman, II; Zaki Rizkalla, CM, 2011
)
0.85
" Trials were grouped into placebo-controlled, dosage and head-to-head comparisons."( Sedation of children undergoing dental treatment.
Ashley, PF; Furness, S; Lourenço-Matharu, L, 2012
)
0.38
" BZD dosage was reduced every 2-4 weeks by 25% of the initial dose with the optional support of Hydroxyzine or Valerian."( Analysis of benzodiazepine withdrawal program managed by primary care nurses in Spain.
Casabella, B; del Val, JL; Diogene, E; Lacasta, D; Lopez-Peig, C; Mundet, X, 2012
)
0.6
"A simple eco-friendly method has been developed for detection of hydroxyzine dihydrochloride in pure and pharmaceutical dosage forms."( Green approach towards the determination of hydroxyzine dihydrochloride in pure and pharmaceutical dosage forms.
Hussain, S; Mumtaz, A; Yasir, M, 2014
)
0.9
" Studies were grouped into placebo-controlled, dosage and head-to-head comparisons."( Sedation of children undergoing dental treatment.
Ashley, PF; Chaudhary, M; Lourenço-Matharu, L, 2018
)
0.48
"This retrospective study compares the efficacy and safety of variable dosing of Chloral Hydrate - Hydroxyzine with and without Meperidine (Mep)for managing varying levels of anxiety and uncooperative behavior of young pediatric dental patients over a 35-year period."( Comparisons of Varying Dosages of Chloral Hydrate-Hydroxyzine with and without Meperidine for Managing Challenging Pediatric Dental Behavior: A Retrospective study of 35 years of Sedation Experiences.
Nathan, JE, 2022
)
1.19
"Reviews of the sedation logs of 2,610 children, 3-7 years were compared in search of what dosing proves safe and effective for differing levels of challenging behavior."( Comparisons of Varying Dosages of Chloral Hydrate-Hydroxyzine with and without Meperidine for Managing Challenging Pediatric Dental Behavior: A Retrospective study of 35 years of Sedation Experiences.
Nathan, JE, 2022
)
0.97
"Where Mep was used, success rates were consistently higher; need for higher-end dosing of CH was not found beneficial when Mep was included."( Comparisons of Varying Dosages of Chloral Hydrate-Hydroxyzine with and without Meperidine for Managing Challenging Pediatric Dental Behavior: A Retrospective study of 35 years of Sedation Experiences.
Nathan, JE, 2022
)
0.97
"There appears to be strong basis for the safety and efficacy of the use of CH-H-Mep in combination at lower dosing than historically used."( Comparisons of Varying Dosages of Chloral Hydrate-Hydroxyzine with and without Meperidine for Managing Challenging Pediatric Dental Behavior: A Retrospective study of 35 years of Sedation Experiences.
Nathan, JE, 2022
)
0.97
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (5)

RoleDescription
H1-receptor antagonistH1-receptor antagonists are the drugs that selectively bind to but do not activate histamine H1 receptors, thereby blocking the actions of endogenous histamine.
anxiolytic drugAnxiolytic drugs are agents that alleviate anxiety, tension, and anxiety disorders, promote sedation, and have a calming effect without affecting clarity of consciousness or neurologic conditions.
dermatologic drugA drug used to treat or prevent skin disorders or for the routine care of skin.
antipruritic drugA drug, usually applied topically, that relieves pruritus (itching).
anticoronaviral agentAny antiviral agent which inhibits the activity of coronaviruses.
[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
N-alkylpiperazine
hydroxyetherAny ether carrying a hydroxy group at unspecified position.
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
Hydroxyzine H1-Antihistamine Action87

Protein Targets (29)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
LuciferasePhotinus pyralis (common eastern firefly)Potency27.54040.007215.758889.3584AID1224835
RAR-related orphan receptor gammaMus musculus (house mouse)Potency2.11320.006038.004119,952.5996AID1159521
TDP1 proteinHomo sapiens (human)Potency31.67680.000811.382244.6684AID686978; AID686979
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency23.91450.000214.376460.0339AID720691
retinoid X nuclear receptor alphaHomo sapiens (human)Potency10.90720.000817.505159.3239AID1159527; AID1159531
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency23.95660.001530.607315,848.9004AID1224841; AID1224848; AID1224849; AID1259401; AID1259403
estrogen nuclear receptor alphaHomo sapiens (human)Potency0.53540.000229.305416,493.5996AID743075
cytochrome P450 2D6Homo sapiens (human)Potency0.43650.00108.379861.1304AID1645840
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency11.88230.001019.414170.9645AID743191
Histone H2A.xCricetulus griseus (Chinese hamster)Potency55.19650.039147.5451146.8240AID1224845
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency24.17390.000323.4451159.6830AID743065; AID743067
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency31.62280.009610.525035.4813AID1479145
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Bile salt export pumpHomo sapiens (human)IC50 (µMol)72.91000.11007.190310.0000AID1449628
D(2) dopamine receptorHomo sapiens (human)Ki0.37800.00000.651810.0000AID1380690
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)Ki0.17500.00010.949010.0000AID1380686; AID1380689
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)Ki0.17500.00000.575110.0000AID1380686; AID1380689
5-hydroxytryptamine receptor 2AHomo sapiens (human)Ki0.05000.00000.385510.0000AID1380689
Histamine H1 receptorHomo sapiens (human)Ki0.00200.00000.511010.0000AID1380688
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)Ki0.17500.00000.965010.0000AID1380686; AID1380689
Histamine H4 receptorHomo sapiens (human)Ki10.00000.00060.478710.0000AID1798265
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Spike glycoproteinBetacoronavirus England 1EC50 (µMol)14.40000.00304.57559.8200AID1804127
Replicase polyprotein 1abBetacoronavirus England 1EC50 (µMol)14.40000.00304.57559.8200AID1804127
Transmembrane protease serine 2Homo sapiens (human)EC50 (µMol)14.40000.00304.51689.8200AID1804127
Procathepsin LHomo sapiens (human)EC50 (µMol)14.40000.00304.48749.8200AID1804127
Replicase polyprotein 1aSevere acute respiratory syndrome-related coronavirusEC50 (µMol)14.40000.00304.61369.8200AID1804127
Replicase polyprotein 1abHuman coronavirus 229EEC50 (µMol)14.40000.00304.61369.8200AID1804127
Replicase polyprotein 1abSevere acute respiratory syndrome-related coronavirusEC50 (µMol)14.40000.00304.45549.8200AID1804127
Replicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2EC50 (µMol)14.40000.00304.11059.8200AID1804127
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusEC50 (µMol)14.40000.00304.57559.8200AID1804127
Angiotensin-converting enzyme 2 Homo sapiens (human)EC50 (µMol)14.40000.00304.57559.8200AID1804127
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (206)

Processvia Protein(s)Taxonomy
viral translationTransmembrane protease serine 2Homo sapiens (human)
proteolysisTransmembrane protease serine 2Homo sapiens (human)
protein autoprocessingTransmembrane protease serine 2Homo sapiens (human)
positive regulation of viral entry into host cellTransmembrane protease serine 2Homo 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)
adaptive immune responseProcathepsin LHomo sapiens (human)
proteolysisProcathepsin LHomo sapiens (human)
protein autoprocessingProcathepsin LHomo sapiens (human)
fusion of virus membrane with host plasma membraneProcathepsin LHomo sapiens (human)
receptor-mediated endocytosis of virus by host cellProcathepsin LHomo sapiens (human)
antigen processing and presentationProcathepsin LHomo sapiens (human)
antigen processing and presentation of exogenous peptide antigen via MHC class IIProcathepsin LHomo sapiens (human)
collagen catabolic processProcathepsin LHomo sapiens (human)
zymogen activationProcathepsin LHomo sapiens (human)
enkephalin processingProcathepsin LHomo sapiens (human)
fusion of virus membrane with host endosome membraneProcathepsin LHomo sapiens (human)
CD4-positive, alpha-beta T cell lineage commitmentProcathepsin LHomo sapiens (human)
symbiont entry into host cellProcathepsin LHomo sapiens (human)
antigen processing and presentation of peptide antigenProcathepsin LHomo sapiens (human)
proteolysis involved in protein catabolic processProcathepsin LHomo sapiens (human)
elastin catabolic processProcathepsin LHomo sapiens (human)
macrophage apoptotic processProcathepsin LHomo sapiens (human)
cellular response to thyroid hormone stimulusProcathepsin LHomo sapiens (human)
positive regulation of apoptotic signaling pathwayProcathepsin LHomo sapiens (human)
positive regulation of peptidase activityProcathepsin LHomo sapiens (human)
immune responseProcathepsin LHomo sapiens (human)
symbiont-mediated perturbation of host ubiquitin-like protein modificationReplicase polyprotein 1aSevere acute respiratory syndrome-related coronavirus
symbiont-mediated perturbation of host ubiquitin-like protein modificationReplicase polyprotein 1abSevere acute respiratory syndrome-related coronavirus
phospholipase C-activating dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
temperature homeostasisD(2) dopamine receptorHomo sapiens (human)
response to hypoxiaD(2) dopamine receptorHomo sapiens (human)
negative regulation of protein phosphorylationD(2) dopamine receptorHomo sapiens (human)
response to amphetamineD(2) dopamine receptorHomo sapiens (human)
nervous system process involved in regulation of systemic arterial blood pressureD(2) dopamine receptorHomo sapiens (human)
regulation of heart rateD(2) dopamine receptorHomo sapiens (human)
regulation of sodium ion transportD(2) dopamine receptorHomo sapiens (human)
G protein-coupled receptor internalizationD(2) dopamine receptorHomo sapiens (human)
positive regulation of neuroblast proliferationD(2) dopamine receptorHomo sapiens (human)
positive regulation of receptor internalizationD(2) dopamine receptorHomo sapiens (human)
autophagyD(2) dopamine receptorHomo sapiens (human)
adenylate cyclase-inhibiting dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
neuron-neuron synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
neuroblast proliferationD(2) dopamine receptorHomo sapiens (human)
axonogenesisD(2) dopamine receptorHomo sapiens (human)
synapse assemblyD(2) dopamine receptorHomo sapiens (human)
sensory perception of smellD(2) dopamine receptorHomo sapiens (human)
long-term memoryD(2) dopamine receptorHomo sapiens (human)
grooming behaviorD(2) dopamine receptorHomo sapiens (human)
locomotory behaviorD(2) dopamine receptorHomo sapiens (human)
adult walking behaviorD(2) dopamine receptorHomo sapiens (human)
protein localizationD(2) dopamine receptorHomo sapiens (human)
negative regulation of cell population proliferationD(2) dopamine receptorHomo sapiens (human)
associative learningD(2) dopamine receptorHomo sapiens (human)
visual learningD(2) dopamine receptorHomo sapiens (human)
response to xenobiotic stimulusD(2) dopamine receptorHomo sapiens (human)
response to light stimulusD(2) dopamine receptorHomo sapiens (human)
response to toxic substanceD(2) dopamine receptorHomo sapiens (human)
response to iron ionD(2) dopamine receptorHomo sapiens (human)
response to inactivityD(2) dopamine receptorHomo sapiens (human)
Wnt signaling pathwayD(2) dopamine receptorHomo sapiens (human)
striatum developmentD(2) dopamine receptorHomo sapiens (human)
orbitofrontal cortex developmentD(2) dopamine receptorHomo sapiens (human)
cerebral cortex GABAergic interneuron migrationD(2) dopamine receptorHomo sapiens (human)
adenohypophysis developmentD(2) dopamine receptorHomo sapiens (human)
negative regulation of cell migrationD(2) dopamine receptorHomo sapiens (human)
peristalsisD(2) dopamine receptorHomo sapiens (human)
auditory behaviorD(2) dopamine receptorHomo sapiens (human)
regulation of synaptic transmission, GABAergicD(2) dopamine receptorHomo sapiens (human)
positive regulation of cytokinesisD(2) dopamine receptorHomo sapiens (human)
circadian regulation of gene expressionD(2) dopamine receptorHomo sapiens (human)
negative regulation of dopamine secretionD(2) dopamine receptorHomo sapiens (human)
response to histamineD(2) dopamine receptorHomo sapiens (human)
response to nicotineD(2) dopamine receptorHomo sapiens (human)
positive regulation of urine volumeD(2) dopamine receptorHomo sapiens (human)
positive regulation of renal sodium excretionD(2) dopamine receptorHomo sapiens (human)
positive regulation of multicellular organism growthD(2) dopamine receptorHomo sapiens (human)
response to cocaineD(2) dopamine receptorHomo sapiens (human)
negative regulation of circadian sleep/wake cycle, sleepD(2) dopamine receptorHomo sapiens (human)
dopamine metabolic processD(2) dopamine receptorHomo sapiens (human)
drinking behaviorD(2) dopamine receptorHomo sapiens (human)
regulation of potassium ion transportD(2) dopamine receptorHomo sapiens (human)
response to morphineD(2) dopamine receptorHomo sapiens (human)
pigmentationD(2) dopamine receptorHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transductionD(2) dopamine receptorHomo sapiens (human)
positive regulation of G protein-coupled receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
negative regulation of blood pressureD(2) dopamine receptorHomo sapiens (human)
negative regulation of innate immune responseD(2) dopamine receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IID(2) dopamine receptorHomo sapiens (human)
negative regulation of insulin secretionD(2) dopamine receptorHomo sapiens (human)
acid secretionD(2) dopamine receptorHomo sapiens (human)
behavioral response to cocaineD(2) dopamine receptorHomo sapiens (human)
behavioral response to ethanolD(2) dopamine receptorHomo sapiens (human)
regulation of long-term neuronal synaptic plasticityD(2) dopamine receptorHomo sapiens (human)
response to axon injuryD(2) dopamine receptorHomo sapiens (human)
branching morphogenesis of a nerveD(2) dopamine receptorHomo sapiens (human)
arachidonic acid secretionD(2) dopamine receptorHomo sapiens (human)
epithelial cell proliferationD(2) dopamine receptorHomo sapiens (human)
negative regulation of epithelial cell proliferationD(2) dopamine receptorHomo sapiens (human)
negative regulation of protein secretionD(2) dopamine receptorHomo sapiens (human)
release of sequestered calcium ion into cytosolD(2) dopamine receptorHomo sapiens (human)
dopamine uptake involved in synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
regulation of dopamine uptake involved in synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
positive regulation of dopamine uptake involved in synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
regulation of synapse structural plasticityD(2) dopamine receptorHomo sapiens (human)
negative regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionD(2) dopamine receptorHomo sapiens (human)
negative regulation of synaptic transmission, glutamatergicD(2) dopamine receptorHomo sapiens (human)
excitatory postsynaptic potentialD(2) dopamine receptorHomo sapiens (human)
positive regulation of growth hormone secretionD(2) dopamine receptorHomo sapiens (human)
prepulse inhibitionD(2) dopamine receptorHomo sapiens (human)
negative regulation of dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeD(2) dopamine receptorHomo sapiens (human)
regulation of locomotion involved in locomotory behaviorD(2) dopamine receptorHomo sapiens (human)
postsynaptic modulation of chemical synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
negative regulation of cellular response to hypoxiaD(2) dopamine receptorHomo sapiens (human)
positive regulation of glial cell-derived neurotrophic factor productionD(2) dopamine receptorHomo sapiens (human)
positive regulation of long-term synaptic potentiationD(2) dopamine receptorHomo sapiens (human)
hyaloid vascular plexus regressionD(2) dopamine receptorHomo sapiens (human)
negative regulation of neuron migrationD(2) dopamine receptorHomo sapiens (human)
negative regulation of cytosolic calcium ion concentrationD(2) dopamine receptorHomo sapiens (human)
regulation of dopamine secretionD(2) dopamine receptorHomo sapiens (human)
negative regulation of adenylate cyclase activityD(2) dopamine receptorHomo sapiens (human)
phospholipase C-activating dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
negative regulation of voltage-gated calcium channel activityD(2) dopamine receptorHomo sapiens (human)
positive regulation of MAPK cascadeD(2) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
temperature homeostasis5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of cytokine production involved in immune response5-hydroxytryptamine receptor 2AHomo sapiens (human)
glycolytic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
intracellular calcium ion homeostasis5-hydroxytryptamine receptor 2AHomo sapiens (human)
activation of phospholipase C activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of cytosolic calcium ion concentration5-hydroxytryptamine receptor 2AHomo sapiens (human)
memory5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of cell population proliferation5-hydroxytryptamine receptor 2AHomo sapiens (human)
response to xenobiotic stimulus5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
regulation of dopamine secretion5-hydroxytryptamine receptor 2AHomo sapiens (human)
artery smooth muscle contraction5-hydroxytryptamine receptor 2AHomo sapiens (human)
urinary bladder smooth muscle contraction5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of heat generation5-hydroxytryptamine receptor 2AHomo sapiens (human)
negative regulation of potassium ion transport5-hydroxytryptamine receptor 2AHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transduction5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of neuron apoptotic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein localization to cytoskeleton5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of fat cell differentiation5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of glycolytic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of vasoconstriction5-hydroxytryptamine receptor 2AHomo sapiens (human)
symbiont entry into host cell5-hydroxytryptamine receptor 2AHomo sapiens (human)
sensitization5-hydroxytryptamine receptor 2AHomo sapiens (human)
behavioral response to cocaine5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of inflammatory response5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylation5-hydroxytryptamine receptor 2AHomo sapiens (human)
detection of temperature stimulus involved in sensory perception of pain5-hydroxytryptamine receptor 2AHomo sapiens (human)
detection of mechanical stimulus involved in sensory perception of pain5-hydroxytryptamine receptor 2AHomo sapiens (human)
release of sequestered calcium ion into cytosol5-hydroxytryptamine receptor 2AHomo sapiens (human)
negative regulation of synaptic transmission, glutamatergic5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 2AHomo sapiens (human)
presynaptic modulation of chemical synaptic transmission5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of execution phase of apoptosis5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of platelet aggregation5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of DNA biosynthetic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 2AHomo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway5-hydroxytryptamine receptor 2AHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 2AHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 2AHomo 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)
negative regulation of signaling receptor activityAngiotensin-converting enzyme 2 Homo sapiens (human)
symbiont entry into host cellAngiotensin-converting enzyme 2 Homo sapiens (human)
regulation of cytokine productionAngiotensin-converting enzyme 2 Homo sapiens (human)
angiotensin maturationAngiotensin-converting enzyme 2 Homo sapiens (human)
angiotensin-mediated drinking behaviorAngiotensin-converting enzyme 2 Homo sapiens (human)
regulation of systemic arterial blood pressure by renin-angiotensinAngiotensin-converting enzyme 2 Homo sapiens (human)
tryptophan transportAngiotensin-converting enzyme 2 Homo sapiens (human)
viral life cycleAngiotensin-converting enzyme 2 Homo sapiens (human)
receptor-mediated endocytosis of virus by host cellAngiotensin-converting enzyme 2 Homo sapiens (human)
regulation of vasoconstrictionAngiotensin-converting enzyme 2 Homo sapiens (human)
regulation of transmembrane transporter activityAngiotensin-converting enzyme 2 Homo sapiens (human)
regulation of cell population proliferationAngiotensin-converting enzyme 2 Homo sapiens (human)
symbiont entry into host cellAngiotensin-converting enzyme 2 Homo sapiens (human)
receptor-mediated virion attachment to host cellAngiotensin-converting enzyme 2 Homo sapiens (human)
negative regulation of smooth muscle cell proliferationAngiotensin-converting enzyme 2 Homo sapiens (human)
regulation of inflammatory responseAngiotensin-converting enzyme 2 Homo sapiens (human)
positive regulation of amino acid transportAngiotensin-converting enzyme 2 Homo sapiens (human)
maternal process involved in female pregnancyAngiotensin-converting enzyme 2 Homo sapiens (human)
positive regulation of cardiac muscle contractionAngiotensin-converting enzyme 2 Homo sapiens (human)
membrane fusionAngiotensin-converting enzyme 2 Homo sapiens (human)
negative regulation of ERK1 and ERK2 cascadeAngiotensin-converting enzyme 2 Homo sapiens (human)
blood vessel diameter maintenanceAngiotensin-converting enzyme 2 Homo sapiens (human)
entry receptor-mediated virion attachment to host cellAngiotensin-converting enzyme 2 Homo sapiens (human)
positive regulation of gap junction assemblyAngiotensin-converting enzyme 2 Homo sapiens (human)
regulation of cardiac conductionAngiotensin-converting enzyme 2 Homo sapiens (human)
positive regulation of L-proline import across plasma membraneAngiotensin-converting enzyme 2 Homo sapiens (human)
positive regulation of reactive oxygen species metabolic processAngiotensin-converting enzyme 2 Homo sapiens (human)
inflammatory responseHistamine H4 receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationHistamine H4 receptorHomo sapiens (human)
biological_processHistamine H4 receptorHomo sapiens (human)
regulation of MAPK cascadeHistamine H4 receptorHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayHistamine H4 receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayHistamine H4 receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerHistamine H4 receptorHomo sapiens (human)
chemical synaptic transmissionHistamine H4 receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (53)

Processvia Protein(s)Taxonomy
serine-type endopeptidase activityTransmembrane protease serine 2Homo sapiens (human)
protein bindingTransmembrane protease serine 2Homo sapiens (human)
serine-type peptidase activityTransmembrane protease serine 2Homo 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)
fibronectin bindingProcathepsin LHomo sapiens (human)
cysteine-type endopeptidase activityProcathepsin LHomo sapiens (human)
protein bindingProcathepsin LHomo sapiens (human)
collagen bindingProcathepsin LHomo sapiens (human)
cysteine-type peptidase activityProcathepsin LHomo sapiens (human)
histone bindingProcathepsin LHomo sapiens (human)
proteoglycan bindingProcathepsin LHomo sapiens (human)
serpin family protein bindingProcathepsin LHomo sapiens (human)
cysteine-type endopeptidase activator activity involved in apoptotic processProcathepsin LHomo sapiens (human)
RNA-dependent RNA polymerase activityReplicase polyprotein 1aSevere acute respiratory syndrome-related coronavirus
cysteine-type endopeptidase activityReplicase polyprotein 1aSevere acute respiratory syndrome-related coronavirus
K63-linked deubiquitinase activityReplicase polyprotein 1aSevere acute respiratory syndrome-related coronavirus
K48-linked deubiquitinase activityReplicase polyprotein 1aSevere acute respiratory syndrome-related coronavirus
3'-5'-RNA exonuclease activityReplicase polyprotein 1abSevere acute respiratory syndrome-related coronavirus
RNA-dependent RNA polymerase activityReplicase polyprotein 1abSevere acute respiratory syndrome-related coronavirus
cysteine-type endopeptidase activityReplicase polyprotein 1abSevere acute respiratory syndrome-related coronavirus
mRNA 5'-cap (guanine-N7-)-methyltransferase activityReplicase polyprotein 1abSevere acute respiratory syndrome-related coronavirus
mRNA (nucleoside-2'-O-)-methyltransferase activityReplicase polyprotein 1abSevere acute respiratory syndrome-related coronavirus
5'-3' RNA helicase activityReplicase polyprotein 1abSevere acute respiratory syndrome-related coronavirus
K63-linked deubiquitinase activityReplicase polyprotein 1abSevere acute respiratory syndrome-related coronavirus
K48-linked deubiquitinase activityReplicase polyprotein 1abSevere acute respiratory syndrome-related coronavirus
3'-5'-RNA exonuclease activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
RNA-dependent RNA polymerase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
cysteine-type endopeptidase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
mRNA 5'-cap (guanine-N7-)-methyltransferase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
mRNA (nucleoside-2'-O-)-methyltransferase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
mRNA guanylyltransferase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
RNA endonuclease activity, producing 3'-phosphomonoestersReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
ISG15-specific peptidase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
5'-3' RNA helicase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
protein guanylyltransferase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
dopamine neurotransmitter receptor activity, coupled via Gi/GoD(2) dopamine receptorHomo sapiens (human)
G-protein alpha-subunit bindingD(2) dopamine receptorHomo sapiens (human)
protein bindingD(2) dopamine receptorHomo sapiens (human)
heterotrimeric G-protein bindingD(2) dopamine receptorHomo sapiens (human)
dopamine bindingD(2) dopamine receptorHomo sapiens (human)
ionotropic glutamate receptor bindingD(2) dopamine receptorHomo sapiens (human)
identical protein bindingD(2) dopamine receptorHomo sapiens (human)
heterocyclic compound bindingD(2) dopamine receptorHomo sapiens (human)
G protein-coupled receptor activityD(2) dopamine receptorHomo sapiens (human)
Gq/11-coupled serotonin receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
virus receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein tyrosine kinase activator activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
identical protein binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein-containing complex binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 2AHomo 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)
virus receptor activityAngiotensin-converting enzyme 2 Homo sapiens (human)
endopeptidase activityAngiotensin-converting enzyme 2 Homo sapiens (human)
carboxypeptidase activityAngiotensin-converting enzyme 2 Homo sapiens (human)
metallocarboxypeptidase activityAngiotensin-converting enzyme 2 Homo sapiens (human)
protein bindingAngiotensin-converting enzyme 2 Homo sapiens (human)
metallopeptidase activityAngiotensin-converting enzyme 2 Homo sapiens (human)
peptidyl-dipeptidase activityAngiotensin-converting enzyme 2 Homo sapiens (human)
zinc ion bindingAngiotensin-converting enzyme 2 Homo sapiens (human)
identical protein bindingAngiotensin-converting enzyme 2 Homo sapiens (human)
histamine receptor activityHistamine H4 receptorHomo sapiens (human)
G protein-coupled serotonin receptor activityHistamine H4 receptorHomo sapiens (human)
G protein-coupled acetylcholine receptor activityHistamine H4 receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (59)

Processvia Protein(s)Taxonomy
extracellular regionTransmembrane protease serine 2Homo sapiens (human)
nucleoplasmTransmembrane protease serine 2Homo sapiens (human)
plasma membraneTransmembrane protease serine 2Homo sapiens (human)
extracellular exosomeTransmembrane protease serine 2Homo 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)
extracellular regionProcathepsin LHomo sapiens (human)
extracellular spaceProcathepsin LHomo sapiens (human)
nucleusProcathepsin LHomo sapiens (human)
lysosomeProcathepsin LHomo sapiens (human)
multivesicular bodyProcathepsin LHomo sapiens (human)
Golgi apparatusProcathepsin LHomo sapiens (human)
plasma membraneProcathepsin LHomo sapiens (human)
apical plasma membraneProcathepsin LHomo sapiens (human)
endolysosome lumenProcathepsin LHomo sapiens (human)
chromaffin granuleProcathepsin LHomo sapiens (human)
lysosomal lumenProcathepsin LHomo sapiens (human)
intracellular membrane-bounded organelleProcathepsin LHomo sapiens (human)
collagen-containing extracellular matrixProcathepsin LHomo sapiens (human)
extracellular exosomeProcathepsin LHomo sapiens (human)
endocytic vesicle lumenProcathepsin LHomo sapiens (human)
extracellular spaceProcathepsin LHomo sapiens (human)
lysosomeProcathepsin LHomo sapiens (human)
double membrane vesicle viral factory outer membraneReplicase polyprotein 1aSevere acute respiratory syndrome-related coronavirus
double membrane vesicle viral factory outer membraneReplicase polyprotein 1abSevere acute respiratory syndrome-related coronavirus
double membrane vesicle viral factory outer membraneReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
Golgi membraneD(2) dopamine receptorHomo sapiens (human)
acrosomal vesicleD(2) dopamine receptorHomo sapiens (human)
plasma membraneD(2) dopamine receptorHomo sapiens (human)
ciliumD(2) dopamine receptorHomo sapiens (human)
lateral plasma membraneD(2) dopamine receptorHomo sapiens (human)
endocytic vesicleD(2) dopamine receptorHomo sapiens (human)
axonD(2) dopamine receptorHomo sapiens (human)
dendriteD(2) dopamine receptorHomo sapiens (human)
synaptic vesicle membraneD(2) dopamine receptorHomo sapiens (human)
sperm flagellumD(2) dopamine receptorHomo sapiens (human)
dendritic spineD(2) dopamine receptorHomo sapiens (human)
perikaryonD(2) dopamine receptorHomo sapiens (human)
axon terminusD(2) dopamine receptorHomo sapiens (human)
postsynaptic membraneD(2) dopamine receptorHomo sapiens (human)
ciliary membraneD(2) dopamine receptorHomo sapiens (human)
non-motile ciliumD(2) dopamine receptorHomo sapiens (human)
dopaminergic synapseD(2) dopamine receptorHomo sapiens (human)
GABA-ergic synapseD(2) dopamine receptorHomo sapiens (human)
G protein-coupled receptor complexD(2) dopamine receptorHomo sapiens (human)
glutamatergic synapseD(2) dopamine receptorHomo sapiens (human)
presynaptic membraneD(2) dopamine receptorHomo sapiens (human)
plasma membraneD(2) dopamine receptorHomo sapiens (human)
neurofilament5-hydroxytryptamine receptor 2AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
caveola5-hydroxytryptamine receptor 2AHomo sapiens (human)
axon5-hydroxytryptamine receptor 2AHomo sapiens (human)
cytoplasmic vesicle5-hydroxytryptamine receptor 2AHomo sapiens (human)
presynaptic membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
neuronal cell body5-hydroxytryptamine receptor 2AHomo sapiens (human)
dendritic shaft5-hydroxytryptamine receptor 2AHomo sapiens (human)
postsynaptic membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
cell body fiber5-hydroxytryptamine receptor 2AHomo sapiens (human)
glutamatergic synapse5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 2AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 2AHomo 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)
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
plasma membraneAngiotensin-converting enzyme 2 Homo sapiens (human)
extracellular regionAngiotensin-converting enzyme 2 Homo sapiens (human)
extracellular spaceAngiotensin-converting enzyme 2 Homo sapiens (human)
endoplasmic reticulum lumenAngiotensin-converting enzyme 2 Homo sapiens (human)
plasma membraneAngiotensin-converting enzyme 2 Homo sapiens (human)
ciliumAngiotensin-converting enzyme 2 Homo sapiens (human)
cell surfaceAngiotensin-converting enzyme 2 Homo sapiens (human)
membraneAngiotensin-converting enzyme 2 Homo sapiens (human)
apical plasma membraneAngiotensin-converting enzyme 2 Homo sapiens (human)
endocytic vesicle membraneAngiotensin-converting enzyme 2 Homo sapiens (human)
brush border membraneAngiotensin-converting enzyme 2 Homo sapiens (human)
membrane raftAngiotensin-converting enzyme 2 Homo sapiens (human)
extracellular exosomeAngiotensin-converting enzyme 2 Homo sapiens (human)
extracellular spaceAngiotensin-converting enzyme 2 Homo sapiens (human)
plasma membraneHistamine H4 receptorHomo sapiens (human)
plasma membraneHistamine H4 receptorHomo sapiens (human)
dendriteHistamine H4 receptorHomo sapiens (human)
synapseHistamine H4 receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (131)

Assay IDTitleYearJournalArticle
AID1604321Antiparasitic activity against Toxoplasma gondii2019European journal of medicinal chemistry, Dec-01, Volume: 183Recent progress on anti-Toxoplasma drugs discovery: Design, synthesis and screening.
AID588216FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
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.
AID1380690Binding affinity to D2 receptor (unknown origin)
AID298031Lipophilicity, log D at pH7.42007Journal of medicinal chemistry, Sep-20, Volume: 50, Issue:19
High-throughput screening of drug-brain tissue binding and in silico prediction for assessment of central nervous system drug delivery.
AID1380688Binding affinity to histamine H1 receptor (unknown origin)
AID496830Antimicrobial activity against Leishmania major2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID496829Antimicrobial activity against Leishmania infantum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
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).
AID395327Dissociation constant, pKa by capillary electrophoresis2009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs.
AID496831Antimicrobial activity against Cryptosporidium parvum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
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).
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).
AID588214FDA HLAED, liver enzyme composite activity2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID588218FDA HLAED, lactate dehydrogenase (LDH) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1449628Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method2012Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12
Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.
AID588217FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID588219FDA HLAED, gamma-glutamyl transferase (GGT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID678717Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-benzyloxyquinoline as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID540237Phospholipidosis-positive literature compound observed in rat
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.
AID1636410Drug activation in human Hep3B cells assessed as human CYP3A4-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 63.5 uM pre-incubated with BSO for 18 hrs followed by incubation with compound for 3 hrs in presence of N2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.
AID678713Inhibition of human CYP2C9 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-methoxy-4-trifluoromethylcoumarin-3-acetic acid as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID496828Antimicrobial activity against Leishmania donovani2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
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).
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.
AID678722Covalent binding affinity to human liver microsomes assessed per mg of protein at 10 uM after 60 mins presence of NADPH2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID496832Antimicrobial activity against Trypanosoma brucei rhodesiense2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
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).
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.
AID22294delta logDoct -dod7.41998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Molecular properties and pharmacokinetic behavior of cetirizine, a zwitterionic H1-receptor antagonist.
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).
AID1380689Binding affinity to 5-HT2A receptor (unknown origin)
AID1215122Percentage unbound in solid supported porcine brain membrane vesicles at 5 uM by TRANSIL assay2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Brain tissue binding of drugs: evaluation and validation of solid supported porcine brain membrane vesicles (TRANSIL) as a novel high-throughput method.
AID588208Literature-mined public compounds from Lowe et al phospholipidosis modelling dataset2010Molecular pharmaceutics, Oct-04, Volume: 7, Issue:5
Predicting phospholipidosis using machine learning.
AID678715Inhibition of human CYP2D6 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 4-methylaminoethyl-7-methoxycoumarin as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID23732Lipophilicity parameter log Pdod N1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Molecular properties and pharmacokinetic behavior of cetirizine, a zwitterionic H1-receptor antagonist.
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.
AID1283268Inhibition of delta 8-7 isomerase in Dhcr7-deficient mouse Neuro2a cells assessed as decrease in 7-DHC levels at 1 uM by LC-MS/GC-MS analysis2016Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
The Effect of Small Molecules on Sterol Homeostasis: Measuring 7-Dehydrocholesterol in Dhcr7-Deficient Neuro2a Cells and Human Fibroblasts.
AID23739Lipophilicity parameter log Poct C1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Molecular properties and pharmacokinetic behavior of cetirizine, a zwitterionic H1-receptor antagonist.
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).
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.
AID1215121Fraction unbound in Wistar rat brain homogenate at 5 uM after 5 hrs by equilibrium dialysis method2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Brain tissue binding of drugs: evaluation and validation of solid supported porcine brain membrane vesicles (TRANSIL) as a novel high-throughput method.
AID1380686Displacement of [3H]prazosin from rat cerebral cortex adrenergic receptor alpha1 by liquid scintillation counting method
AID1280179Cytotoxicity against human Huh7.5.1 cells assessed as ATP level by luminescence analysis2016Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
Discovery, Optimization, and Characterization of Novel Chlorcyclizine Derivatives for the Treatment of Hepatitis C Virus Infection.
AID588215FDA HLAED, alkaline phosphatase increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID23740Lipophilicity parameter log Poct N1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Molecular properties and pharmacokinetic behavior of cetirizine, a zwitterionic H1-receptor antagonist.
AID496827Antimicrobial activity against Leishmania amazonensis2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
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.
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).
AID1280180Selectivity index, ratio of CC50 for human Huh7.5.1 cells infected with HCV JFH-1 virus to EC50 for HCV JFH-1 virus2016Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
Discovery, Optimization, and Characterization of Novel Chlorcyclizine Derivatives for the Treatment of Hepatitis C Virus Infection.
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).
AID26527Partition coefficient (logD7.4)1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Molecular properties and pharmacokinetic behavior of cetirizine, a zwitterionic H1-receptor antagonist.
AID678714Inhibition of human CYP2C19 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 3-butyryl-7-methoxycoumarin as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID395324Lipophilicity, log D at pH 7.4 by liquid chromatography2009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs.
AID496819Antimicrobial activity against Plasmodium falciparum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID496824Antimicrobial activity against Toxoplasma gondii2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
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.
AID496826Antimicrobial activity against Entamoeba histolytica2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
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.
AID1280178Antiviral activity against HCV JFH-1 infected in Huh7.5.1 cells after 48 hrs by luciferase reporter gene assay2016Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
Discovery, Optimization, and Characterization of Novel Chlorcyclizine Derivatives for the Treatment of Hepatitis C Virus Infection.
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).
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.
AID678716Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using diethoxyfluorescein as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID22296Delta logPoct -dod1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Molecular properties and pharmacokinetic behavior of cetirizine, a zwitterionic H1-receptor antagonist.
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).
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).
AID603955In-vivo blood to lung partition coefficients of the compound, logP(lung) in rat2008European journal of medicinal chemistry, Mar, Volume: 43, Issue:3
Air to lung partition coefficients for volatile organic compounds and blood to lung partition coefficients for volatile organic compounds and drugs.
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).
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.
AID1215127Ratio of fraction unbound in solid supported porcine brain membrane vesicles at 5 uM by TRANSIL assay to fraction unbound in Wistar rat brain homogenate at 5 uM after 5 hrs by equilibrium dialysis method2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Brain tissue binding of drugs: evaluation and validation of solid supported porcine brain membrane vesicles (TRANSIL) as a novel high-throughput method.
AID643383Induction of phospholipidosis in bovine corneal fibroblasts assessed as lamellar inclusion bodies after 72 hrs by light microscopy2012Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1
In silico assay for assessing phospholipidosis potential of small druglike molecules: training, validation, and refinement using several data sets.
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).
AID678721Metabolic stability in human liver microsomes assessed as GSH adduct formation at 100 uM after 90 mins by HPLC-MS analysis2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
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).
AID26524Partition coefficient between dodecane and water (logDdod7.4)1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Molecular properties and pharmacokinetic behavior of cetirizine, a zwitterionic H1-receptor antagonist.
AID23939Lipophilicity parameter log Poct Z.1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Molecular properties and pharmacokinetic behavior of cetirizine, a zwitterionic H1-receptor antagonist.
AID19006Calculated membrane partition coefficient (Kmemb)2004Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7
Surface activity profiling of drugs applied to the prediction of blood-brain barrier permeability.
AID298032Acid dissociation constant, pKa of the compound2007Journal of medicinal chemistry, Sep-20, Volume: 50, Issue:19
High-throughput screening of drug-brain tissue binding and in silico prediction for assessment of central nervous system drug delivery.
AID588220Literature-mined public compounds from Kruhlak et al phospholipidosis modelling dataset2008Toxicology mechanisms and methods, , Volume: 18, Issue:2-3
Development of a phospholipidosis database and predictive quantitative structure-activity relationship (QSAR) models.
AID678712Inhibition of human CYP1A2 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using ethoxyresorufin as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID497005Antimicrobial activity against Pneumocystis carinii2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID496820Antimicrobial activity against Trypanosoma brucei2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID496825Antimicrobial activity against Leishmania mexicana2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID496823Antimicrobial activity against Trichomonas vaginalis2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID496817Antimicrobial activity against Trypanosoma cruzi2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1870222Inhibition of human ERG expressed in CHO cells at 1 uM by whole cell patch-clamp method
AID496821Antimicrobial activity against Leishmania2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID496818Antimicrobial activity against Trypanosoma brucei brucei2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID625278FDA Liver Toxicity Knowledge Base Benchmark Dataset (LTKB-BD) drugs of no concern for DILI2011Drug discovery today, Aug, Volume: 16, Issue:15-16
FDA-approved drug labeling for the study of drug-induced liver injury.
AID1636471Drug activation in human Hep3B cells assessed as human CYP2D6-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 274 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.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1508591NCATS Rat Liver Microsome Stability Profiling2020Scientific reports, 11-26, Volume: 10, Issue:1
Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1645848NCATS Kinetic Aqueous Solubility Profiling2019Bioorganic & medicinal chemistry, 07-15, Volume: 27, Issue:14
Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
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.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
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.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
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.
AID1804127No assay is provided from Article 10.1002/med.21724: \\The recent outbreaks of human coronaviruses: A medicinal chemistry perspective.\\2021Medicinal research reviews, 01, Volume: 41, Issue:1
The recent outbreaks of human coronaviruses: A medicinal chemistry perspective.
AID1798265H4R Radioligand Binding Assay from Article 10.1124/jpet.105.087965: \\Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist.\\2005The Journal of pharmacology and experimental therapeutics, Sep, Volume: 314, Issue:3
Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist.
AID1346037Human H1 receptor (Histamine receptors)2002Molecular pharmacology, Feb, Volume: 61, Issue:2
Binding characteristics of cetirizine and levocetirizine to human H(1) histamine receptors: contribution of Lys(191) and Thr(194).
AID1508612NCATS Parallel Artificial Membrane Permeability Assay (PAMPA) Profiling2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Highly predictive and interpretable models for PAMPA permeability.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (1,298)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990738 (56.86)18.7374
1990's201 (15.49)18.2507
2000's150 (11.56)29.6817
2010's163 (12.56)24.3611
2020's46 (3.54)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 138.58

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 Index138.58 (24.57)
Research Supply Index7.52 (2.92)
Research Growth Index4.40 (4.65)
Search Engine Demand Index265.41 (26.88)
Search Engine Supply Index2.02 (0.95)

This Compound (138.58)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials349 (23.44%)5.53%
Reviews87 (5.84%)6.00%
Case Studies170 (11.42%)4.05%
Observational2 (0.13%)0.25%
Other881 (59.17%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (22)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Prise en Charge Pharmacologique de l'anxiété et de la Douleur Chez Les Patients Qui Souffrent en Situation d'Urgence Traumatique pré-hospitalière : étude randomisée contrôlée en Double Aveugle [NCT01151696]Phase 4140 participants (Actual)Interventional2010-05-31Completed
Efficacy and Safety of 20 mg Levocetirizine and 15 mg Levocetirizine + 50 mg Bed-Time Hydroxyzine in Severe Chronic Urticaria in Adults: a Pilot, Randomized, Double-blind, Cross-over and Parallel, Active-controlled, Single-centre Study [NCT01250652]Phase 424 participants (Actual)Interventional2011-03-31Completed
Oral Sedation With/Without Nitrous Oxide in Pediatric Dental Patients [NCT03728894]Phase 330 participants (Actual)Interventional2018-11-17Completed
Hydroxyzine Effects on Meal-Related Anxiety in Underweight Adolescents and Young Adults Diagnosed With an Eating Disorder - A Pilot Study [NCT01372670]Phase 40 participants (Actual)Interventional2012-01-31Withdrawn(stopped due to Due to unforseen recruiting difficulties, the study was closed.)
Melatonin Versus Hydroxizin for Pre Operative Anxiety in Elderly Patients With Hip Fracture [NCT05224167]50 participants (Anticipated)Interventional2022-03-01Not yet recruiting
Evaluation of the Effect of Chloral Hydrate, Hydroxyzine and Melatonin Used as Sedative Drugs in EEG Recording in Children [NCT05492812]180 participants (Actual)Interventional2021-01-01Completed
Efficacy and Tolerability of Combination Varenicline With Hydroxyzine as a Potential Smoking Cessation Treatment [NCT04188106]Phase 426 participants (Actual)Interventional2019-06-17Completed
Hydroxyzine for the Prevention of Pruritus and Nausea Vomiting From Spinal Morphine in Patients Having Transabdominal Hysterectomy Under Combined Spinal-general Anesthesia: A Randomized Control Trial [NCT01055236]Phase 480 participants (Actual)Interventional2007-08-31Completed
Comparing Pediatric Oral Sedation Outcomes Using Midazolam and Hydroxyzine With and Without Meperidine [NCT04068948]Phase 437 participants (Actual)Interventional2019-06-25Completed
The Effect of Hydroxyzine and Alprazolam Premedication on Preoperative Anxiety and Patient Satisfaction [NCT04184141]Phase 490 participants (Anticipated)Interventional2019-12-01Not yet recruiting
RELIEF OF PSYCHOEMOTIONAL STRESS BEFORE REFRACTIVE LASER VISION CORRECTION SURGERY USING XENON SEDATION [NCT06080100]Early Phase 1140 participants (Anticipated)Interventional2023-11-01Not yet recruiting
Comparative Effects of Rupatadine 10 mg, Hydroxyzine 50 mg and Placebo on Actual Driving Performance [NCT00162786]Phase 420 participants Interventional2005-05-31Terminated
Examination of Palonosetron and Hydroxyzine Pre-treatment as a Possible Method to Reduce the Objective Signs of Experimentally-induced Acute Opioid Withdrawal in Humans: a Double-blind, Randomized, Placebo-controlled Crossover Study [NCT00661674]10 participants (Actual)Interventional2008-04-30Completed
Comparison Between the Effect of Oral Melatonin and Hydroxyzine for Preventing Preoperative Anxiety in Pediatric Patients Undergoing Adenotonsillectomy [NCT05680584]Phase 178 participants (Anticipated)Interventional2023-02-01Recruiting
Aprepitant Versus Hydroxyzine in Association With Cytoreductive Treatments for Patients With Myeloproliferative Neoplasia Suffering From Persistent Aquagenic Pruritus. [NCT03808805]Phase 380 participants (Anticipated)Interventional2019-04-16Recruiting
Interaction Between Drug and Placebo Effect:Randomized Placebo Controlled Trials May Not be Accurate in Determining Drug Effect Size [NCT01501591]480 participants (Actual)Interventional2012-11-30Completed
Study to Investigate the Effects of Levocetirizine and Hydroxyzine on Cognitive and Psychomotor Functioning During Simulated Diving at 2 Bar and 4 Bar in Professional Navy Divers [NCT01496911]Phase 424 participants (Actual)Interventional2012-04-30Completed
Hydroxyzine Dihydrochloride Premedication is a Necessity for Pediatric Patients Undergoing Strabismus Surgery; An Observational Clinical Trial Controlled With Midazolam [NCT03806270]45 participants (Actual)Observational [Patient Registry]2018-10-01Completed
Efficacy of Hydroxyzine Versus Treatment as Usual for Panic Disorder: An Eight-Week, Open Label, Pilot, Randomized Controlled Trial. [NCT05737511]Phase 480 participants (Anticipated)Interventional2023-12-30Not yet recruiting
Pharmacovigilance in Gerontopsychiatric Patients [NCT02374567]Phase 3407 participants (Actual)Interventional2015-01-31Terminated
[NCT01675986]Phase 2306 participants (Actual)InterventionalCompleted
Double-blind Randomized Clinical Trial to Compare Presurgery Anxiolysis in Children Treated With Hydroxyzine Versus Non-pharmacological Intervention (Distractoria Technique Clown) [NCT03324828]Phase 4170 participants (Actual)Interventional2017-11-01Terminated(stopped due to COVID-19)
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00661674 (2) [back to overview]OOWS Score
NCT00661674 (2) [back to overview]SOWS Score
NCT03806270 (5) [back to overview]Heart Rate-1
NCT03806270 (5) [back to overview]Heart Rate-2
NCT03806270 (5) [back to overview]Heart Rate-3
NCT03806270 (5) [back to overview]Number of Observed Oculocardiac Reflex(OCR)
NCT03806270 (5) [back to overview]Number of Orbital Muscles of the Participants With Different Considerations Taken With Respect to the Treatment of OCR
NCT04068948 (1) [back to overview]Number of Participants With Successful Sedation
NCT04188106 (5) [back to overview]Effects of Varenicline on Self-reported Smoking Reduction Prior to the Quit Date
NCT04188106 (5) [back to overview]Effects of Varenicline on Self-reported Smoking Reduction Prior to the Quit Date
NCT04188106 (5) [back to overview]Change in 10-item Perceived Stress Scale (PSS-10) Following Smoking Cessation (While Taking Arenicline and Hydroxyzine).
NCT04188106 (5) [back to overview]Changes in Anxiety Using the 6-item State-Trait Anxiety Inventory (STAI)
NCT04188106 (5) [back to overview]Changes in Depression Using the Patient Health Questionnaire (PHQ-9)

OOWS Score

"The OOWS is a 13-item instrument documenting physically observable signs of withdrawal, which are rated as present (1) or absent (0) during the observation period. Maximum score possible = 13, minimum score possible = 0. T=15 minutes post naloxone administration coordinates with T = 180 (min) for the entire study session.~OOWS scores at T=180 is the primary outcome measure of the study compared with baseline OOWS scores at T=-30 (30 minutes prior to study medication administration). Reported time frames are in relation to time past since administration of study medications.~Mean post-Naloxone OOWS scores (+/- SEM) were determined for pretreatment groups" (NCT00661674)
Timeframe: Change from baseline in OOWS score at 180 minutes (15 minutes post naloxone administration)

Interventionunits on a scale (OOWS Scale) (Mean)
Placebo3.5
Palonosetron1.0
Palonosetron + Hydroxyzine0

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SOWS Score

"The SOWS score is composed of 16 subjective symptoms rated on a scale of 0 to 4 (0=not at all, 4=extremely) based on what subjects were experiencing at the time of testing. 15 minutes post naloxone administration coordinates with T = 180 (min) for the entire study session.~The highest score possible (64) would indicate that the individual was experiencing every symptom of opioid withdrawal to the fullest extent possible while the lowest score (0) would indicate that the individual was not experiencing any symptoms of opioid withdrawal.~Mean post-naloxone SOWS scores (+/- SEM) were computed for pretreatment groups: Placebo, palonosetron, and palonosetron with hydroxyzine" (NCT00661674)
Timeframe: Change from baseline in SOWS score at 180 minutes (15 minutes post naloxone administration)

Interventionunits on a scale (SOWS Scale) (Mean)
Placebo6.0
Palonosetron4.0
Palonosetron + Hydroxyzine3.5

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Heart Rate-1

"The lowest heart rate observed from EKG monitorization at the time-out after the anesthesia induction, and just before the surgery starts. Heart rate-1 is a data, not an assessing change, which is recoded during the time-out. The time-out is when the patient's name, the procedure, the surgent name is repeated before the operation starts." (NCT03806270)
Timeframe: "1 minute, at the time out, through study completion an average of 6 months"

Interventionbeats per minute (Mean)
Midazolam114.4
Midazolam&Hydroxyzine dihydrochloride1/2125.8
Midazolam&Hydroxyzine Dihydrochloride122.3

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Heart Rate-2

The heart rate observed from EKG monitorization at the time operator warns the investigator just before the traction of the orbital muscle. Heart rate-2 is a data, not an assessing change, which is recorded during the operation at the time operator warns. The heart rate observed from EKG monitorization, before every orbital muscle traction at the time the operator's warning before traction. (NCT03806270)
Timeframe: 1 minute, at the strabismus surgery operation, through study completion an average of 6 months

Interventionbeats per minute (Mean)
Midazolam110.4
Midazolam&Hydroxyzine dihydrochloride1/2125.3
Midazolam&Hydroxyzine Dihydrochloride124.8

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Heart Rate-3

The lowest heart rate observed from EKG monitorization, after every orbital muscle traction within 120 seconds. Heart rate-3 is a data, not an assessing change, which is recorded within 120 seconds after traction applied. (NCT03806270)
Timeframe: within 120 seconds after the orbital muscle traction, at the strabismus surgery operation, through study completion an average of 6 months

Interventionbeats per minute (Mean)
Midazolam90.8
Midazolam&Hydroxyzine dihydrochloride1/2113.4
Midazolam&Hydroxyzine Dihydrochloride117.9

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Number of Observed Oculocardiac Reflex(OCR)

The OCR is a heartbeat anomaly(bradycardia, any arrhythmia, or cardiac arrest) associated with traction applied to the extraocular muscles during strabismus surgery. The specific criteria were as follows: the lowest heart rate observed within 120 seconds from EKG monitorization, after every orbital muscle traction, was less than 20% of the heart rate observed directly preceding traction of the orbital muscle. Additionally, any kind of arrhythmia or cardiac arrest occurrence within 120 seconds after orbital muscle traction was also defined as an OCR. (NCT03806270)
Timeframe: 2 minutes, at the strabismus surgery operation after recording Heart Rate-3, through study completion an average of 6 months

Interventionorbital muscles (Count of Units)
Midazolam15
Midazolam&Hydroxyzine dihydrochloride1/26
Midazolam&Hydroxyzine Dihydrochloride1

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Number of Orbital Muscles of the Participants With Different Considerations Taken With Respect to the Treatment of OCR

The investigator records every OCR treatment like; pausing surgery, atropin 20mcg/kg intravenous treatment or cardiac resuscitation. (NCT03806270)
Timeframe: within 5 minutes after defining the OCR occurrence, at the strabismus surgery operation, through study completion an average of 6 months

,,
Interventionnumber of orbital muscle/s, OCR occured (Number)
pausing surgeryatropin administrationcardiac resuscitation
Midazolam1320
Midazolam&Hydroxyzine Dihydrochloride100
Midazolam&Hydroxyzine dihydrochloride1/2600

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Number of Participants With Successful Sedation

Children's behavior during sedation is rated on the Houpt Behavior Rating Scale. A successful sedation is rated as Excellent, Very Good, or Good. A failed sedation is rated as Fair, Poor, or Aborted. (NCT04068948)
Timeframe: At completion of procedure

InterventionParticipants (Count of Participants)
Midazolam, Hydroxyzine, Meperidine11
Midazolam, Hydroxyzine9

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Effects of Varenicline on Self-reported Smoking Reduction Prior to the Quit Date

"Previous research has shown that abstinence at the end of treatment is strongly predicted by the extent to which smokers spontaneously reduce ad libitum smoking in the initial weeks of pharmacotherapy that is initiated before the quit-smoking date.~This measure will assess the extent of smoking reduction in participants during the initial seven days of treatment (prior to their planned quit date) - assessed via a self-report number of cigarettes per day. Data is recorded as a mean change." (NCT04188106)
Timeframe: 7 Days

InterventionCigs smoked per day (Mean)
Hydroxyzine and Varenicline -- Successful in Quitting Smoking-9.14
Hydroxyzine and Varenicline -- Unsuccessful in Quitting Smoking-5.53

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Effects of Varenicline on Self-reported Smoking Reduction Prior to the Quit Date

"Previous research has shown that abstinence at the end of treatment is strongly predicted by the extent to which smokers spontaneously reduce ad libitum smoking in the initial weeks of pharmacotherapy that is initiated before the quit-smoking date.~This measure will assess the extent of smoking reduction in participants during the initial seven days of treatment (prior to their planned quit date) - assessed via expired air carbon monoxide (CO). Data is recorded as a mean change." (NCT04188106)
Timeframe: 7 Days

InterventionCO in ppm (Mean)
Hydroxyzine and Varenicline -- Successful in Quitting Smoking-11.00
Hydroxyzine and Varenicline -- Unsuccessful in Quitting Smoking-2.12

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Change in 10-item Perceived Stress Scale (PSS-10) Following Smoking Cessation (While Taking Arenicline and Hydroxyzine).

"Stress levels in the last 30 days will be measured using the 10-item Perceived Stress Scale (PSS-10). The PSS-10 uses a 5-point scale (0 - never, 1 = almost never, 2 = once in a while, 3 = often, 4 = very often). Total scores range from 0 to 40.~Scores ranging from 0-13 would be considered low stress.~Scores ranging from 14-26 would be considered moderate stress.~Scores ranging from 27-40 would be considered high perceived stress." (NCT04188106)
Timeframe: Weeks 1, 2, 4, 8, 12

Interventionscore on a scale (Mean)
Change in PPS-10 from BL to Week 1Change in PPS-10 from BL to Week 2Change in PPS-10 from BL to Week 4Change in PPS-10 from BL to Week 8Change in PPS-10 from BL to Week 12
Hydroxyzine and Varenicline-1.38-1.48-1.55-2.05-2.75

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Changes in Anxiety Using the 6-item State-Trait Anxiety Inventory (STAI)

"Trait and state anxiety levels will be monitored for changes using the 6-item State-Trait Anxiety Inventory (STAI). All items are rated on a 4-point scale (1-Almost Never to 4-Almost Always). The range of scores is from 6 to 24. Higher scores indicate greater anxiety." (NCT04188106)
Timeframe: Weeks 1, 2, 4, 8, 12

Interventionscore on a scale (Mean)
Change in STAI from BL to Week 1Change in STAI from BL to Week 2Change in STAI from BL to Week 4Change in STAI from BL to Week 8Change in STAI from BL to Week 12
Hydroxyzine and Varenicline-0.54-1.09-0.86-1.82-1.65

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Changes in Depression Using the Patient Health Questionnaire (PHQ-9)

"Depression will be monitored for changes using the Patient Health Questionnaire (PHQ-9). The PHQ-9 uses a 4-point scale (Not at all = 0; Several days = 1;More than half the days = 2; Nearly every day = 3). The sum of the scores is calculated (Score range is 0 to 27):~1-4 Minimal depression~5-9 Mild depression~10-14 Moderate depression~15-19 Moderately severe depression~20-27 Severe depression" (NCT04188106)
Timeframe: Weeks 1, 2, 4, 8, 12

Interventionscore on a scale (Mean)
Change in PHQ-9 from BL to Week 1Change in PHQ-9 from BL to Week 2Change in PHQ-9 from BL to Week 4Change in PHQ-9 from BL to Week 8Change in PHQ-9 from BL to Week 12
Hydroxyzine and Varenicline-0.150.630.43-0.27-0.41

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