Page last updated: 2024-12-07

rupatadine

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Description

rupatadine: structure given in first source; RN given refers to trihydrochloride [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID133017
CHEMBL ID91397
CHEBI ID135673
SCHEMBL ID27703
MeSH IDM0270941

Synonyms (54)

Synonym
AC-4726
ur-12592
CHEMBL91397 ,
bdbm50036935
8-chloro-11-[1-(5-methyl-pyridin-3-ylmethyl)-piperidin-4-ylidene]-6,11-dihydro-5h-benzo[5,6]cyclohepta[1,2-b]pyridine
rinialer
rupax
rupatadine (inn)
D07407
158876-82-5
rupatadine
CHEBI:135673
FT-0656455
pafinur
rupatadine [inn]
5h-benzo(5,6)cyclohepta(1,2-b)pyridine, 8-chloro-6,11-dihydro-11-(1-((5-methyl-3-pyridinyl)methyl)-4-piperidinylidene)-
unii-2ae8m83g3e
2ae8m83g3e ,
8-chloro-6,11-dihydro-11-(1-((5-methyl-3-pyridyl)methyl)-4-piperidylidene)-5h-benzo(5,6)cyclohepta(1,2-b)pyridine
8-chloro-11-(1-((5-methylpyridin-3-yl)methyl)piperidin-4-ylidene)-6,11-dihydro-5h-benzo[5,6]cyclohepta[1,2-b]pyridine
AKOS015907788
rupatadine [mi]
rupatadine [who-dd]
rupatadine [mart.]
8-chloro-11-(1-[(5-methyl-3-pyridyl)methyl]-4-piperidyliden)-6,11-dihydro-5h-benzo[5,6]cyclohepta[1,2-b]pyridine
WUZYKBABMWJHDL-UHFFFAOYSA-N
SCHEMBL27703
CS-3481
Q-201687
HY-13511
DTXSID00166534
sr-01000945073
SR-01000945073-1
13-chloro-2-[1-[(5-methylpyridin-3-yl)methyl]piperidin-4-ylidene]-4-azatricyclo[9.4.0.03,8]pentadeca-1(11),3(8),4,6,12,14-hexaene
DB11614
rupatidine
8-chloro-11-{1-[(5-methylpyridin-3-yl)methyl]piperidin-4-ylidene}-6,11-dihydro-5h-benzo[5,6]cyclohepta[1,2-b]pyridine
8-chloro-11-[1-[(5-methylpyridin-3-yl)methyl]piperidin-4-ylidene]-5,6-dihydrobenzo[1,2]cyclohepta[2,4-b]pyridine
Q423450
ur12592
gtpl10103
BCP02444
rupatadine free base
rupafi
SB17506
NCGC00386213-04
5h-benzo[5,6]cyclohepta[1,2-b]pyridine, 8-chloro-6,11-dihydro-11-[1-[(5-methyl-3-pyridinyl)methyl]-4-piperidinylidene]-
A883340
8-chloro-6,11-dihydro-11-[1-[(5-methyl-3-pyridyl)methyl]-4-piperidylidene]-5h-benzo[5,6]cyclohepta[1,2-b]pyridine;
13-chloro-2-[1-[(5-methylpyridin-3-yl)methyl]piperidin-4-ylidene]-4-azatricyclo[9.4.0.0^{3,8]pentadeca-1(11),3(8),4,6,12,14-hexaene
EN300-1272665
13-chloro-2-{1-[(5-methylpyridin-3-yl)methyl]piperidin-4-ylidene}-4-azatricyclo[9.4.0.0,3,8]pentadeca-1(11),3(8),4,6,12,14-hexaene
F77181
Z2681891941

Research Excerpts

Overview

Rupatadine is a potent histamine receptor 1 (H1R) and platelet-activating factor (PAF) blocker. It is a safe and well tolerated drug in patients over 2 years old.

ExcerptReferenceRelevance
"Rupatadine is a potent histamine receptor 1 (H1R) and platelet-activating factor (PAF) blocker."( Therapeutic effect of rupatadine against l-arginine-induced acute pancreatitis in rats: role of inflammation.
Khalaf, HM; Mohamed, MZ; Mohammed, HH, 2022
)
1.76
"Rupatadine is a novel non-sedating second-generation H"( Efficacy and safety of rupatadine in Japanese patients with seasonal allergic rhinitis: A double-blind, randomized, multicenter, placebo-controlled clinical trial.
Aoki, H; Okubo, K; Suzuki, T; Tanaka, A, 2019
)
2.27
"Rupatadine is a novel H1 antihistamine with platelet-activating factor antagonist activity. "( Long-term safety and efficacy of rupatadine in Japanese patients with itching due to chronic spontaneous urticaria, dermatitis, or pruritus: A 12-month, multicenter, open-label clinical trial.
Aoki, H; Hide, M; Suzuki, T; Tanaka, A, 2019
)
2.24
"Rupatadine fumarate is a second-generation antihistamine provided with a potent, long-lasting and balanced in vivo dual platelet-activating factor (PAF) and histamine antagonist activity and it uniquely combines both activities at a high level of potency. "( Rupatadine for the treatment of urticaria.
Calogiuri, GF; Delle Donne, P; Di Leo, E; Ferrannini, A; Nettis, E; Vacca, A, 2013
)
3.28
"Rupatadine is a selective non-sedating H1 -antihistamine approved for the treatment of CsU."( Clinical effectiveness and safety of cetirizine versus rupatadine in chronic spontaneous urticaria: a randomized, double-blind, 6-week trial.
Dakhale, GN; Hiware, SK; Mahatme, MS; Mishra, DB; Mukhi, JI; Salve, AM; Shinde, AT, 2014
)
1.37
"Rupatadine (RUP) is an oral antihistamine and platelet-activating factor antagonist and is shown as the substrate of CYP3A5 and P-gp. "( CYP3A5*3 and MDR1 C3435T are influencing factors of inter-subject variability in rupatadine pharmacokinetics in healthy Chinese volunteers.
Huang, S; Li, X; Liu, M; Xia, C; Xiong, Y; Yang, J; Yuan, Z; Zhang, H, 2016
)
2.1
"Rupatadine is a new, second-generation, selective oral H1-antihistamine."( Rupatadine relieves allergic rhinitis: a prospective observational study.
Eloy, P; Imschoot, J; Tobback, L, 2015
)
2.58
"Rupatadine is a second-generation H1-antihistamine with dual affinity for histamine H1 and PAF receptors. "( Rupatadine: global safety evaluation in allergic rhinitis and urticaria.
Bachert, C; González-Núñez, V; Mullol, J, 2016
)
3.32
"Rupatadine is a safe and well tolerated drug in patients over 2 years old, with no central nervous system or cardiovascular effects and it can be taken with or without foods."( Rupatadine: global safety evaluation in allergic rhinitis and urticaria.
Bachert, C; González-Núñez, V; Mullol, J, 2016
)
2.6
"Rupatadine is a marketed second generation antihistamine, with anti-PAF activity, indicated for symptomatic treatment of allergic rhinitis and urticaria. "( Pharmacokinetics, Safety and Cognitive Function Profile of Rupatadine 10, 20 and 40 mg in Healthy Japanese Subjects: A Randomised Placebo-Controlled Trial.
Ferber, G; Fernandes, S; Izquierdo, I; Lorch, U; Santamaría, E; Täubel, J, 2016
)
2.12
"Rupatadine is an antihistamine with a demonstrated anti-PAF effect, although its capacity to inhibit PAF-induced MC degranulation has not been fully evaluated."( Effects of Rupatadine on Platelet- Activating Factor-Induced Human Mast Cell Degranulation Compared With Desloratadine and Levocetirizine (The MASPAF Study).
Ainsua-Enrich, E; Bartra, J; Martin, M; Mullol, J; Munoz-Cano, R; Picado, C; Sánchez-Lopez, J; Torres-Atencio, I; Valero, A,
)
1.24
"Rupatadine is a once-daily non-sedative, selective, long-acting H1 anti-histamine with antagonistic PAF effects through its interaction with specific receptors."( Pharmacological profile, efficacy and safety of rupatadine in allergic rhinitis.
Katiyar, S; Prakash, S, 2009
)
1.33
"Rupatadine is a new oral antihistaminic agent used for the management of allergic inflammatory conditions, such as rhinitis and chronic urticaria. "( Antihistaminic effects of rupatadine and PKPD modelling.
Carbo, ML; Izquierdo, I; Merlos, M; Nadal, T; Peña, J; Solans, A,
)
1.87
"Rupatadine is an oral active antihistamine and platelet-activating factor antagonist indicated for the management of allergic rhinitis and chronic urticaria in Europe."( Pharmacokinetic and safety profile of rupatadine when coadministered with azithromycin at steady-state levels: a randomized, open-label, two-way, crossover, Phase I study.
Antonijoan, R; Barbanoj, M; Carbó, ML; Donado, E; Izquierdo, I; Merlos, M; Nadal, T; Peña, J; Solans, A, 2008
)
2.06
"Rupatadine is a second generation antihistamine with increased affinity to histamine receptor H1; it is also a potent PAF (platelet-activating factor) antagonist."( Futura study: evaluation of efficacy and safety of rupatadine fumarate in the treatment of persistent allergic rhinitis.
Antila, M; Campos, RA; Castro, FM; Chavarria, ML; de Mello Junior, JF; de Mello, JF; Di Gesu, G; Guimarães, RE; Mion, Ode G; Mocellin, M; Rapoport, PB; Rosario, N; Solé, D; Wexler, L,
)
1.1
"Rupatadine is a dual antagonist of both histamine and platelet-activating factor."( Rupatadine and its effects on symptom control, stimulation time, and temperature thresholds in patients with acquired cold urticaria.
Ferrán, M; Giménez-Arnau, A; Izquierdo, I; Maurer, M; Metz, M; Scholz, E, 2010
)
2.52
"Rupatadine is a new antihistamine with potential antiallergic activities."( Rupatadine improves nasal symptoms, airflow and inflammation in patients with persistent allergic rhinitis: a pilot study.
Ciprandi, G; Cirillo, I,
)
2.3
"Rupatadine is a new H(1)-antihistamine which also inhibits platelet activating factor (PAF) release and has been shown to be clinically effective at doses of 10 mg."( Rupatadine does not potentiate the CNS depressant effects of lorazepam: randomized, double-blind, crossover, repeated dose, placebo-controlled study.
Antonijoan, RM; Ballester, MR; Barbanoj, MJ; Donado, E; García-Gea, C; Izquierdo, I; Martínez, J, 2010
)
2.52
"Rupatadine is a better choice for seasonal allergic rhinitis compared with levocetirizine because of its better efficacy and safety profile."( Rupatadine and levocetirizine for seasonal allergic rhinitis: a comparative study of efficacy and safety.
Allala, U; Jaida, J; Maiti, R; Palani, A; Rahman, J, 2010
)
3.25
"Rupatadine is a better choice in CIU in comparison to levocetirizine due to better efficacy and safety profile."( Rupatadine and levocetirizine in chronic idiopathic urticaria: a comparative study of efficacy and safety.
Ahmed, I; Goud, P; Jaida, J; Maiti, R; Palani, A; Raghavendra, BN, 2011
)
3.25
"Rupatadine is a new antihistamine effective in allergic rhinitis and urticaria, but the effect on mosquito-bite allergy is not known."( Rupatadine 10 mg in the treatment of immediate mosquito-bite allergy.
Brummer-Korvenkontio, H; Izquierdo, I; Karppinen, A; Reunala, T, 2012
)
2.54
"Rupatadine is a new second-generation antihistamine with H(1) receptor antagonist activity and platelet-activating factor antagonist properties. "( The effect of rupatadine on lung histopathology in a murine model of chronic asthma.
Bagriyanik, AH; Firinci, F; Karaman, M; Karaman, O; Kiray, M; Tuncel, T; Uysal, P; Uzuner, N; Yilmaz, O, 2013
)
2.19
"Rupatadine is a new agent for the management of diseases with allergic inflammatory conditions, such as seasonal and perennial rhinitis. "( Rupatadine: a new selective histamine H1 receptor and platelet-activating factor (PAF) antagonist. A review of pharmacological profile and clinical management of allergic rhinitis.
García-Rafanell, J; Izquierdo, I; Merlos, M, 2003
)
3.2
"Rupatadine is a new second generation H(1)-antihistamine with once-daily dosing that may provide better control of symptoms than the currently used H(1)-receptor blockers because of its dual pharmacological profile (anti-PAF and anti-H(1))."( Rupatadine 10 mg and ebastine 10 mg in seasonal allergic rhinitis: a comparison study.
Castillo, JA; De Molina, M; Guadaño, EM; Meseguer, J; Picado, C; Serra-Batlles, J; Valero, A, 2004
)
2.49
"Rupatadine (RUP) is a new H(1)-antihistamine which also inhibits platelet activating factor (PAF) release in inflammatory reactions."( 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
)
1.29
"Rupatadine is a novel compound with potent dual antihistamine and platelet-activating factor antagonist activities and no sedative effects."( Effects of rupatadine vs placebo on allergen-induced symptoms in patients exposed to aeroallergens in the Vienna Challenge Chamber.
Arnáiz, E; Horak, F; Izquierdo, I; Leuratti, C; Pérez, I; Stuebner, P; Zieglmayer, R, 2006
)
2.17
"Rupatadine is a once-daily, non-sedating, selective and long-acting new drug with a strong antagonist activity towards both histamine H(1) receptors and platelet-activating factor receptors. "( Rupatadine: pharmacological profile and its use in the treatment of allergic disorders.
Picado, C, 2006
)
3.22
"Rupatadine is a new potent nonsedative anti-H1."( Rupatadine in the treatment of chronic idiopathic urticaria: a double-blind, randomized, placebo-controlled multicentre study.
Arnaiz, E; Donado, E; Gimenez-Arnau, A; Ianosi, S; Izquierdo, I; Kaszuba, A; Malbran, A; Perez, I; Poop, G; Pujol, RM, 2007
)
2.5
"Rupatadine 10 mg is a fast, long-acting, efficacious and safe treatment option for the management of patients with moderate-to-severe CIU."( Rupatadine in the treatment of chronic idiopathic urticaria: a double-blind, randomized, placebo-controlled multicentre study.
Arnaiz, E; Donado, E; Gimenez-Arnau, A; Ianosi, S; Izquierdo, I; Kaszuba, A; Malbran, A; Perez, I; Poop, G; Pujol, RM, 2007
)
3.23
"Rupatadine fumarate is a potent, selective, histamine H(1)-receptor antagonist and PAF inhibitor with demonstrated efficacy for the relief of allergic rhinitis. "( Lack of effects between rupatadine 10 mg and placebo on actual driving performance of healthy volunteers.
Jolles, J; Theunissen, E; van Leeuwen, C; van Oers, A; Vuurman, E, 2007
)
2.09
"Rupatadine is an oral active antihistamine for the management of diseases with allergic inflammatory conditions, such as perennial and seasonal rhinitis and chronic idiopathic urticaria. "( Influence of food on the oral bioavailability of rupatadine tablets in healthy volunteers: a single-dose, randomized, open-label, two-way crossover study.
Carbó, ML; Izquierdo, I; Merlos, M; Nadal, T; Peña, J; Solans, A, 2007
)
2.04

Effects

Rupatadine has a suppressing effect on H1R and B2R gene expression which could add to its efficacy towards allergy and allergy-like conditions. Once-daily dosing is permitted, moreover is well tolerated by young adults and the elders.

Rupatadine has dual affinity for histamine H1 -receptors and PAF receptors. It has a suppressing effect on H1R and B2R gene expression which could add to its efficacy towards allergy and allergy-like conditions. Oral rupat adine has been approved for the treatment of allergic rhinitis and chronic urticaria in several European countries.

ExcerptReferenceRelevance
"Rupatadine has a rapid onset of action and a long-lasting effect, so a once-daily dosing is permitted, moreover is well tolerated by young adults and the elders."( Rupatadine for the treatment of urticaria.
Calogiuri, GF; Delle Donne, P; Di Leo, E; Ferrannini, A; Nettis, E; Vacca, A, 2013
)
2.55
"Rupatadine has a suppressing effect on H1R and B2R gene expression which could add to its efficacy towards allergy and allergy-like conditions."( Rupatadine effectively prevents the histamine-induced up regulation of histamine H1R and bradykinin B2R receptor gene expression in the rat paw.
Dedi, H; Goulas, A; Kalokasidis, K; Karkavelas, G; Mirtsou, V; Molyva, D; Poulios, C, 2014
)
3.29
"Rupatadine has a rapid onset of action, and its long-lasting effect (>24 h) permits once-daily dosing."( Rupatadine: a new selective histamine H1 receptor and platelet-activating factor (PAF) antagonist. A review of pharmacological profile and clinical management of allergic rhinitis.
García-Rafanell, J; Izquierdo, I; Merlos, M, 2003
)
2.48
"Rupatadine has a rapid onset of action and a long-lasting effect, so a once-daily dosing is permitted, moreover is well tolerated by young adults and the elders."( Rupatadine for the treatment of urticaria.
Calogiuri, GF; Delle Donne, P; Di Leo, E; Ferrannini, A; Nettis, E; Vacca, A, 2013
)
2.55
"Rupatadine has a suppressing effect on H1R and B2R gene expression which could add to its efficacy towards allergy and allergy-like conditions."( Rupatadine effectively prevents the histamine-induced up regulation of histamine H1R and bradykinin B2R receptor gene expression in the rat paw.
Dedi, H; Goulas, A; Kalokasidis, K; Karkavelas, G; Mirtsou, V; Molyva, D; Poulios, C, 2014
)
3.29
"Rupatadine has dual affinity for histamine H1 -receptors and PAF receptors."( Update on rupatadine in the management of allergic disorders.
Bachert, C; Bousquet, J; Canonica, GW; Giménez-Arnau, A; Kowalski, ML; Maurer, M; Mullol, J; Ryan, D; Scadding, G; Simons, FE, 2015
)
1.54
"Rupatadine has a rapid onset of action, and its long-lasting effect (>24 h) permits once-daily dosing."( Rupatadine: a new selective histamine H1 receptor and platelet-activating factor (PAF) antagonist. A review of pharmacological profile and clinical management of allergic rhinitis.
García-Rafanell, J; Izquierdo, I; Merlos, M, 2003
)
2.48
"Oral rupatadine has been approved for the treatment of allergic rhinitis and chronic urticaria in adults and adolescents in several European countries."( Influence of food on the oral bioavailability of rupatadine tablets in healthy volunteers: a single-dose, randomized, open-label, two-way crossover study.
Carbó, ML; Izquierdo, I; Merlos, M; Nadal, T; Peña, J; Solans, A, 2007
)
1.05

Actions

ExcerptReferenceRelevance
"Rupatadine can inhibit histamine and cytokine secretion from human mast cells in response to allergic, immune and neuropeptide triggers. "( Rupatadine inhibits proinflammatory mediator secretion from human mast cells triggered by different stimuli.
Chliva, C; Clemons, A; House, M; Kalogeromitros, D; Kempuraj, D; Makris, M; Theoharides, TC; Vasiadi, M; Wolfberg, A; Zhang, B, 2010
)
3.25

Treatment

Rupatadine treatment is effective and well tolerated in patients with allergen-induced symptoms exposed to aeroallergens in a controlled exposure chamber. Pretreatment with rup atadine has a beneficial effect on acute lung injury induced by oleic acid in rabbits. Rupat adine preserved a nearly normal intestinal mucosa picture with replenished GSH and elevated IL-10.

ExcerptReferenceRelevance
"Rupatadine pretreatment reduced the previously mentioned parameters, preserved a nearly normal intestinal mucosa picture with replenished GSH and elevated IL-10."( Rupatadine protects the intestinal mucosa from injury by 5-flurouracil via modulation of inflammation, apoptosis and intestinal permeability.
Mohamed, MZ; Mohammed, HH, 2022
)
2.89
"Rupatadine treatment induced significant symptom relief (both nasal and ocular, respectively p=0.005 and p=0.0004), including obstruction (p=0.0015) and significant increase of nasal airflow (p=0.0025)."( Rupatadine improves nasal symptoms, airflow and inflammation in patients with persistent allergic rhinitis: a pilot study.
Ciprandi, G; Cirillo, I,
)
2.3
"Rupatadine treatment is effective and well tolerated in patients with allergen-induced symptoms exposed to aeroallergens in a controlled exposure chamber."( Effects of rupatadine vs placebo on allergen-induced symptoms in patients exposed to aeroallergens in the Vienna Challenge Chamber.
Arnáiz, E; Horak, F; Izquierdo, I; Leuratti, C; Pérez, I; Stuebner, P; Zieglmayer, R, 2006
)
2.17
"Pretreatment with rupatadine has a beneficial effect on acute lung injury induced by oleic acid in rabbits."( [Protective effect of rupatadine against oleic acid-induced acute lung injury in rabbits].
He, JL; Lu, J; Xu, GL; Yu, SQ; Zhang, LL; Zhou, M, 2007
)
0.98

Toxicity

rupatadine effectively controls persistent allergic rhinitis; it is safe and presents low incidence of side effects. The overall incidence of adverse drug reactions was also found to be less in rupatadine group.

ExcerptReferenceRelevance
" All treatments were well tolerated and no serious adverse events were recorded."( A randomized, double-blind, parallel-group study, comparing the efficacy and safety of rupatadine (20 and 10 mg), a new PAF and H1 receptor-specific histamine antagonist, to loratadine 10 mg in the treatment of seasonal allergic rhinitis.
Dumur, JP; Izquierdo, I; Pérez, I; Saint-Martin, F, 2004
)
0.55
"The present results suggest that rupatadine 10 mg a day may be a valuable and safe alternative for the symptomatic treatment of seasonal allergic rhinitis."( A randomized, double-blind, parallel-group study, comparing the efficacy and safety of rupatadine (20 and 10 mg), a new PAF and H1 receptor-specific histamine antagonist, to loratadine 10 mg in the treatment of seasonal allergic rhinitis.
Dumur, JP; Izquierdo, I; Pérez, I; Saint-Martin, F, 2004
)
0.83
" Tolerability was based on the recording of adverse events (AEs), physical examination, electrocardiograms, and laboratory screen controls at baseline and the final study visit."( Pharmacokinetic and safety profile of rupatadine when coadministered with azithromycin at steady-state levels: a randomized, open-label, two-way, crossover, Phase I study.
Antonijoan, R; Barbanoj, M; Carbó, ML; Donado, E; Izquierdo, I; Merlos, M; Nadal, T; Peña, J; Solans, A, 2008
)
0.62
"Rupatadine (Rupafin), a novel antihistamine approved recently in Europe for the treatment of allergic rhinitis (AR) and chronic idiopathic urticaria in patients aged>or=12 years, has been shown to be highly efficacious, and as safe and well tolerated as other commonly employed antihistamines in the treatment of allergic disease."( Safety of rupatadine administered over a period of 1 year in the treatment of persistent allergic rhinitis: a multicentre, open-label study in Spain.
Antépara, I; Borja, J; Castillo, JA; de la Torre, F; del Cuvillo, A; Donado, E; Izquierdo, I; Molà, O; Rivas, P; Valero, A, 2009
)
2.2
" Safety was assessed by means of adverse events (AEs) reported by patients or detected by investigators, scheduled centralized ECG with special attention to Bazzet corrected QT interval (QTcB) and standard laboratory investigations."( Safety of rupatadine administered over a period of 1 year in the treatment of persistent allergic rhinitis: a multicentre, open-label study in Spain.
Antépara, I; Borja, J; Castillo, JA; de la Torre, F; del Cuvillo, A; Donado, E; Izquierdo, I; Molà, O; Rivas, P; Valero, A, 2009
)
0.76
" Adverse events occurred in 19."( Futura study: evaluation of efficacy and safety of rupatadine fumarate in the treatment of persistent allergic rhinitis.
Antila, M; Campos, RA; Castro, FM; Chavarria, ML; de Mello Junior, JF; de Mello, JF; Di Gesu, G; Guimarães, RE; Mion, Ode G; Mocellin, M; Rapoport, PB; Rosario, N; Solé, D; Wexler, L,
)
0.38
"rupatadine effectively controls persistent allergic rhinitis; it is safe and presents low incidence of side effects."( Futura study: evaluation of efficacy and safety of rupatadine fumarate in the treatment of persistent allergic rhinitis.
Antila, M; Campos, RA; Castro, FM; Chavarria, ML; de Mello Junior, JF; de Mello, JF; Di Gesu, G; Guimarães, RE; Mion, Ode G; Mocellin, M; Rapoport, PB; Rosario, N; Solé, D; Wexler, L,
)
1.83
" Incidence of adverse effects was less in the rupatadine group compared with the levocetirizine group."( Rupatadine and levocetirizine for seasonal allergic rhinitis: a comparative study of efficacy and safety.
Allala, U; Jaida, J; Maiti, R; Palani, A; Rahman, J, 2010
)
2.06
" The overall incidence of adverse drug reactions was also found to be less in rupatadine group."( Rupatadine and levocetirizine in chronic idiopathic urticaria: a comparative study of efficacy and safety.
Ahmed, I; Goud, P; Jaida, J; Maiti, R; Palani, A; Raghavendra, BN, 2011
)
2.04
"The review of these data indicates that rupatadine is highly selective for histamine H1-receptors, exhibits additional PAF antagonism in in vitro and in vivo studies, does not cross the blood-brain barrier, and has similar adverse events comparable with other second-generation antihistamines."( Rupatadine: global safety evaluation in allergic rhinitis and urticaria.
Bachert, C; González-Núñez, V; Mullol, J, 2016
)
2.14
" The safety assessments showed that all treatment related side effects were of mild intensity and there were no serious adverse events (SAEs) or withdrawals due to treatment-emergent adverse events (TEAEs) in this study."( Pharmacokinetics, Safety and Cognitive Function Profile of Rupatadine 10, 20 and 40 mg in Healthy Japanese Subjects: A Randomised Placebo-Controlled Trial.
Ferber, G; Fernandes, S; Izquierdo, I; Lorch, U; Santamaría, E; Täubel, J, 2016
)
0.68
"This study demonstrated that rupatadine is safe and well tolerated by Japanese healthy subjects."( Pharmacokinetics, Safety and Cognitive Function Profile of Rupatadine 10, 20 and 40 mg in Healthy Japanese Subjects: A Randomised Placebo-Controlled Trial.
Ferber, G; Fernandes, S; Izquierdo, I; Lorch, U; Santamaría, E; Täubel, J, 2016
)
0.97
" No noteworthy dose-related increase in the incidence of adverse drug reactions was observed."( Efficacy and safety of rupatadine in Japanese adult and adolescent patients with chronic spontaneous urticaria: A double-blind, randomized, multicenter, placebo-controlled clinical trial.
Aoki, H; Hide, M; Suzuki, T; Tanaka, A, 2019
)
0.82
" Adverse drug reactions (ADRs) were reported at an overall incidence of 18."( Long-term safety and efficacy of rupatadine in Japanese patients with itching due to chronic spontaneous urticaria, dermatitis, or pruritus: A 12-month, multicenter, open-label clinical trial.
Aoki, H; Hide, M; Suzuki, T; Tanaka, A, 2019
)
0.8

Pharmacokinetics

Study found no significant differences in pharmacokinetic parameters between rupatadine 10 mg administered alone or with azithromycin 500 mg on day 2 and 250 mg from day 3 to day 6.

ExcerptReferenceRelevance
" Except for maximum observed concentration during a dosing interval (Cmax,ss) of 3-hydroxydesloratadine, on average, there were no statistically significant differences in mean plasma concentrations in any of the main pharmacokinetic parameters of rupatadine, desloratadine, and 3-hydroxydesloratadine when administered in combination with azithromycin or alone."( Pharmacokinetic and safety profile of rupatadine when coadministered with azithromycin at steady-state levels: a randomized, open-label, two-way, crossover, Phase I study.
Antonijoan, R; Barbanoj, M; Carbó, ML; Donado, E; Izquierdo, I; Merlos, M; Nadal, T; Peña, J; Solans, A, 2008
)
0.8
" The method has been successfully applied to a pharmacokinetic study of rupatadine and its major metabolite after oral administration of 10, 20 and 40mg rupatadine tablets to healthy Chinese volunteers."( Simultaneous determination of rupatadine and its metabolite desloratadine in human plasma by a sensitive LC-MS/MS method: application to the pharmacokinetic study in healthy Chinese volunteers.
Fan, G; Hong, Z; Wei, H; Wen, J; Wu, Y, 2009
)
0.87
" The relationship between RUP plasma concentration, pharmacokinetic parameters, and polymorphic alleles (CYP3A5 and MDR1) were assessed."( CYP3A5*3 and MDR1 C3435T are influencing factors of inter-subject variability in rupatadine pharmacokinetics in healthy Chinese volunteers.
Huang, S; Li, X; Liu, M; Xia, C; Xiong, Y; Yang, J; Yuan, Z; Zhang, H, 2016
)
0.66
" The method was successfully applied to a pharmacokinetic study of RT and its two metabolite DT and 3-OH-DT in healthy volunteers following single (10, 20, 40 mg) and multiple (10 mg) oral doses of rupatadine fumarate tablets."( Development of a highly sensitive LC-MS/MS method for simultaneous determination of rupatadine and its two active metabolites in human plasma: Application to a clinical pharmacokinetic study.
Ding, L; Gu, P; Li, Q; Liu, B; Pan, L; Sun, C; Wu, C; Zhang, J, 2015
)
0.83
"Exposure to rupatadine as measured by Cmax and AUC was found to increase in a dose dependent manner over the dose range of 10-40 mg for both single and multiple dose administration."( Pharmacokinetics, Safety and Cognitive Function Profile of Rupatadine 10, 20 and 40 mg in Healthy Japanese Subjects: A Randomised Placebo-Controlled Trial.
Ferber, G; Fernandes, S; Izquierdo, I; Lorch, U; Santamaría, E; Täubel, J, 2016
)
1.06
"To optimise a pharmacokinetic (PK) study design of rupatadine for 2-5 year olds by using a population PK model developed with data from a study in 6-11 year olds."( Population pharmacokinetic modelling of rupatadine solution in 6-11 year olds and optimisation of the experimental design in younger children.
Estévez, JA; Izquierdo, I; Riba, J; Santamaría, E; Valle, M, 2017
)
0.97
"5 mg, as it provided a Cmax below the 3 ng/ml threshold."( Population pharmacokinetic modelling of rupatadine solution in 6-11 year olds and optimisation of the experimental design in younger children.
Estévez, JA; Izquierdo, I; Riba, J; Santamaría, E; Valle, M, 2017
)
0.72

Compound-Compound Interactions

Study aimed to observe the effect of rupatadine fumarate combined with acupoint application in the treatment of allergic rhinitis complicated with diabetes. Results showed that single oral doses of r upadine 10 mg in combination with alcohol do not produce more cognitive and psychomotor impairment than alcohol alone.

ExcerptReferenceRelevance
"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
)
0.82
" Except for maximum observed concentration during a dosing interval (Cmax,ss) of 3-hydroxydesloratadine, on average, there were no statistically significant differences in mean plasma concentrations in any of the main pharmacokinetic parameters of rupatadine, desloratadine, and 3-hydroxydesloratadine when administered in combination with azithromycin or alone."( Pharmacokinetic and safety profile of rupatadine when coadministered with azithromycin at steady-state levels: a randomized, open-label, two-way, crossover, Phase I study.
Antonijoan, R; Barbanoj, M; Carbó, ML; Donado, E; Izquierdo, I; Merlos, M; Nadal, T; Peña, J; Solans, A, 2008
)
0.8
" This study aimed to observe the effect of rupatadine fumarate combined with acupoint application in the treatment of allergic rhinitis complicated with diabetes and its effect on serum IgE levels."( Efficacy and Safety of Rupatadine Fumarate Combined with Acupoint Application in Allergic Rhinitis Complicated with Diabetes.
Chen, X; Jiang, P; Liu, Y; Shi, J; Zhang, W, 2022
)
1.29

Bioavailability

The purpose of this study was to describe the effect of the concomitant intake of food on the pharmacokinetic profile and bioavailability of a single dose of rupatadine. The 90% CIs were included in the interval 80% to 125% for deslorat adine and 3-hydroxydesloratAdine.

ExcerptReferenceRelevance
"The purpose of this study was to describe the effect of the concomitant intake of food on the pharmacokinetic profile and bioavailability of a single dose of rupatadine."( Influence of food on the oral bioavailability of rupatadine tablets in healthy volunteers: a single-dose, randomized, open-label, two-way crossover study.
Carbó, ML; Izquierdo, I; Merlos, M; Nadal, T; Peña, J; Solans, A, 2007
)
0.79
" The 90% CIs were included in the interval 80% to 125% for desloratadine and 3-hydroxydesloratadine, whereas 90% CI for rupatadine was shifted to the right of the interval used for comparing bioavailability of the drugs."( Pharmacokinetic and safety profile of rupatadine when coadministered with azithromycin at steady-state levels: a randomized, open-label, two-way, crossover, Phase I study.
Antonijoan, R; Barbanoj, M; Carbó, ML; Donado, E; Izquierdo, I; Merlos, M; Nadal, T; Peña, J; Solans, A, 2008
)
0.83
" The significant interindividual differences of CYP3A5 and P-gp often cause bioavailability differences of some clinical drugs."( CYP3A5*3 and MDR1 C3435T are influencing factors of inter-subject variability in rupatadine pharmacokinetics in healthy Chinese volunteers.
Huang, S; Li, X; Liu, M; Xia, C; Xiong, Y; Yang, J; Yuan, Z; Zhang, H, 2016
)
0.66

Dosage Studied

Rupatadine is a new second generation H(1)-antihistamine with once-daily dosing. It may provide better control of symptoms than the currently used H( 1)-receptor blockers because of its dual pharmacological profile (anti-PAF and anti-H(1) Rupat adine has a rapid onset of action and a long-lasting effect.

ExcerptRelevanceReference
" Rupatadine is a new second generation H(1)-antihistamine with once-daily dosing that may provide better control of symptoms than the currently used H(1)-receptor blockers because of its dual pharmacological profile (anti-PAF and anti-H(1))."( Rupatadine 10 mg and ebastine 10 mg in seasonal allergic rhinitis: a comparison study.
Castillo, JA; De Molina, M; Guadaño, EM; Meseguer, J; Picado, C; Serra-Batlles, J; Valero, A, 2004
)
2.68
"A stability-indicating MEKC was developed and validated for the analysis of rupatadine in tablet dosage forms, using nimesulide as internal standard."( Determination of rupatadine in pharmaceutical formulations by a validated stability-indicating MEKC method.
da Silva Sangoi, M; da Silva, LM; Dalmora, SL; Nogueira, DR; Todeschini, V, 2008
)
0.92
" The simulated response after repeated once-daily administrations of 10 mg rupatadine showed a significant and maintained antihistaminic effect over time, between two consecutive dosing intervals."( Antihistaminic effects of rupatadine and PKPD modelling.
Carbo, ML; Izquierdo, I; Merlos, M; Nadal, T; Peña, J; Solans, A,
)
0.66
" Except for maximum observed concentration during a dosing interval (Cmax,ss) of 3-hydroxydesloratadine, on average, there were no statistically significant differences in mean plasma concentrations in any of the main pharmacokinetic parameters of rupatadine, desloratadine, and 3-hydroxydesloratadine when administered in combination with azithromycin or alone."( Pharmacokinetic and safety profile of rupatadine when coadministered with azithromycin at steady-state levels: a randomized, open-label, two-way, crossover, Phase I study.
Antonijoan, R; Barbanoj, M; Carbó, ML; Donado, E; Izquierdo, I; Merlos, M; Nadal, T; Peña, J; Solans, A, 2008
)
0.8
" Flares were induced before dosing and up to 96 h afterwards by intradermal PAF and histamine."( Efficacy and tolerability of rupatadine at four times the recommended dose against histamine- and platelet-activating factor-induced flare responses and ex vivo platelet aggregation in healthy males.
Church, MK, 2010
)
0.65
" Rupatadine has a rapid onset of action and a long-lasting effect, so a once-daily dosing is permitted, moreover is well tolerated by young adults and the elders."( Rupatadine for the treatment of urticaria.
Calogiuri, GF; Delle Donne, P; Di Leo, E; Ferrannini, A; Nettis, E; Vacca, A, 2013
)
2.74
" The developed methods were applied to estimate rupatadine content in its pharmaceutical tablet dosage form with acceptable recoveries."( Resonance Rayleigh scattering and spectrofluorimetric approaches for the selective determination of rupatadine using erythrosin B as a probe: application to content uniformity test.
Abdel-Lateef, MA; Almahri, A; Derayea, SM; El Hamd, MA; Samir, E, 2021
)
1.09
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
benzocycloheptapyridine
[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
Rupatadine H1-Antihistamine Action87

Protein Targets (4)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency39.81070.009610.525035.4813AID1479145
[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)
Platelet-activating factor receptorHomo sapiens (human)IC50 (µMol)3.70000.00030.63183.7000AID254775
Histamine H1 receptorHomo sapiens (human)IC50 (µMol)0.00390.00000.44365.1768AID254701
Histamine H1 receptorHomo sapiens (human)Ki0.00400.00000.511010.0000AID1569605
Sodium-dependent neutral amino acid transporter B(0)AT2Homo sapiens (human)IC50 (µMol)40.00004.00004.00004.0000AID1169507
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (46)

Processvia Protein(s)Taxonomy
positive regulation of cellular extravasationPlatelet-activating factor receptorHomo sapiens (human)
regulation of transcription by RNA polymerase IIPlatelet-activating factor receptorHomo sapiens (human)
chemotaxisPlatelet-activating factor receptorHomo sapiens (human)
inflammatory responsePlatelet-activating factor receptorHomo sapiens (human)
immune responsePlatelet-activating factor receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayPlatelet-activating factor receptorHomo sapiens (human)
parturitionPlatelet-activating factor receptorHomo sapiens (human)
response to symbiotic bacteriumPlatelet-activating factor receptorHomo sapiens (human)
lipopolysaccharide-mediated signaling pathwayPlatelet-activating factor receptorHomo sapiens (human)
positive regulation of interleukin-6 productionPlatelet-activating factor receptorHomo sapiens (human)
positive regulation of tumor necrosis factor productionPlatelet-activating factor receptorHomo sapiens (human)
inositol trisphosphate biosynthetic processPlatelet-activating factor receptorHomo sapiens (human)
G protein-coupled purinergic nucleotide receptor signaling pathwayPlatelet-activating factor receptorHomo sapiens (human)
positive regulation of neutrophil degranulationPlatelet-activating factor receptorHomo sapiens (human)
transcytosisPlatelet-activating factor receptorHomo sapiens (human)
positive regulation of translationPlatelet-activating factor receptorHomo sapiens (human)
negative regulation of blood pressurePlatelet-activating factor receptorHomo sapiens (human)
positive regulation of smooth muscle cell proliferationPlatelet-activating factor receptorHomo sapiens (human)
positive regulation of inositol phosphate biosynthetic processPlatelet-activating factor receptorHomo sapiens (human)
cellular response to gravityPlatelet-activating factor receptorHomo sapiens (human)
cellular response to cAMPPlatelet-activating factor receptorHomo sapiens (human)
cellular response to fatty acidPlatelet-activating factor receptorHomo sapiens (human)
response to dexamethasonePlatelet-activating factor receptorHomo sapiens (human)
positive regulation of leukocyte tethering or rollingPlatelet-activating factor receptorHomo sapiens (human)
positive regulation of transcytosisPlatelet-activating factor receptorHomo sapiens (human)
positive regulation of maternal process involved in parturitionPlatelet-activating factor receptorHomo sapiens (human)
positive regulation of gastro-intestinal system smooth muscle contractionPlatelet-activating factor receptorHomo sapiens (human)
cellular response to 2-O-acetyl-1-O-hexadecyl-sn-glycero-3-phosphocholinePlatelet-activating factor receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayPlatelet-activating factor receptorHomo 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)
amino acid transmembrane transportSodium-dependent neutral amino acid transporter B(0)AT2Homo sapiens (human)
neurotransmitter transportSodium-dependent neutral amino acid transporter B(0)AT2Homo sapiens (human)
amino acid transportSodium-dependent neutral amino acid transporter B(0)AT2Homo sapiens (human)
neutral amino acid transportSodium-dependent neutral amino acid transporter B(0)AT2Homo sapiens (human)
L-leucine transportSodium-dependent neutral amino acid transporter B(0)AT2Homo sapiens (human)
proline transportSodium-dependent neutral amino acid transporter B(0)AT2Homo sapiens (human)
carboxylic acid transmembrane transportSodium-dependent neutral amino acid transporter B(0)AT2Homo sapiens (human)
sodium ion transmembrane transportSodium-dependent neutral amino acid transporter B(0)AT2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (16)

Processvia Protein(s)Taxonomy
lipopolysaccharide bindingPlatelet-activating factor receptorHomo sapiens (human)
lipopolysaccharide immune receptor activityPlatelet-activating factor receptorHomo sapiens (human)
G protein-coupled receptor activityPlatelet-activating factor receptorHomo sapiens (human)
platelet activating factor receptor activityPlatelet-activating factor receptorHomo sapiens (human)
protein bindingPlatelet-activating factor receptorHomo sapiens (human)
phospholipid bindingPlatelet-activating factor receptorHomo sapiens (human)
mitogen-activated protein kinase bindingPlatelet-activating factor receptorHomo sapiens (human)
G protein-coupled purinergic nucleotide receptor activityPlatelet-activating factor receptorHomo 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)
neutral L-amino acid:sodium symporter activitySodium-dependent neutral amino acid transporter B(0)AT2Homo sapiens (human)
neurotransmitter transmembrane transporter activitySodium-dependent neutral amino acid transporter B(0)AT2Homo sapiens (human)
protein bindingSodium-dependent neutral amino acid transporter B(0)AT2Homo sapiens (human)
amino acid transmembrane transporter activitySodium-dependent neutral amino acid transporter B(0)AT2Homo sapiens (human)
branched-chain amino acid:sodium symporter activitySodium-dependent neutral amino acid transporter B(0)AT2Homo sapiens (human)
proline:sodium symporter activitySodium-dependent neutral amino acid transporter B(0)AT2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (8)

Processvia Protein(s)Taxonomy
plasma membranePlatelet-activating factor receptorHomo sapiens (human)
membranePlatelet-activating factor receptorHomo sapiens (human)
secretory granule membranePlatelet-activating factor receptorHomo sapiens (human)
tertiary granule membranePlatelet-activating factor receptorHomo 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 membraneSodium-dependent neutral amino acid transporter B(0)AT2Homo sapiens (human)
membraneSodium-dependent neutral amino acid transporter B(0)AT2Homo sapiens (human)
plasma membraneSodium-dependent neutral amino acid transporter B(0)AT2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (21)

Assay IDTitleYearJournalArticle
AID130606Dose required to inhibit PAF-induced mortality1994Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17
[(3-Pyridylalkyl)piperidylidene]benzocycloheptapyridine derivatives as dual antagonists of PAF and histamine.
AID183446Tested for dose required to inhibit antigen induced increased permeability1994Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17
[(3-Pyridylalkyl)piperidylidene]benzocycloheptapyridine derivatives as dual antagonists of PAF and histamine.
AID1569608Displacement of [3H]levocetirizine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells assessed as dissociation rate constant by microbeta scintillation counting method2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Route to Prolonged Residence Time at the Histamine H
AID192816Tested at 10 (mg/kg) intravenous dose for percent inhibition of the arterial blood pressure in normotensive rats caused by histamine1994Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17
[(3-Pyridylalkyl)piperidylidene]benzocycloheptapyridine derivatives as dual antagonists of PAF and histamine.
AID1569611Antagonist activity at H1R in human HeLa cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 10 times Ki incubated for 18 to 20 hrs prior to Fluo-4NW dye addition for 1 hr followed by compound washout and subsequent sti2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Route to Prolonged Residence Time at the Histamine H
AID1569606Displacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 80 mins by microbeta scintillation counting method2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Route to Prolonged Residence Time at the Histamine H
AID462891Inhibition of protein farnesyltransferase by continuous fluorescence assay2010Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
Prediction and evaluation of protein farnesyltransferase inhibition by commercial drugs.
AID1569605Displacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting method2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Route to Prolonged Residence Time at the Histamine H
AID183460Intravenous dose required to reduce the lowering of the arterial blood pressure caused by PAF1994Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17
[(3-Pyridylalkyl)piperidylidene]benzocycloheptapyridine derivatives as dual antagonists of PAF and histamine.
AID76375Tested for concentration required to inhibit H1 histamine -induced guinea pig ileum contraction1994Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17
[(3-Pyridylalkyl)piperidylidene]benzocycloheptapyridine derivatives as dual antagonists of PAF and histamine.
AID1569609Displacement of [3H]levocetirizine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells assessed as residence time by microbeta scintillation counting method2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Route to Prolonged Residence Time at the Histamine H
AID183447Tested for dose required to inhibit endotoxin induced mortality in rats1994Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17
[(3-Pyridylalkyl)piperidylidene]benzocycloheptapyridine derivatives as dual antagonists of PAF and histamine.
AID161773Concentration required to inhibit PAF-induced maximum aggregation1994Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17
[(3-Pyridylalkyl)piperidylidene]benzocycloheptapyridine derivatives as dual antagonists of PAF and histamine.
AID130607Tested for dose required to inhibit endotoxin induced mortality in mice1994Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17
[(3-Pyridylalkyl)piperidylidene]benzocycloheptapyridine derivatives as dual antagonists of PAF and histamine.
AID140564Tested for effect on central nervous system in mice at 100 mg/kg peroral dose for spontaneous motor activity (SMA) expressed as percentage relative to control1994Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17
[(3-Pyridylalkyl)piperidylidene]benzocycloheptapyridine derivatives as dual antagonists of PAF and histamine.
AID254701Inhibitory concentration against histamine H1 receptor2005Journal of medicinal chemistry, Oct-20, Volume: 48, Issue:21
Designed multiple ligands. An emerging drug discovery paradigm.
AID1169507Inhibition of eGFP-tagged human B0AT2 expressed in HEK293 cells measured within 10 mins by [3H]proline uptake assay2014Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22
Loratadine and analogues: discovery and preliminary structure-activity relationship of inhibitors of the amino acid transporter B(0)AT2.
AID254775Inhibitory concentration against platelet activating factor receptor2005Journal of medicinal chemistry, Oct-20, Volume: 48, Issue:21
Designed multiple ligands. An emerging drug discovery paradigm.
AID130468Antiallergic activity was evaluated using active anaphylactic test after po administration in mice1994Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17
[(3-Pyridylalkyl)piperidylidene]benzocycloheptapyridine derivatives as dual antagonists of PAF and histamine.
AID139398Tested for effect on central nervous system in mice at 100 mg/kg peroral dose barbiturate-sleeping time (BST)1994Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17
[(3-Pyridylalkyl)piperidylidene]benzocycloheptapyridine derivatives as dual antagonists of PAF and histamine.
AID1569610Kinetic rate index, ratio of compound effect for displacement of [3H]levocetirizine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells at Ki measured after 6 hrs to compound effect for displacement of [3H]levocetirizine from N-termi2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Route to Prolonged Residence Time at the Histamine H
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (107)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's3 (2.80)18.2507
2000's33 (30.84)29.6817
2010's50 (46.73)24.3611
2020's21 (19.63)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 78.92

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 Index78.92 (24.57)
Research Supply Index5.08 (2.92)
Research Growth Index5.51 (4.65)
Search Engine Demand Index135.80 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (78.92)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials43 (37.07%)5.53%
Reviews17 (14.66%)6.00%
Case Studies4 (3.45%)4.05%
Observational2 (1.72%)0.25%
Other50 (43.10%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]