Page last updated: 2024-12-05

benzydamine

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Description

Benzydamine is a non-steroidal anti-inflammatory drug (NSAID) with analgesic and antipyretic properties. It is structurally related to the benzodiazepines, but it does not possess any psychoactive effects. Benzydamine is typically used to treat pain and inflammation associated with musculoskeletal conditions, such as arthritis and sprains. The mechanism of action of benzydamine is believed to involve inhibition of cyclooxygenase (COX) enzymes, which are involved in the production of prostaglandins, inflammatory mediators. Benzydamine is also thought to have a direct effect on nerve endings, reducing pain transmission. It is commonly available in various forms, including tablets, capsules, topical creams, and gels. Benzydamine has been studied extensively for its efficacy and safety in treating various inflammatory conditions. Research has demonstrated its effectiveness in reducing pain and inflammation in conditions such as osteoarthritis, rheumatoid arthritis, and post-surgical pain. The compound has also shown promise in treating other inflammatory conditions, such as inflammatory bowel disease and migraine headaches. Further studies are ongoing to investigate the full therapeutic potential of benzydamine and explore its potential applications in other areas of medicine.'
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Benzydamine: A benzyl-indazole having analgesic, antipyretic, and anti-inflammatory effects. It is used to reduce post-surgical and post-traumatic pain and edema and to promote healing. It is also used topically in treatment of RHEUMATIC DISEASES and INFLAMMATION of the mouth and throat. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

benzydamine : A member of the class of indazoles carrying benzyl and 3-(dimethylamino)propyl groups at positions 1 and 3 respectively. A locally-acting nonsteroidal anti-inflammatory drug that also exhibits local anaesthetic and analgesic properties. [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 CID12555
CHEMBL ID12610
CHEBI ID94563
SCHEMBL ID26172
MeSH IDM0002384

Synonyms (73)

Synonym
AC-15604
{3-[(1-benzyl-1h-indazol-3-yl)oxy]propyl}dimethylamine
BRD-K28542495-003-03-6
1h-indazole, 1-benzyl-3-(3-(dimethylamino)propoxy)-
1-propanamine, n,n-dimethyl-3-[[1-(phenylmethyl)-1h-indazol-3-yl]oxy]-
BSPBIO_000234
PRESTWICK3_000297
brn 0896536
c 1523
1-propanamine, n,n-dimethyl-3-((1-(phenylmethyl)-1h-indazol-3-yl)oxy)-
einecs 211-388-8
benzydaminum [inn-latin]
benzydamine
benzidamina [dcit]
bencidamina [inn-spanish]
benzidamine
benzydamine [inn:ban]
1-benzyl-3-(3-(dimethylamino)propoxy)-1h-indazole
NCGC00016397-01
cas-132-69-4
PRESTWICK2_000297
D07516
benzydamine (inn)
apo-benzydamine (tn)
642-72-8
BPBIO1_000258
SPBIO_002453
PRESTWICK1_000297
PRESTWICK0_000297
NCGC00016397-02
benzindamine
HMS2090P22
3-(1-benzylindazol-3-yl)oxy-n,n-dimethylpropan-1-amine
CHEMBL12610
apo-benzydamine
STK711092
3-[(1-benzyl-1h-indazol-3-yl)oxy]-n,n-dimethylpropan-1-amine
BBL009932
AKOS005530662
benzydaminum
4o21u048ef ,
unii-4o21u048ef
benzidamina
bencidamina
5-23-11-00248 (beilstein handbook reference)
benzydamine [mi]
benzydamine [who-dd]
benzydamine [inn]
1-benzyl-1h-indazol-3-yl 3-(dimethylamino)propyl ether
n,n-dimethyl-3-((1-(phenylmethyl)-1h-indazol-3-yl)oxy)-1-propanamine
BRD-K28542495-001-01-4
SCHEMBL26172
DTXSID7047859
1benzyl-3-[3-(dimethylamino)propoxy]-1h-indazole
benzydamide
n-(3-[(1-benzyl-1h-indazol-3-yl)oxy]propyl)-n,n-dimethylamine #
DB09084
1-benzyl-3-[3-(dimethylamino)propoxy]-1h-indazole
SR-01000799149-2
sr-01000799149
CHEBI:94563
n,n-dimethyl-3-[[1-(phenylmethyl)-3-indazolyl]oxy]-1-propanamine
3-[(1-benzyl-1h-indazol-3-yl)oxy]-n,n-dimethylpropan-1-aminie
bdbm50103598
SBI-0206866.P001
NCGC00016397-07
3-(1-benzyl-1h-indazol-3-yloxy)-n,n-dimethylpropan-1-amine
FT-0740906
Q793143
BRD-K28542495-003-07-7
SB16913
2-{[(2-methoxyethyl)amino]-carbonyl}cyclohexanecarboxylicacid
EN300-12576563

Research Excerpts

Overview

Benzydamine is an active pharmaceutical compound used in the oral care pharmaceutical preparation as NSAID. It has analgesic, local anesthetic, and anti-inflammatory effects that have been known to be effective in reducing postoperative sore throat.

ExcerptReferenceRelevance
"Benzydamine hydrochloride is a locally-acting Non-Steroidal Anti-Inflammatory Drug (NSAID) with combined local anesthetic and analgesic properties, indicated for the symptomatic relief of pain in acute sore throat. "( International Delphi-based consensus on the appropriate use and effect of Benzydamine hydrochloride in the treatment of sore throat.
Barat, V; Cadevall, O; Freire, HM; Grattagliano, I; Gutu, I; Mösges, R; Passali, D; Pavlysh, A, 2022
)
2.39
"Benzydamine is an active pharmaceutical compound used in the oral care pharmaceutical preparation as NSAID. "( Benzydamine plays a role in limiting inflammatory pain induced by neuronal sensitization.
Devesa, I; Espinosa, A; Ferrer-Montiel, A; Mangano, G; Nikolaeva-Koleva, M; Polenzani, L; Ragni, L; Vergassola, M; Zucchi, S,
)
3.02
"Benzydamine hydrochloride is a topical non-steroidal anti-inflammatory drug that has analgesic, local anesthetic, and anti-inflammatory effects that have been known to be effective in reducing postoperative sore throat."( Effectivity of benzydamine hydrochloride gargle to reduce propofol consumption in endoscopic retrograde cholangiopancreatography procedure: a randomized controlled trial.
Chrisnata, V; Kapuangan, C; Sugiarto, A; Tantri, AR, 2020
)
1.63
"Benzydamine is a local anti-inflammatory drug with analgesic properties. "( The role of benzydamine in prevention and treatment of chemoradiotherapy-induced mucositis.
Bossi, P; Nicolatou-Galitis, O; Orlandi, E, 2021
)
2.44
"Benzydamine is a non-steroidal anti-inflammatory and antiseptic drug which is used for treatment of vaginal infections."( Development and characterization of chitosan nanoparticles loaded nanofiber hybrid system for vaginal controlled release of benzydamine.
Acartürk, F; Kara, AA; Saar, S; Tuğcu-Demiröz, F; Tunçel, E; Yıldız, A, 2021
)
1.55
"Benzydamine (BZY) is a non-steroidal anti-inflammatory drug used for the topical treatment of inflammations of the oral and vaginal mucosae. "( Intravenous self-administration of benzydamine, a non-steroidal anti-inflammatory drug with a central cannabinoidergic mechanism of action.
Avvisati, R; Badiani, A; Malavasi, E; Marinelli, S; Meringolo, M; Stendardo, E, 2018
)
2.2
"Benzydamine hydrochloride is a non-steroidal anti-inflammatory drug available for topical use."( Topical benzydamine hydrochloride for prevention of postoperative sore throat in adults undergoing tracheal intubation for elective surgery: a systematic review and meta-analysis.
Aga, M; Kuriyama, A; Maeda, H, 2018
)
1.64
"Benzydamine hydrochloride is a non-steroidal anti-inflammatory drug with analgesic and antipyretic effects. "( Chronic psychosis related to benzydamine hydrochloride abuse.
Cengiz, GF; Gürü, M; Kuru, E; Örsel, S; Şafak, Y,
)
1.87
"Benzydamine/Tantum Rosa is a drug for external use. "( [Analysis of online reports on the potential misuse of benzidamine].
Blaszko, U; Corazza, O; Davey, Z; Deluca, P; Di Melchiorre, G; Enea, A; Marchi, A; Schifano, F; Sferrazza, E,
)
1.57
"Benzydamine hydrochloride is a topically-applied non-steroidal anti-inflammatory drug (NSAID)."( Efficacy of benzydamine hydrochloride dripping at endotracheal tube cuff for prevention of postoperative sore throat.
Chanchayanon, T; Chokkijchai, K; Nimmaanrat, S, 2013
)
1.49
"Benzydamine is an anti-inflammatory drug that undergoes flavin-containing monooxygenase (FMO)-dependent metabolism to benzydamine N-oxide; however, benzydamine N-demethylation is also catalyzed by liver microsomes. "( Benzydamine N-oxygenation as an index for flavin-containing monooxygenase activity and benzydamine N-demethylation by cytochrome P450 enzymes in liver microsomes from rats, dogs, monkeys, and humans.
Kume, T; Shimizu, M; Taniguchi-Takizawa, T; Yamazaki, H, 2015
)
3.3
"Benzydamine is a non-steroidal antiinflammatory drug used as vaginal lavage for non-specific vaginitis. "( Ingestions of benzydamine-containing vaginal preparations.
Ballesteros, S; Martínez-Arrieta, R; Ramón, MF, 2009
)
2.16
"Benzydamine is a nonsteroidal anti-inflammatory drug that undergoes flavin-containing monooxygenase (FMO)-dependent metabolism to a stable N-oxide. "( Benzydamine N-oxygenation as a measure of flavin-containing monooxygenase activity.
Rettie, AE; Yeung, CK, 2006
)
3.22
"Benzydamine HCL (Tantum) is a topical nonsteroidal anti-inflammatory drug (NSAID) with anti-inflammatory, analgesic, antipyretic and local anesthetic activity. "( Benzydamine Hydrochloride (Tantum) in the management of oral inflammatory conditions.
Turnbull, RS, 1995
)
3.18
"Benzydamine is a non-steroidal antiinflammatory drug, devoid of activity on arachidonic acid metabolism, which is extensively used as a topical drug in inflammatory conditions, particularly for the treatment of bacterial vaginosis and Candida albicans-sustained vaginitis. "( Benzydamine inhibits the release of tumor necrosis factor-alpha and monocyte chemotactic protein-1 by Candida albicans-stimulated human peripheral blood cells.
Coletta, I; Guglielmotti, A; Landolfi, C; Mantovani, A; Milanese, C; Pinza, M; Polenzani, L; Sironi, M; Soldo, L; Vecchi, A, 1997
)
3.18
"Benzydamine is a nonsteroidal anti-inflammatory drug, currently available as mouthwash, aerosol, dermal cream, vaginal douche preparation, pills and otic drops. "( Acute overdose due to benzydamine.
Gómez-López, L; Hernández-Rodríguez, J; Nogué, S; Pou, J, 1999
)
2.06
"Benzydamine is a well tolerated drug in patients with nimesulide-induced urticaria and it may represent a valid alternative NSAID in nimesulide-sensitive patients."( Benzydamine: an alternative nonsteroidal anti-inflammatory drug in patients with nimesulide-induced urticaria.
Di Paola, R; Ferrannini, A; Napoli, G; Nettis, E; Tursi, A, 2002
)
3.2
"Benzydamine (Tantum) is an indolic non-steroidal antiinflammatory drug (NSAID) for systemic use in acute traumatic lesions and locally as mouth gargle wash. "( [New pharmacologic and biochemical findings on the mechanism of action of the non-steroidal antiphlogistic, benzydamine. A synopsis].
Müller-Peddinghaus, R, 1987
)
1.93
"Benzydamine HCl is a new nonsteroidal analgesic and anti-inflammatory compound which is not chemically related to local anesthetics such as procaine and xylocaine. "( Benzydamine HCl, a new agent for the treatment of radiation mucositis of the oropharynx.
Chu, FC; Houde, R; Kim, JH; Lakshmi, V, 1986
)
3.16
"Benzydamine is an anti-inflammatory drug with unique medical uses, namely the topical treatment of oro-pharyngeal and gynaecological conditions. "( Benzydamine, an unique model of anti-inflammatory activity.
Silvestrini, B, 1987
)
3.16
"Benzydamine is a non-steroidal anti-inflammatory drug especially used topically for the treatment of primary or normoreactive types of inflammation. "( Pharmacokinetics of benzydamine.
Catanese, B; Kumakura, T; Schoenwald, RD, 1987
)
2.04

Effects

Benzydamine hydrochloride has similar efficacy to diclofenac potassium. It can be used as a nonsteroidal anti-inflammatory analgesic drug. Benzydamine has no effect on sulphydryl-group reactivity.

ExcerptReferenceRelevance
"Benzydamine hydrochloride has similar efficacy to diclofenac potassium, and it can be used as a nonsteroidal anti-inflammatory analgesic drug."( Comparison of Clinical Efficacies of Preoperatively Initiated Naproxen Sodium-Codeine Phosphate in Combination, Diclofenac Potassium, and Benzydamine Hydrochloride for Pain, Edema, and Trismus After Extraction of Impacted Lower Third Molar: A Randomized D
Cigerim, L; Eroglu, CN, 2018
)
1.4
"Benzydamine has recently been introduced for alleviating this condition."( The effect of chlorhexidine and benzydamine mouthwashes on mucositis induced by therapeutic irradiation.
Ferguson, MM; Hunter, IP; MacFarlane, G; MacFarlane, TW; Robertson, AG; Samaranayake, LP; Soutar, DS, 1988
)
1.28
"Benzydamine has no effect on sulphydryl-group reactivity, contrary to most NSAIDs."( Aspects of the mechanisms of action of benzydamine.
Hammarström, S; Segre, G, 1985
)
1.26

Actions

Benzydamine could suppress ESCC proliferation in vivo and in vitro. benzydamine can also cause hallucinations in infancy.

ExcerptReferenceRelevance
"Benzydamine could suppress ESCC proliferation in vivo and in vitro."( Repurposed benzydamine targeting CDK2 suppresses the growth of esophageal squamous cell carcinoma.
Chen, X; Dong, Z; Guo, Y; He, X; Jiang, Y; Li, J; Liu, K; Liu, Z; Wang, Z; Wu, W; Yu, Y; Zhang, C; Zhao, J; Zhou, Y, 2023
)
2.02
"benzydamine can also cause hallucinations in infancy."( [Non-delirious toxic psychoses in children (author's transl)].
Eggers, C, 1975
)
0.98

Toxicity

ExcerptReferenceRelevance
" Adverse drug-related effects reported included numbness of the tissues in the oral cavity, sensation of tingling in the tissues in the oral cavity, dry mouth, thirst, and nausea."( Efficacy and safety of ketoprofen lysine salt mouthwash versus benzydamine hydrochloride mouthwash in acute pharyngeal inflammation: a randomized, single-blind study.
Bellussi, L; Damiani, V; Passàli, D; Passàli, GC; Volonté, M, 2001
)
0.55
" Survival rates of flies used in the experiments were significantly lower than those of the control group, with both mouthwash products showing toxic effects on Drosophila melanogaster larvae."( Genotoxicity of two mouthwash products in the Drosophila Wing-Spot Test.
Erciyas, AF; Erciyas, K; Sarıkaya, R, 2010
)
0.36
"A survey questionnaire about the clinical experience with topical benzydamine and morphine to manage oral mucositis and their related adverse effects (AEs) was electronically distributed to the members of the Mucositis Study Group of MASCC/ISOO."( Clinicians' experience with topical benzydamine and morphine for the management of oral mucositis: adverse effects and barriers.
Blanchard, A; Bossi, P; Cheng, KKF; Elad, S; Levi, L; Yarom, N; Zadik, Y, 2022
)
1.23

Pharmacokinetics

Simulations of human plasma concentrations of benzydamine and its N-oxide were achieved. The bioavailability, pharmacokinetic parameters and excretion in milk of Benzydamine were evaluated.

ExcerptReferenceRelevance
" 1101); the apparent terminal half-life in plasma was ca."( Pharmacokinetics of benzydamine after intravenous, oral, and topical doses to human subjects.
Baldock, GA; Brodie, RR; Catanese, B; Chasseaud, LF; Taylor, T; Walmsley, LM, 1991
)
0.6
" The bioavailability, pharmacokinetic parameters and excretion in milk of benzydamine were evaluated."( Pharmacokinetics of benzydamine in dairy cows following intravenous or intramuscular administration.
Anfossi, P; Bolognini, M; Catraro, N; Malvisi, J; Stracciari, GL; Tomasi, L, 1993
)
0.84
" Simulations of human plasma concentrations of benzydamine and its N-oxide were achieved using simplified physiologically based pharmacokinetic models based on data from control TK-NOG mice and from reported benzydamine concentrations after low-dose administration in humans."( Human plasma metabolic profiles of benzydamine, a flavin-containing monooxygenase probe substrate, simulated with pharmacokinetic data from control and humanized-liver mice.
Mitsui, M; Nishiwaki, M; Shimizu, M; Suemizu, H; Yamazaki, H; Yamazaki-Nishioka, M, 2018
)
1.01

Bioavailability

Benzydamine was well absorbed after oral administration, as indicated by a mean systemic availability of 87 per cent. Oral doses of benzydamine are apparently well absorbed and plasma drug concentrations reach a peak fairly rapidly.

ExcerptReferenceRelevance
" Benzydamine was well absorbed after oral administration, as indicated by a mean systemic availability of 87 per cent."( Pharmacokinetics of benzydamine after intravenous, oral, and topical doses to human subjects.
Baldock, GA; Brodie, RR; Catanese, B; Chasseaud, LF; Taylor, T; Walmsley, LM, 1991
)
1.52
" Oral doses of benzydamine are apparently well absorbed and plasma drug concentrations reach a peak fairly rapidly (e."( Pharmacokinetics of benzydamine.
Catanese, B; Chasseaud, LF, 1985
)
0.95
" Benzydamine bioavailability was very high (92."( Pharmacokinetics of benzydamine in dairy cows following intravenous or intramuscular administration.
Anfossi, P; Bolognini, M; Catraro, N; Malvisi, J; Stracciari, GL; Tomasi, L, 1993
)
1.52
" Pharmacokinetic studies in rats showed that compound 32 exhibits modest oral bioavailability (12%)."( Synthesis and biological evaluation of novel pyrazoles and indazoles as activators of the nitric oxide receptor, soluble guanylate cyclase.
Brummell, DG; Budworth, J; Burtin, GE; Campbell, RO; Chana, SS; Charles, IG; Fernandez, PA; Glen, RC; Goggin, MC; Hobbs, AJ; Kling, MR; Liu, Q; Madge, DJ; Meillerais, S; Powell, KL; Reynolds, K; Selwood, DL; Spacey, GD; Stables, JN; Tatlock, MA; Wheeler, KA; Wishart, G; Woo, CK, 2001
)
0.31
" Compound 12 also shows 22% oral bioavailability in rats."( Solution-Phase parallel synthesis of 5-carboxamido 1-benzyl-3-(3-dimethylaminopropyloxy)-1H-pyrazoles as activators of soluble guanylate cyclase with improved oral bioavailability.
Brummell, DG; Glen, RC; Goggin, MC; Reynolds, K; Selwood, DL; Tatlock, MA; Wishart, G, 2001
)
0.31
"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
" In addition, the confirmed low bioavailability of the drugs excludes the possibility of any accumulation effects and limits the risk of undesired systemic effects."( Phase I Study in Healthy Women of a Novel Antimycotic Vaginal Ovule Combining Econazole and Benzydamine.
Bovi, G; Caccia, G; Comandini, A; Di Stefano, AFD; Focanti, F; Olivieri, S; Pelacchi, F; Picollo, R; Radicioni, MM; Rosignoli, MT; Salvatori, E; Vaccani, A, 2020
)
0.78

Dosage Studied

The aim of this work was the design of new mucoadhesive semisolid dosage forms for vaginal delivery of benzydamine. According to the online reports, Benzydamine is typically taken at a dosage of 1-4 sachets, dissolved in water and ingested orally. HPMC tablets could be a proper delivery system forBenzydamine administration.

ExcerptRelevanceReference
" We may conclude that this model is adequate and precise for selecting the most appropriate galenic dosage form for an active compound in terms of its clinical efficacy when topically administered."( UV-induced erythema model: a tool in dermatopharmacology for testing the topical activity of non-steroidal anti-inflammatory agents in man.
Barbanoj, MJ; Izquierdo, I; Jané, F; Lauroba, J; Moreno, J; Torrent, J, 1988
)
0.27
" The final conclusion of our study is that bendazac at a dosage ten-fold lower than that used in the clinics is anticataract drug when orally administered to "BLOA test selected" patients, at least for short term treatment of young, otherwise healthy humans with cortical cataract."( Bendazac and benzydamine for treatment of cataract: individualized therapy by the "BLOA test".
Buongiovanni, C; Iuliano, G; Marino, E; Mortow, P; Paolercio, F; Testa, M; Trapanese, A, 1986
)
0.64
" A dose-response curve of animal lethality versus endotoxin dose was performed (LD50 = 45 micrograms/mouse)."( Benzydamine protection in a mouse model of endotoxemia.
Aquilini, L; Coletta, I; Guglielmotti, A; Landolfi, C; Pinza, M; Rosignoli, MT; Soldo, L, 1997
)
1.74
"The aim of this work was the design of new mucoadhesive semisolid dosage forms for vaginal delivery of benzydamine."( Formulation studies of benzydamine mucoadhesive formulations for vaginal administration.
Ambrogi, V; Giovagnoli, S; Pagano, C; Perioli, L; Rossi, C; Venezia, L, 2009
)
0.88
" HPMC mucoadhesive tablets could be a proper delivery system for benzydamine administration representing a good alternative to traditional dosage forms for vaginal topical therapy."( New solid mucoadhesive systems for benzydamine vaginal administration.
Ambrogi, V; Massetti, E; Pagano, C; Perioli, L; Rossi, C, 2011
)
0.88
" According to the online reports, benzydamine is typically taken at a dosage of 1-4 sachets, dissolved in water and ingested orally."( [Analysis of online reports on the potential misuse of benzidamine].
Blaszko, U; Corazza, O; Davey, Z; Deluca, P; Di Melchiorre, G; Enea, A; Marchi, A; Schifano, F; Sferrazza, E,
)
0.41
" Further RCTs are required to overcome the limitations of heterogeneity and to determine the optimal dosage and application of BH for managing POST."( Benzydamine hydrochloride on postoperative sore throat: a meta-analysis of randomized controlled trials.
Chen, CY; Kuo, CJ; Lam, F; Lee, YW; Tam, KW, 2014
)
1.85
" However, before these agents are recommended for general use, large multicenter trials should be done exploring not only efficacy but also dose-response relationships and side effects."( Novel preoperative pharmacologic methods of preventing postoperative sore throat due to tracheal intubation.
Austin, PN; Kalil, DM; Silvestro, LS, 2014
)
0.4
" The modified printing method shows great promise in a compounding production of personalized film dosage forms, and brings in possibilities such as one step preparation of films with compartmented drugs and incorporation of taste masking or release control layers."( 3D printing of multilayered orodispersible films with in-process drying.
Elbl, J; Gajdziok, J; Kolarczyk, J, 2020
)
0.56
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (5)

RoleDescription
central nervous system stimulantAny drug that enhances the activity of the central nervous system.
non-steroidal anti-inflammatory drugAn anti-inflammatory drug that is not a steroid. In addition to anti-inflammatory actions, non-steroidal anti-inflammatory drugs have analgesic, antipyretic, and platelet-inhibitory actions. They act by blocking the synthesis of prostaglandins by inhibiting cyclooxygenase, which converts arachidonic acid to cyclic endoperoxides, precursors of prostaglandins.
hallucinogenDrugs capable of inducing illusions, hallucinations, delusions, paranoid ideations and other alterations of mood and thinking.
local anaestheticAny member of a group of drugs that reversibly inhibit the propagation of signals along nerves. Wide variations in potency, stability, toxicity, water-solubility and duration of action determine the route used for administration, e.g. topical, intravenous, epidural or spinal block.
analgesicAn agent capable of relieving pain without the loss of consciousness or without producing anaesthesia. In addition, analgesic is a role played by a compound which is exhibited by a capability to cause a reduction of pain symptoms.
[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
indazoles
aromatic etherAny ether in which the oxygen is attached to at least one aryl substituent.
tertiary amino compoundA compound formally derived from ammonia by replacing three hydrogen atoms by organyl groups.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (11)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency15.84890.177814.390939.8107AID2147
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency7.94330.00207.533739.8107AID891
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency5.48970.005612.367736.1254AID624032
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)Potency12.58930.316212.765731.6228AID881
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency12.58930.00638.235039.8107AID881
[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)
Cytochrome P450 2C9 Homo sapiens (human)IC50 (µMol)50.00000.00002.800510.0000AID1210069
Cytochrome P450 2J2Homo sapiens (human)IC50 (µMol)50.00000.01202.53129.4700AID1210069
[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)
Guanylate cyclase soluble subunit beta-2Homo sapiens (human)EC50 (µMol)1.02001.02001.02001.0200AID205476
Guanylate cyclase soluble subunit alpha-2Homo sapiens (human)EC50 (µMol)1.02001.02001.02001.0200AID205476
Guanylate cyclase soluble subunit alpha-1Homo sapiens (human)EC50 (µMol)1.02001.02001.02001.0200AID205476
Guanylate cyclase soluble subunit beta-1Homo sapiens (human)EC50 (µMol)1.02001.02001.02001.0200AID205476
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (52)

Processvia Protein(s)Taxonomy
lipid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
phospholipid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
apoptotic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of cell population proliferationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of macrophage derived foam cell differentiationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
arachidonic acid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of cell migrationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
prostate gland developmentPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
regulation of epithelial cell differentiationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of chemokine productionPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of peroxisome proliferator activated receptor signaling pathwayPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of keratinocyte differentiationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of cell cyclePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of growthPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
hepoxilin biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
endocannabinoid signaling pathwayPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cannabinoid biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipoxin A4 biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
linoleic acid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipid oxidationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipoxygenase pathwayPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cGMP biosynthetic processGuanylate cyclase soluble subunit beta-2Homo sapiens (human)
response to oxygen levelsGuanylate cyclase soluble subunit beta-2Homo sapiens (human)
cGMP-mediated signalingGuanylate cyclase soluble subunit beta-2Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2C9 Homo sapiens (human)
steroid metabolic processCytochrome P450 2C9 Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2C9 Homo sapiens (human)
estrogen metabolic processCytochrome P450 2C9 Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2C9 Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
urea metabolic processCytochrome P450 2C9 Homo sapiens (human)
monocarboxylic acid metabolic processCytochrome P450 2C9 Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2C9 Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
amide metabolic processCytochrome P450 2C9 Homo sapiens (human)
icosanoid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
oxidative demethylationCytochrome P450 2C9 Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
cGMP biosynthetic processGuanylate cyclase soluble subunit alpha-2Homo sapiens (human)
signal transductionGuanylate cyclase soluble subunit alpha-2Homo sapiens (human)
nitric oxide mediated signal transductionGuanylate cyclase soluble subunit alpha-2Homo sapiens (human)
positive regulation of nitric oxide mediated signal transductionGuanylate cyclase soluble subunit alpha-2Homo sapiens (human)
response to oxygen levelsGuanylate cyclase soluble subunit alpha-2Homo sapiens (human)
cGMP-mediated signalingGuanylate cyclase soluble subunit alpha-2Homo sapiens (human)
fatty acid metabolic processCytochrome P450 2J2Homo sapiens (human)
icosanoid metabolic processCytochrome P450 2J2Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2J2Homo sapiens (human)
regulation of heart contractionCytochrome P450 2J2Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2J2Homo sapiens (human)
linoleic acid metabolic processCytochrome P450 2J2Homo sapiens (human)
organic acid metabolic processCytochrome P450 2J2Homo sapiens (human)
cGMP biosynthetic processGuanylate cyclase soluble subunit alpha-1Homo sapiens (human)
nitric oxide mediated signal transductionGuanylate cyclase soluble subunit alpha-1Homo sapiens (human)
blood circulationGuanylate cyclase soluble subunit alpha-1Homo sapiens (human)
regulation of blood pressureGuanylate cyclase soluble subunit alpha-1Homo sapiens (human)
positive regulation of nitric oxide mediated signal transductionGuanylate cyclase soluble subunit alpha-1Homo sapiens (human)
nitric oxide-cGMP-mediated signalingGuanylate cyclase soluble subunit alpha-1Homo sapiens (human)
relaxation of vascular associated smooth muscleGuanylate cyclase soluble subunit alpha-1Homo sapiens (human)
retrograde trans-synaptic signaling by nitric oxide, modulating synaptic transmissionGuanylate cyclase soluble subunit alpha-1Homo sapiens (human)
response to oxygen levelsGuanylate cyclase soluble subunit alpha-1Homo sapiens (human)
cGMP-mediated signalingGuanylate cyclase soluble subunit alpha-1Homo sapiens (human)
cGMP biosynthetic processGuanylate cyclase soluble subunit beta-1Homo sapiens (human)
nitric oxide mediated signal transductionGuanylate cyclase soluble subunit beta-1Homo sapiens (human)
blood circulationGuanylate cyclase soluble subunit beta-1Homo sapiens (human)
nitric oxide-cGMP-mediated signalingGuanylate cyclase soluble subunit beta-1Homo sapiens (human)
cellular response to nitric oxideGuanylate cyclase soluble subunit beta-1Homo sapiens (human)
trans-synaptic signaling by nitric oxide, modulating synaptic transmissionGuanylate cyclase soluble subunit beta-1Homo sapiens (human)
cGMP-mediated signalingGuanylate cyclase soluble subunit beta-1Homo sapiens (human)
response to oxygen levelsGuanylate cyclase soluble subunit beta-1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (33)

Processvia Protein(s)Taxonomy
iron ion bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
calcium ion bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
protein bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipid bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
linoleate 13S-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
arachidonate 8(S)-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
arachidonate 15-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
linoleate 9S-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
GTP bindingGuanylate cyclase soluble subunit beta-2Homo sapiens (human)
heme bindingGuanylate cyclase soluble subunit beta-2Homo sapiens (human)
metal ion bindingGuanylate cyclase soluble subunit beta-2Homo sapiens (human)
guanylate cyclase activityGuanylate cyclase soluble subunit beta-2Homo sapiens (human)
monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
iron ion bindingCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 14,15-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 11,12-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 7-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
caffeine oxidase activityCytochrome P450 2C9 Homo sapiens (human)
(R)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
aromatase activityCytochrome P450 2C9 Homo sapiens (human)
heme bindingCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2C9 Homo sapiens (human)
protein bindingGuanylate cyclase soluble subunit alpha-2Homo sapiens (human)
GTP bindingGuanylate cyclase soluble subunit alpha-2Homo sapiens (human)
heme bindingGuanylate cyclase soluble subunit alpha-2Homo sapiens (human)
guanylate cyclase activityGuanylate cyclase soluble subunit alpha-2Homo sapiens (human)
monooxygenase activityCytochrome P450 2J2Homo sapiens (human)
iron ion bindingCytochrome P450 2J2Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2J2Homo sapiens (human)
arachidonic acid 14,15-epoxygenase activityCytochrome P450 2J2Homo sapiens (human)
arachidonic acid 11,12-epoxygenase activityCytochrome P450 2J2Homo sapiens (human)
isomerase activityCytochrome P450 2J2Homo sapiens (human)
linoleic acid epoxygenase activityCytochrome P450 2J2Homo sapiens (human)
hydroperoxy icosatetraenoate isomerase activityCytochrome P450 2J2Homo sapiens (human)
arachidonic acid 5,6-epoxygenase activityCytochrome P450 2J2Homo sapiens (human)
heme bindingCytochrome P450 2J2Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2J2Homo sapiens (human)
guanylate cyclase activityGuanylate cyclase soluble subunit alpha-1Homo sapiens (human)
protein bindingGuanylate cyclase soluble subunit alpha-1Homo sapiens (human)
GTP bindingGuanylate cyclase soluble subunit alpha-1Homo sapiens (human)
heme bindingGuanylate cyclase soluble subunit alpha-1Homo sapiens (human)
signaling receptor activityGuanylate cyclase soluble subunit alpha-1Homo sapiens (human)
adenylate cyclase activityGuanylate cyclase soluble subunit beta-1Homo sapiens (human)
guanylate cyclase activityGuanylate cyclase soluble subunit beta-1Homo sapiens (human)
protein bindingGuanylate cyclase soluble subunit beta-1Homo sapiens (human)
GTP bindingGuanylate cyclase soluble subunit beta-1Homo sapiens (human)
heme bindingGuanylate cyclase soluble subunit beta-1Homo sapiens (human)
signaling receptor activityGuanylate cyclase soluble subunit beta-1Homo sapiens (human)
protein-containing complex bindingGuanylate cyclase soluble subunit beta-1Homo sapiens (human)
metal ion bindingGuanylate cyclase soluble subunit beta-1Homo sapiens (human)
cytidylate cyclase activityGuanylate cyclase soluble subunit beta-1Homo sapiens (human)
Hsp90 protein bindingGuanylate cyclase soluble subunit beta-1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (15)

Processvia Protein(s)Taxonomy
nucleusPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cytosolPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cytoskeletonPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
plasma membranePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
adherens junctionPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
focal adhesionPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
membranePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
extracellular exosomePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cytosolGuanylate cyclase soluble subunit beta-2Homo sapiens (human)
guanylate cyclase complex, solubleGuanylate cyclase soluble subunit beta-2Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2C9 Homo sapiens (human)
plasma membraneCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
cytoplasmCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
cytosolGuanylate cyclase soluble subunit alpha-2Homo sapiens (human)
guanylate cyclase complex, solubleGuanylate cyclase soluble subunit alpha-2Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2J2Homo sapiens (human)
extracellular exosomeCytochrome P450 2J2Homo sapiens (human)
cytoplasmCytochrome P450 2J2Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2J2Homo sapiens (human)
cytosolGuanylate cyclase soluble subunit alpha-1Homo sapiens (human)
guanylate cyclase complex, solubleGuanylate cyclase soluble subunit alpha-1Homo sapiens (human)
glutamatergic synapseGuanylate cyclase soluble subunit alpha-1Homo sapiens (human)
GABA-ergic synapseGuanylate cyclase soluble subunit alpha-1Homo sapiens (human)
cytosolGuanylate cyclase soluble subunit beta-1Homo sapiens (human)
guanylate cyclase complex, solubleGuanylate cyclase soluble subunit beta-1Homo sapiens (human)
presynaptic active zone cytoplasmic componentGuanylate cyclase soluble subunit beta-1Homo sapiens (human)
glutamatergic synapseGuanylate cyclase soluble subunit beta-1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (30)

Assay IDTitleYearJournalArticle
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
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.
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.
AID1347160Primary screen NINDS Rhodamine 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.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings 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.
AID781326pKa (acid-base dissociation constant) as determined by Avdeef ref: DOI: 10.1002/047145026X2014Pharmaceutical research, Apr, Volume: 31, Issue:4
Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds.
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).
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).
AID567091Drug absorption in human assessed as human intestinal absorption rate2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Prediction of drug intestinal absorption by new linear and non-linear QSPR.
AID1210069Inhibition of human recombinant CYP2J2 assessed as reduction in astemizole O-demethylation by LC-MS/MS method2013Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1
Discovery and characterization of novel, potent, and selective cytochrome P450 2J2 inhibitors.
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).
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).
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).
AID625291Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625280Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1739434Metabolic stability in human liver microsomes assessed as intrinsic clearance at 100 uM measured per mg protein upto 30 mins2020European journal of medicinal chemistry, Aug-15, Volume: 200Substituted benzothiophene and benzofuran derivatives as a novel class of bone morphogenetic Protein-2 upregulators: Synthesis, anti-osteoporosis efficacies in ovariectomized rats and a zebrafish model, and ADME properties.
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).
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).
AID228807Activation of bovine sGC Enzyme (soluble Guanylate Cyclase) in Sf21 cells infected with baculo virus in the presence of 30 nM of PAPA/NO2001Journal of medicinal chemistry, Jan-04, Volume: 44, Issue:1
Synthesis and biological evaluation of novel pyrazoles and indazoles as activators of the nitric oxide receptor, soluble guanylate cyclase.
AID205476The cGMP produced by compound was expressed as a ratio between the percentage of the DEA/NO response for the compound2001Bioorganic & medicinal chemistry letters, Apr-23, Volume: 11, Issue:8
Solution-Phase parallel synthesis of 5-carboxamido 1-benzyl-3-(3-dimethylaminopropyloxy)-1H-pyrazoles as activators of soluble guanylate cyclase with improved oral bioavailability.
AID92973Concentration required to inhibit collagen-induced platelet aggregation by 50%2001Journal of medicinal chemistry, Jan-04, Volume: 44, Issue:1
Synthesis and biological evaluation of novel pyrazoles and indazoles as activators of the nitric oxide receptor, soluble guanylate cyclase.
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).
AID1739433Metabolic stability in human liver microsomes assessed as half life at 100 uM measured upto 30 mins2020European journal of medicinal chemistry, Aug-15, Volume: 200Substituted benzothiophene and benzofuran derivatives as a novel class of bone morphogenetic Protein-2 upregulators: Synthesis, anti-osteoporosis efficacies in ovariectomized rats and a zebrafish model, and ADME properties.
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).
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).
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).
AID228809Bovine sGC stimulation measured as relative enzyme activity (percentage of DEA/NO response for the compound to compound 3)2001Journal of medicinal chemistry, Jan-04, Volume: 44, Issue:1
Synthesis and biological evaluation of novel pyrazoles and indazoles as activators of the nitric oxide receptor, soluble guanylate cyclase.
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).
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (362)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990141 (38.95)18.7374
1990's46 (12.71)18.2507
2000's58 (16.02)29.6817
2010's83 (22.93)24.3611
2020's34 (9.39)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 70.22

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 Index70.22 (24.57)
Research Supply Index6.21 (2.92)
Research Growth Index4.59 (4.65)
Search Engine Demand Index171.20 (26.88)
Search Engine Supply Index2.80 (0.95)

This Compound (70.22)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials108 (27.91%)5.53%
Reviews30 (7.75%)6.00%
Case Studies31 (8.01%)4.05%
Observational0 (0.00%)0.25%
Other218 (56.33%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (20)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
The Effect Of Two Packing Types For Throat Pain And Postoperative Nausea And Vomiting During Maxillofacial Surgery [NCT03574246]Phase 4111 participants (Actual)Interventional2018-01-10Completed
A Phase 1/Phase 2 Study for the Prevention of Oral Mucositis (SPOM) [NCT05338398]Phase 1/Phase 2100 participants (Anticipated)Interventional2022-04-15Enrolling by invitation
A Phase I Study of a Novel Mouthwash Formulation (Cetylpyridinium Chloride 0.05% + Benzydamine HCl 0.15% + Mucus - Adhesive Polymer) Administered Twice a Day for 7 Days to Healthy Subjects in Comparison With Marketed Tantum Verde Bocca Mouthwash Solution [NCT03706781]Phase 126 participants (Actual)Interventional2017-11-14Completed
Evaluation of the Effects of Different Analgesics on Pain and Health-related Quality of Life of Patients With Pericoronitis in the Short-term Period: A Randomized, Double-blind, Clinical Trial [NCT03745599]Phase 460 participants (Actual)Interventional2017-11-01Completed
Effect of Over-the-counter Non-steroidal Anti-inflammatory Treatments on Cough Reflex Sensitivity in Subjects With Upper Respiratory Tract Infection [NCT05955885]Early Phase 1120 participants (Anticipated)Interventional2023-07-01Recruiting
The Use of Tulsi Extract for The Management of Oral Mucositis in Head & Neck Cancer Patients Undergoing Radiotherapy: A Randomized Clinical Trial [NCT05323058]Phase 242 participants (Anticipated)Interventional2022-07-31Not yet recruiting
Effect of Benzydamine Hydrochloride to Postoperative Sore Throat in Pediatric Patients: a Randomized Controlled Trial [NCT03074968]Phase 4142 participants (Actual)Interventional2017-03-08Completed
Phase IV Study Comparing the Efficacy and Safety of Benzydamine Hydrochloride 0,3% Oromucosal Spray and Benzydamine Hydrochloride 3 mg Lozenges in Patients With Acute Sore Throat [NCT04941976]Phase 4356 participants (Actual)Interventional2020-08-13Completed
Clinical Evaluation of Solcosreyl and Pumpkin Seed Oil Versus Benzydamine Hydrochloride in Management of Patients With Chemotherapy and Radiotherapy Induced Oral Mucositis [NCT04303312]Phase 354 participants (Anticipated)Interventional2021-12-31Not yet recruiting
"MISTRAL (Mouthwash In Sore Throat Relief: Antiinflammatory vs. Local Anesthetic Therapy) Efficacy and Tolerability of Ketoprofen Lysine Salt as a Mouthwash in Acute Phlogosis of the Pharyngeal Cavity; Multicentre, Randomized, Single-blind, Parallel-group [NCT02178293]Phase 4214 participants (Actual)Interventional1998-09-30Completed
A Phase III Study of Magic Mouthwash Plus Sucralfate Versus Benzydamine HCl for Treatment of Radiation-induced Oral Mucositis in Head and Neck Cancer Patients. [NCT00814359]Phase 367 participants (Actual)Interventional2009-05-31Completed
A Phase I Study of a Novel Antimycotic Vaginal Pessary Formulation (Econazole Nitrate 150 mg + Benzydamine HCl 6 mg) Administered Once Daily for 3 Days to Healthy Women [NCT02720783]Phase 149 participants (Actual)Interventional2016-03-04Completed
Phase IV Study on the Feasibility of a Preventative/Therapeutic Approach With Benzydamine Oromucosal Solution in Radiation-induced Oral Mucositis (OM) in Patients With Head and Neck Cancer (HNC) [NCT05055726]Phase 4100 participants (Actual)Interventional2021-12-06Completed
Effectivity of Benzydamine Hydrochloride Gargle to Reduce Propofol Consumption in Endoscopic Retrograde Cholangiopancreatography Procedure [NCT04167592]72 participants (Actual)Interventional2018-08-01Completed
A Phase I Study of a Novel Intravaginal Antimycotic Cream (Econazole Nitrate 1% Plus Benzydamine HCl 0.12%) Administered Once Daily for 15 Days to Healthy Women [NCT02713893]Phase 148 participants (Actual)Interventional2015-09-30Completed
Efficacy of Natural Enzymes Mouthwash: a Randomised Controlled Trial [NCT05640362]48 participants (Actual)Interventional2016-11-10Completed
A Double-Blind, Randomized, Vehicle-Controlled Study Comparing the Safety and Efficacy of Benzydamine HCl 0.15% Oral Rinse Including a Separate Open-Label Standard of Care Arm in Subjects With Radiation-Induced Mucositis [NCT00051441]Phase 3605 participants (Actual)InterventionalCompleted
Efficacy of Benzydamine Hydrochloride Dripping at Endotracheal Tube Cuff for Prevention of Postoperative Sore Throat [NCT01637883]Phase 386 participants (Anticipated)Interventional2011-01-31Recruiting
''Comparison of Preoperative Aspirin and Benzydamine Hydrochloride Gargles on Reduction in Severity and Duration of Post-Operative Sore Throat. A Randomized Controlled Parallel Study.'' [NCT05343429]Phase 460 participants (Anticipated)Interventional2022-04-01Recruiting
Effect of St. John's Wort Oil and Olive Oil on the Postoperative Complications After Impacted Third Molar Surgery: Randomized, Double-blind Clinical Trial [NCT04373421]Phase 490 participants (Actual)Interventional2018-08-15Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT04373421 (20) [back to overview]Postoperative Jaw Function
NCT04373421 (20) [back to overview]Postoperative Jaw Function
NCT04373421 (20) [back to overview]Postoperative Jaw Function
NCT04373421 (20) [back to overview]Postoperative Jaw Function
NCT04373421 (20) [back to overview]Postoperative Jaw Function
NCT04373421 (20) [back to overview]Postoperative Jaw Function
NCT04373421 (20) [back to overview]Postoperative Jaw Function
NCT04373421 (20) [back to overview]Postoperative Pain
NCT04373421 (20) [back to overview]Postoperative Pain
NCT04373421 (20) [back to overview]Postoperative Pain
NCT04373421 (20) [back to overview]Postoperative Pain
NCT04373421 (20) [back to overview]Postoperative Pain
NCT04373421 (20) [back to overview]Postoperative Pain
NCT04373421 (20) [back to overview]Postoperative Pain
NCT04373421 (20) [back to overview]Postoperative Swelling
NCT04373421 (20) [back to overview]Postoperative Swelling
NCT04373421 (20) [back to overview]Postoperative Swelling
NCT04373421 (20) [back to overview]Postoperative Trismus
NCT04373421 (20) [back to overview]Postoperative Trismus
NCT04373421 (20) [back to overview]Postoperative Trismus

Postoperative Jaw Function

For the assessment of difficulty during jaw function, patients were asked to rate it on a 100-mm VAS, wherein 0 indicated no limitation and 100 indicated severe limitation. (NCT04373421)
Timeframe: Postoperatif 1st day

Interventionscore on a scale (Mean)
Chlorhexidine Gluconate Plus Benzydamine Hydrochloride61.5
St. John's Wort Oil63.9
Virgin Olive Oil65.9

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Postoperative Jaw Function

For the assessment of difficulty during jaw function, patients were asked to rate it on a 100-mm VAS, wherein 0 indicated no limitation and 100 indicated severe limitation. (NCT04373421)
Timeframe: Postoperatif 2nd day

Interventionscore on a scale (Mean)
Chlorhexidine Gluconate Plus Benzydamine Hydrochloride55.8
St. John's Wort Oil51.9
Virgin Olive Oil62.0

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Postoperative Jaw Function

For the assessment of difficulty during jaw function, patients were asked to rate it on a 100-mm VAS, wherein 0 indicated no limitation and 100 indicated severe limitation. (NCT04373421)
Timeframe: Postoperatif 3rd day

Interventionscore on a scale (Mean)
Chlorhexidine Gluconate Plus Benzydamine Hydrochloride47.8
St. John's Wort Oil42.5
Virgin Olive Oil47.2

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Postoperative Jaw Function

For the assessment of difficulty during jaw function, patients were asked to rate it on a 100-mm VAS, wherein 0 indicated no limitation and 100 indicated severe limitation. (NCT04373421)
Timeframe: Postoperatif 4th day

Interventionscore on a scale (Mean)
Chlorhexidine Gluconate Plus Benzydamine Hydrochloride44.4
St. John's Wort Oil36.6
Virgin Olive Oil35.1

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Postoperative Jaw Function

For the assessment of difficulty during jaw function, patients were asked to rate it on a 100-mm VAS, wherein 0 indicated no limitation and 100 indicated severe limitation. (NCT04373421)
Timeframe: Postoperatif 5th day

Interventionscore on a scale (Mean)
Chlorhexidine Gluconate Plus Benzydamine Hydrochloride29.5
St. John's Wort Oil26.1
Virgin Olive Oil28.6

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Postoperative Jaw Function

For the assessment of difficulty during jaw function, patients were asked to rate it on a 100-mm VAS, wherein 0 indicated no limitation and 100 indicated severe limitation. (NCT04373421)
Timeframe: Postoperatif 6th day

Interventionscore on a scale (Mean)
Chlorhexidine Gluconate Plus Benzydamine Hydrochloride19.5
St. John's Wort Oil21.4
Virgin Olive Oil20.6

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Postoperative Jaw Function

For the assessment of difficulty during jaw function, patients were asked to rate it on a 100-mm VAS, wherein 0 indicated no limitation and 100 indicated severe limitation. (NCT04373421)
Timeframe: Postoperatif 7th day

Interventionscore on a scale (Mean)
Chlorhexidine Gluconate Plus Benzydamine Hydrochloride11.5
St. John's Wort Oil13.9
Virgin Olive Oil13.8

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Postoperative Pain

To record the level of pain, patients were instructed to rate it on a 100-mm visual analog scale (VAS) was used wherein 0 indicated no pain and 100 indicated the worst pain imaginable. (NCT04373421)
Timeframe: Postoperatif 1st day

Interventionscore on a scale (Mean)
Chlorhexidine Gluconate Plus Benzydamine Hydrochloride51.4
St. John's Wort Oil56.3
Virgin Olive Oil60.9

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Postoperative Pain

To record the level of pain, patients were instructed to rate it on a 100-mm visual analog scales (VAS) was used wherein 0 indicated no pain and 100 indicated the worst pain imaginable. (NCT04373421)
Timeframe: Postoperatif 2nd day

Interventionscore on a scale (Mean)
Chlorhexidine Gluconate Plus Benzydamine Hydrochloride44.5
St. John's Wort Oil44.1
Virgin Olive Oil55.8

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Postoperative Pain

To record the level of pain, patients were instructed to rate it on a 100-mm visual analog scales (VAS) was used wherein 0 indicated no pain and 100 indicated the worst pain imaginable. (NCT04373421)
Timeframe: Postoperatif 4th day

Interventionscore on a scale (Mean)
Chlorhexidine Gluconate Plus Benzydamine Hydrochloride33.6
St. John's Wort Oil30.3
Virgin Olive Oil30.4

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Postoperative Pain

To record the level of pain, patients were instructed to rate it on a 100-mm visual analog scales (VAS) was used wherein 0 indicated no pain and 100 indicated the worst pain imaginable. (NCT04373421)
Timeframe: Postoperatif 5th day

Interventionscore on a scale (Mean)
Chlorhexidine Gluconate Plus Benzydamine Hydrochloride22.0
St. John's Wort Oil17.7
Virgin Olive Oil26.3

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Postoperative Pain

To record the level of pain, patients were instructed to rate it on a 100-mm visual analog scales (VAS) was used wherein 0 indicated no pain and 100 indicated the worst pain imaginable. (NCT04373421)
Timeframe: Postoperatif 6th day

Interventionscore on a scale (Mean)
Chlorhexidine Gluconate Plus Benzydamine Hydrochloride16.3
St. John's Wort Oil15.5
Virgin Olive Oil19.0

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Postoperative Pain

To record the level of pain, patients were instructed to rate it on a 100-mm visual analog scales (VAS) was used wherein 0 indicated no pain and 100 indicated the worst pain imaginable. (NCT04373421)
Timeframe: Postoperatif 7th day

Interventionscore on a scale (Mean)
Chlorhexidine Gluconate Plus Benzydamine Hydrochloride10.5
St. John's Wort Oil10.7
Virgin Olive Oil9.6

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Postoperative Pain

To record the level of pain, patients were instructed to rate it on a 100-mm visual analog scales (VAS) was used wherein 0 indicated no pain and 100 indicated the worst pain imaginable.. (NCT04373421)
Timeframe: Postoperatif 3rd day

Interventionscore on a scale (Mean)
Chlorhexidine Gluconate Plus Benzydamine Hydrochloride36.2
St. John's Wort Oil31.6
Virgin Olive Oil40.6

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Postoperative Swelling

Facial swelling was assessed using a thread and millimeter ruler and averaged the following five measurements: Distance I (from the angle of the mandible to labial commissure); Distance II (from the angle of the mandible to the nasal border); Distance III (from the angle of the mandible to the external corner of the eye); Distance IV (from the angle of the mandible to tragus) and Distance V (from the angle of the mandible to soft pogonion). For evaluation of changes in the abovementioned distances during the postoperative period, the percentage of facial swelling was calculated by subtracting the preoperative measurements from the postoperative measurements then divided by the preoperative measurements and multiplied by 100. (NCT04373421)
Timeframe: Postoperative 1st day

Interventionpercent change (Mean)
Chlorhexidine Gluconate Plus Benzydamine Hydrochloride4.93
St. John's Wort Oil3.90
Virgin Olive Oil4.96

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Postoperative Swelling

Facial swelling was assessed using a thread and millimeter ruler and averaged the following five measurements: Distance I (from the angle of the mandible to labial commissure); Distance II (from the angle of the mandible to the nasal border); Distance III (from the angle of the mandible to the external corner of the eye); Distance IV (from the angle of the mandible to tragus) and Distance V (from the angle of the mandible to soft pogonion). For evaluation of changes in the abovementioned distances during the postoperative period, the percentage of facial swelling was calculated by subtracting the preoperative measurements from the postoperative measurements then divided by the preoperative measurements and multiplied by 100. (NCT04373421)
Timeframe: Postoperative 3rd day

Interventionpercentage of swelling (Mean)
Chlorhexidine Gluconate Plus Benzydamine Hydrochloride4.09
St. John's Wort Oil3.24
Virgin Olive Oil4.22

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Postoperative Swelling

Facial swelling was assessed using a thread and millimeter ruler and averaged the following five measurements: Distance I (from the angle of the mandible to labial commissure); Distance II (from the angle of the mandible to the nasal border); Distance III (from the angle of the mandible to the external corner of the eye); Distance IV (from the angle of the mandible to tragus) and Distance V (from the angle of the mandible to soft pogonion). For evaluation of changes in the abovementioned distances during the postoperative period, the percentage of facial swelling was calculated by subtracting the preoperative measurements from the postoperative measurements then divided by the preoperative measurements and multiplied by 100. (NCT04373421)
Timeframe: Postoperative 7th day

Interventionpercent change (Mean)
Chlorhexidine Gluconate Plus Benzydamine Hydrochloride2.66
St. John's Wort Oil1.58
Virgin Olive Oil2.30

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Postoperative Trismus

For evaluation of trismus, the percentage of difference in maximum mouth opening during the postoperative period (B) was calculated by subtracting the preoperative measurement (A) from the postoperative measurement then dividing by the preoperative measurement (A) and multiplying by 100 (percentage of difference = [B - A]/B × 100). (NCT04373421)
Timeframe: Postoperative 1st day

Interventionpercent change (Mean)
Chlorhexidine Gluconate Plus Benzydamine Hydrochloride30.1
St. John's Wort Oil28.7
Virgin Olive Oil28.1

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Postoperative Trismus

For evaluation of trismus, the percentage of difference in maximum mouth opening during the postoperative period (B) was calculated by subtracting the preoperative measurement (A) from the postoperative measurement then dividing by the preoperative measurement (A) and multiplying by 100 (percentage of difference = [B - A]/B × 100). (NCT04373421)
Timeframe: Postoperative 3rd day

Interventionpercent change (Mean)
Chlorhexidine Gluconate Plus Benzydamine Hydrochloride33.8
St. John's Wort Oil32.4
Virgin Olive Oil31.6

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Postoperative Trismus

For evaluation of trismus, the percentage of difference in maximum mouth opening during the postoperative period (B) was calculated by subtracting the preoperative measurement (A) from the postoperative measurement then dividing by the preoperative measurement (A) and multiplying by 100 (percentage of difference = [B - A]/B × 100). (NCT04373421)
Timeframe: Postoperative 7th day

Interventionpercent change (Mean)
Chlorhexidine Gluconate Plus Benzydamine Hydrochloride38.7
St. John's Wort Oil38.3
Virgin Olive Oil36.7

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