Compounds > flesinoxan
Page last updated: 2024-09-23

flesinoxan

Cross-References

ID SourceID
PubMed CID57347
CHEMBL ID1742477
SCHEMBL ID220401
MeSH IDM0159436

Synonyms (25)

Synonym
(+)-flesinoxan
gtpl1
4-fluoro-n-[2-[4-[(3s)-3-(hydroxymethyl)-2,3-dihydro-1,4-benzodioxin-8-yl]piperazin-1-yl]ethyl]benzamide
du-29,373
D02568 ,
flesinoxan (inn)
98206-10-1
benzamide, n-(2-(4-(2,3-dihydro-2-(hydroxymethyl)-1,4-benzodioxin-5-yl)-1-piperazinyl)ethyl)-4-fluoro-, (r)-
flesinoxan
benzamide, n-(2-(4-((2r)-2,3-dihydro-2-(hydroxymethyl)-1,4-benzodioxin-5-yl)-1-piperazinyl)ethyl)-4-fluoro-
(+)-(s)-p-fluoro-n-(2-(4-(2-(hydroxymethyl)-1,4-benzodioxan-5-yl)-1-piperazinyl)ethyl)benzamide
flesinoxan [inn]
PDSP2_000754
PDSP1_000766
4-fluoro-n-[2-[4-[(2s)-2-(hydroxymethyl)-2,3-dihydro-1,4-benzodioxin-5-yl]piperazin-1-yl]ethyl]benzamide
unii-3v574s89e1
3v574s89e1 ,
CHEMBL1742477
SCHEMBL220401
flesinoxan [mi]
NYSDRDDQELAVKP-SFHVURJKSA-N
bdbm50454759
(s)-4-fluoro-n-(2-(4-(2-(hydroxymethyl)-2,3-dihydrobenzo[b][1,4]dioxin-5-yl)piperazin-1-yl)ethyl)benzamide
Q5458730
4-fluoro-n-[2-[4-[2-(hydroxymethyl)-2,3-dihydro-1,4-benzodioxin-5-yl]piperazin-1-yl]ethyl]benzamide

Research Excerpts

Overview

ExcerptReference
"Flesinoxan is a highly potent and selective 5-HT(1A) agonist and appears to be a potentially interesting neuroendocrine serotonergic probe."( Ansseau, M; Fuchs, S; Hansenne, M; Legros, JJ; Pinto, E; Pitchot, W; Reggers, J; Wauthy, J, 2002)
"Flesinoxan is a highly potent and selective 5-HT1A agonist. "( Ansseau, M; Legros, JJ; Pitchot, W; Wauthy, J, 2004)
"Flesinoxan is a potent and selective 5-HT1A receptor agonist. "( Cole, JC; Davies, A; Rodgers, RJ, 1994)
"Flesinoxan is a high affinity and selective 5-hydroxytryptamine1A (5-HT1A) ligand which, unlike the 5-HT1A agonists of the azapirone class, does not generate 1-(2-pyrimidinyl)piperazine, an alpha 2-adrenoreceptor antagonist. "( Blier, P; de Montigny, C; Dennis, T; Hadrava, V; Ortemann, C, 1995)
"Flesinoxan is an example which is highly selective for the 5-HT1A receptor subtype."( Cryan, JF; Kelly, JP; Leonard, BE; Redmond, AM, 1997)
"Flesinoxan acts as a full 5-HT1A receptor agonist and displays anxiolytic and anti-depressant properties. "( Compaan, JC; De Kloet, ER; Meijer, OC; Olivier, B; Sibug, RM; Van der Gugten, J, 1998)

Treatment

ExcerptReference
"Flesinoxan-treated rats also exhibited higher plasma corticosterone levels than vehicle-treated animals, which suggests the involvement of corticotropin-releasing hormone (CRH) or vasopressin in the hypothalamus."( Compaan, JC; Groenink, L; Maes, RA; Olivier, B; van der Gugten, J, 1996)
"Flesinoxan pretreatment resulted in an attenuated response of plasma corticosterone levels and Fos-positive neurons in the paraventricular nucleus of the hypothalamus, but not in the central amygdala and the bed nucleus after a flesinoxan challenge."( Compaan, JC; Groenink, L; Maes, RA; Olivier, B; Van der Gugten, J, 1997)

Protein Targets (4)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
D(2) dopamine receptorRattus norvegicus (Norway rat)Ki0.14000.00000.437510.0000AID65108
[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)
5-hydroxytryptamine receptor 1AHomo sapiens (human)EC50 (µMol)0.00660.00010.25718.0000AID3904
Type-1 angiotensin II receptorHomo sapiens (human)EC50 (µMol)0.00660.00050.01350.0676AID3904
Type-2 angiotensin II receptorHomo sapiens (human)EC50 (µMol)0.00660.00660.03710.0676AID3904
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (62)

Processvia Protein(s)Taxonomy
behavioral fear response5-hydroxytryptamine receptor 1AHomo sapiens (human)
G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 1AHomo sapiens (human)
adenylate cyclase-inhibiting serotonin receptor signaling pathway5-hydroxytryptamine receptor 1AHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 1AHomo sapiens (human)
gamma-aminobutyric acid signaling pathway5-hydroxytryptamine receptor 1AHomo sapiens (human)
positive regulation of cell population proliferation5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of serotonin secretion5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of vasoconstriction5-hydroxytryptamine receptor 1AHomo sapiens (human)
exploration behavior5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of dopamine metabolic process5-hydroxytryptamine receptor 1AHomo sapiens (human)
serotonin metabolic process5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of hormone secretion5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of behavior5-hydroxytryptamine receptor 1AHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 1AHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of cell growthType-1 angiotensin II receptorHomo sapiens (human)
kidney developmentType-1 angiotensin II receptorHomo sapiens (human)
renin-angiotensin regulation of aldosterone productionType-1 angiotensin II receptorHomo sapiens (human)
maintenance of blood vessel diameter homeostasis by renin-angiotensinType-1 angiotensin II receptorHomo sapiens (human)
regulation of systemic arterial blood pressure by renin-angiotensinType-1 angiotensin II receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayType-1 angiotensin II receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayType-1 angiotensin II receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationType-1 angiotensin II receptorHomo sapiens (human)
Rho protein signal transductionType-1 angiotensin II receptorHomo sapiens (human)
positive regulation of macrophage derived foam cell differentiationType-1 angiotensin II receptorHomo sapiens (human)
regulation of vasoconstrictionType-1 angiotensin II receptorHomo sapiens (human)
calcium-mediated signalingType-1 angiotensin II receptorHomo sapiens (human)
positive regulation of phospholipase A2 activityType-1 angiotensin II receptorHomo sapiens (human)
low-density lipoprotein particle remodelingType-1 angiotensin II receptorHomo sapiens (human)
regulation of renal sodium excretionType-1 angiotensin II receptorHomo sapiens (human)
angiotensin-activated signaling pathwayType-1 angiotensin II receptorHomo sapiens (human)
regulation of cell population proliferationType-1 angiotensin II receptorHomo sapiens (human)
symbiont entry into host cellType-1 angiotensin II receptorHomo sapiens (human)
regulation of inflammatory responseType-1 angiotensin II receptorHomo sapiens (human)
positive regulation of inflammatory responseType-1 angiotensin II receptorHomo sapiens (human)
positive regulation of protein metabolic processType-1 angiotensin II receptorHomo sapiens (human)
cell chemotaxisType-1 angiotensin II receptorHomo sapiens (human)
phospholipase C-activating angiotensin-activated signaling pathwayType-1 angiotensin II receptorHomo sapiens (human)
blood vessel diameter maintenanceType-1 angiotensin II receptorHomo sapiens (human)
positive regulation of blood vessel endothelial cell proliferation involved in sprouting angiogenesisType-1 angiotensin II receptorHomo sapiens (human)
positive regulation of CoA-transferase activityType-1 angiotensin II receptorHomo sapiens (human)
positive regulation of reactive oxygen species metabolic processType-1 angiotensin II receptorHomo sapiens (human)
inflammatory responseType-1 angiotensin II receptorHomo sapiens (human)
blood vessel remodelingType-2 angiotensin II receptorHomo sapiens (human)
regulation of systemic arterial blood pressure by circulatory renin-angiotensinType-2 angiotensin II receptorHomo sapiens (human)
angiotensin-mediated vasodilation involved in regulation of systemic arterial blood pressureType-2 angiotensin II receptorHomo sapiens (human)
brain renin-angiotensin systemType-2 angiotensin II receptorHomo sapiens (human)
cell surface receptor signaling pathwayType-2 angiotensin II receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayType-2 angiotensin II receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway coupled to cGMP nucleotide second messengerType-2 angiotensin II receptorHomo sapiens (human)
brain developmentType-2 angiotensin II receptorHomo sapiens (human)
regulation of blood pressureType-2 angiotensin II receptorHomo sapiens (human)
negative regulation of heart rateType-2 angiotensin II receptorHomo sapiens (human)
negative regulation of cell growthType-2 angiotensin II receptorHomo sapiens (human)
positive regulation of phosphoprotein phosphatase activityType-2 angiotensin II receptorHomo sapiens (human)
regulation of metanephros sizeType-2 angiotensin II receptorHomo sapiens (human)
exploration behaviorType-2 angiotensin II receptorHomo sapiens (human)
nitric oxide-cGMP-mediated signalingType-2 angiotensin II receptorHomo sapiens (human)
angiotensin-activated signaling pathwayType-2 angiotensin II receptorHomo sapiens (human)
vasodilationType-2 angiotensin II receptorHomo sapiens (human)
negative regulation of blood vessel endothelial cell migrationType-2 angiotensin II receptorHomo sapiens (human)
positive regulation of DNA-templated transcriptionType-2 angiotensin II receptorHomo sapiens (human)
negative regulation of neurotrophin TRK receptor signaling pathwayType-2 angiotensin II receptorHomo sapiens (human)
neuron apoptotic processType-2 angiotensin II receptorHomo sapiens (human)
positive regulation of metanephric glomerulus developmentType-2 angiotensin II receptorHomo sapiens (human)
positive regulation of branching involved in ureteric bud morphogenesisType-2 angiotensin II receptorHomo sapiens (human)
positive regulation of extrinsic apoptotic signaling pathwayType-2 angiotensin II receptorHomo sapiens (human)
inflammatory responseType-2 angiotensin II receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (10)

Processvia Protein(s)Taxonomy
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 1AHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 1AHomo sapiens (human)
receptor-receptor interaction5-hydroxytryptamine receptor 1AHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 1AHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 1AHomo sapiens (human)
angiotensin type I receptor activityType-1 angiotensin II receptorHomo sapiens (human)
angiotensin type II receptor activityType-1 angiotensin II receptorHomo sapiens (human)
protein bindingType-1 angiotensin II receptorHomo sapiens (human)
bradykinin receptor bindingType-1 angiotensin II receptorHomo sapiens (human)
protein heterodimerization activityType-1 angiotensin II receptorHomo sapiens (human)
angiotensin type II receptor activityType-2 angiotensin II receptorHomo sapiens (human)
protein bindingType-2 angiotensin II receptorHomo sapiens (human)
receptor antagonist activityType-2 angiotensin II receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (4)

Processvia Protein(s)Taxonomy
plasma membrane5-hydroxytryptamine receptor 1AHomo sapiens (human)
synapse5-hydroxytryptamine receptor 1AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 1AHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 1AHomo sapiens (human)
plasma membraneType-1 angiotensin II receptorHomo sapiens (human)
membraneType-1 angiotensin II receptorHomo sapiens (human)
plasma membraneType-1 angiotensin II receptorHomo sapiens (human)
plasma membraneType-2 angiotensin II receptorHomo sapiens (human)
plasma membraneType-2 angiotensin II receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (29)

Assay IDTitleYearJournalArticle
AID3904Compound was tested for its potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells1998Bioorganic & medicinal chemistry letters, Sep-22, Volume: 8, Issue:18
Functional characteristics of a series of N4-substituted 1-(2,3-dihydro-1,4-benzodioxin-5-yl)piperazines as 5-HT1A receptor ligands. Structure-activity relationships.
AID3528Antagonistic efficacy was evaluated by adenylyl cyclase assay in CHO cells stably expressing the human 5-HT1A receptor1998Bioorganic & medicinal chemistry letters, Sep-22, Volume: 8, Issue:18
Functional characteristics of a series of N4-substituted 1-(2,3-dihydro-1,4-benzodioxin-5-yl)piperazines as 5-HT1A receptor ligands. Structure-activity relationships.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID4417Inhibition of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor of rat frontal cortex membranes1998Bioorganic & medicinal chemistry letters, Sep-22, Volume: 8, Issue:18
Functional characteristics of a series of N4-substituted 1-(2,3-dihydro-1,4-benzodioxin-5-yl)piperazines as 5-HT1A receptor ligands. Structure-activity relationships.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID678901TP_TRANSPORTER: increase in brain concentration in mdr1a(-/-) mouse2001European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences, Aug, Volume: 14, Issue:1
Active efflux of the 5-HT(1A) receptor agonist flesinoxan via P-glycoprotein at the blood-brain barrier.
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID65108In vitro displacement of [3H]spiperone from Dopamine receptor D2 binding site in rat striatum.1997Journal of medicinal chemistry, Jan-31, Volume: 40, Issue:3
5-HT1A-versus D2-receptor selectivity of flesinoxan and analogous N4-substituted N1-arylpiperazines.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID679246TP_TRANSPORTER: transepithelial transport (basal to apical) in MDR1-expressing LLC-PK1 cells2001European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences, Aug, Volume: 14, Issue:1
Active efflux of the 5-HT(1A) receptor agonist flesinoxan via P-glycoprotein at the blood-brain barrier.
AID3524Agonistic efficacy was evaluated by adenylyl cyclase assay in CHO cells stably expressing the human 5-HT1A receptor1998Bioorganic & medicinal chemistry letters, Sep-22, Volume: 8, Issue:18
Functional characteristics of a series of N4-substituted 1-(2,3-dihydro-1,4-benzodioxin-5-yl)piperazines as 5-HT1A receptor ligands. Structure-activity relationships.
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID4029Binding affinity was evaluated by determining in vitro displacement of [3H]8-OH-DPAT from the central 5-hydroxytryptamine 1A receptor recognition site in rat frontal cortex homogenate.1997Journal of medicinal chemistry, Jan-31, Volume: 40, Issue:3
5-HT1A-versus D2-receptor selectivity of flesinoxan and analogous N4-substituted N1-arylpiperazines.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID624210Agonists at Human 5-Hydroxytryptamine receptor 5-HT1A1998European journal of pharmacology, Aug-21, Volume: 355, Issue:2-3
Agonist and antagonist actions of antipsychotic agents at 5-HT1A receptors: a [35S]GTPgammaS binding study.
AID1345615Human 5-HT1A receptor (5-Hydroxytryptamine receptors)1998European journal of pharmacology, Aug-21, Volume: 355, Issue:2-3
Agonist and antagonist actions of antipsychotic agents at 5-HT1A receptors: a [35S]GTPgammaS binding study.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (150)

TimeframeStudies, This Drug (%)All Drugs %
pre-19907 (4.67)18.7374
1990's87 (58.00)18.2507
2000's50 (33.33)29.6817
2010's6 (4.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials11 (7.14%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other143 (92.86%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceDescriptionRelationhip StrengthStudiesTrialsClassesRoles
1-(2-methoxyphenyl)piperazine[no description available]medium10piperazines
phenylpiperazine[no description available]medium10
fluanisone[no description available]medium10aromatic ketone
eltoprazine[no description available]medium50
8-hydroxy-2-(di-n-propylamino)tetralin[no description available]medium530phenols;
tertiary amino compound;
tetralins		serotonergic antagonist
5-carboxamidotryptamine[no description available]medium40tryptamines
buspirone[no description available]medium90azaspiro compound;
N-alkylpiperazine;
N-arylpiperazine;
organic heteropolycyclic compound;
piperidones;
pyrimidines		anxiolytic drug;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
sedative;
serotonergic agonist
chlorpromazine[no description available]medium10organochlorine compound;
phenothiazines;
tertiary amine		anticoronaviral agent;
antiemetic;
dopaminergic antagonist;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
phenothiazine antipsychotic drug
haloperidol[no description available]medium20aromatic ketone;
hydroxypiperidine;
monochlorobenzenes;
organofluorine compound;
tertiary alcohol		antidyskinesia agent;
antiemetic;
dopaminergic antagonist;
first generation antipsychotic;
serotonergic antagonist
haloperidol[no description available]medium21aromatic ketone;
hydroxypiperidine;
monochlorobenzenes;
organofluorine compound;
tertiary alcohol		antidyskinesia agent;
antiemetic;
dopaminergic antagonist;
first generation antipsychotic;
serotonergic antagonist
methiothepin[no description available]medium30aryl sulfide;
dibenzothiepine;
N-alkylpiperazine;
tertiary amino compound		antipsychotic agent;
dopaminergic antagonist;
geroprotector;
serotonergic antagonist
nan 190[no description available]medium50N-alkylpiperazine;
N-arylpiperazine;
phthalimides		serotonergic antagonist
quetiapine[no description available]medium10dibenzothiazepine;
N-alkylpiperazine;
N-arylpiperazine		adrenergic antagonist;
dopaminergic antagonist;
histamine antagonist;
second generation antipsychotic;
serotonergic antagonist
risperidone[no description available]medium101,2-benzoxazoles;
heteroarylpiperidine;
organofluorine compound;
pyridopyrimidine		alpha-adrenergic antagonist;
dopaminergic antagonist;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
H1-receptor antagonist;
psychotropic drug;
second generation antipsychotic;
serotonergic antagonist
spiperone[no description available]medium40aromatic ketone;
azaspiro compound;
organofluorine compound;
piperidines;
tertiary amino compound		alpha-adrenergic antagonist;
antipsychotic agent;
dopaminergic antagonist;
psychotropic drug;
serotonergic antagonist
spiroxatrine[no description available]medium10imidazolidines
thioridazine[no description available]medium10phenothiazines;
piperidines		alpha-adrenergic antagonist;
dopaminergic antagonist;
EC 1.8.1.12 (trypanothione-disulfide reductase) inhibitor;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
first generation antipsychotic;
H1-receptor antagonist;
serotonergic antagonist
n-(2-(4-(2-methoxyphenyl)-1-piperazinyl)ethyl)-n-(2-pyridinyl)cyclohexanecarboxamide[no description available]medium20piperazines
pimozide[no description available]medium10benzimidazoles;
heteroarylpiperidine;
organofluorine compound		antidyskinesia agent;
dopaminergic antagonist;
first generation antipsychotic;
H1-receptor antagonist;
serotonergic antagonist
butaclamol[no description available]medium10organic heteropentacyclic compound
tiospirone[no description available]medium10
ipsapirone[no description available]medium80N-arylpiperazine
sertindole[no description available]medium10heteroarylpiperidine;
imidazolidinone;
organochlorine compound;
organofluorine compound;
phenylindole		alpha-adrenergic antagonist;
H1-receptor antagonist;
second generation antipsychotic;
serotonergic antagonist
ziprasidone[no description available]medium201,2-benzisothiazole;
indolones;
organochlorine compound;
piperazines		antipsychotic agent;
dopaminergic antagonist;
histamine antagonist;
muscarinic antagonist;
psychotropic drug;
serotonergic antagonist
tandospirone[no description available]medium20bridged compound;
dicarboximide;
N-alkylpiperazine;
N-arylpiperazine;
pyrimidines		antidepressant;
anxiolytic drug
5-methoxy 3-(1,2,3,6-tetrahydro-4-pyridinyl)1h indole[no description available]medium50indoles
alpha-(4-fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazine butanol[no description available]medium10N-arylpiperazine
1-(2-(4-aminophenyl)ethyl)-4-(3-trifluoromethylphenyl)piperazine[no description available]medium20(trifluoromethyl)benzenes;
N-alkylpiperazine;
N-arylpiperazine;
primary arylamine;
substituted aniline		geroprotector;
serotonergic agonist
uh 301[no description available]medium30
fg 5893[no description available]medium10
s 14671[no description available]medium10
asenapine[no description available]medium105-chloro-2-methyl-2,3,3a,12b-tetrahydrodibenzo[2,3:6,7]oxepino[4,5-c]pyrrole
zalospirone[no description available]medium10
raclopride[no description available]medium20salicylamides
nafadotride[no description available]medium10aromatic ether;
naphthalenecarboxamide;
nitrile;
pyrrolidines;
tertiary amino compound		dopaminergic antagonist
clozapine[no description available]medium10benzodiazepine;
N-arylpiperazine;
N-methylpiperazine;
organochlorine compound		adrenergic antagonist;
dopaminergic antagonist;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
environmental contaminant;
GABA antagonist;
histamine antagonist;
muscarinic antagonist;
second generation antipsychotic;
serotonergic antagonist;
xenobiotic
olanzapine[no description available]medium10benzodiazepine;
N-arylpiperazine;
N-methylpiperazine		antiemetic;
dopaminergic antagonist;
histamine antagonist;
muscarinic antagonist;
second generation antipsychotic;
serotonergic antagonist;
serotonin uptake inhibitor
1,2-benzisothiazol-3(2h)-one, 2-(4-(4-(7-chloro-2,3-dihydro-1,4-benzodioxin-5-yl)-1-piperazinyl)butyl)-, 1,1-dioxide[no description available]medium40
vortioxetine[no description available]medium20aryl sulfide;
N-arylpiperazine		antidepressant;
anxiolytic drug;
serotonergic agonist;
serotonergic antagonist
piperidines[no description available]medium50
gr 113808[no description available]medium10indolyl carboxylate ester;
piperidines;
sulfonamide		serotonergic antagonist
rs 67333[no description available]medium10aromatic ketone
ly 341495[no description available]medium10
xanthenes[no description available]medium10xanthene
td-5108[no description available]medium10
paroxetine[no description available]medium10aromatic ether;
benzodioxoles;
organofluorine compound;
piperidines		antidepressant;
anxiolytic drug;
hepatotoxic agent;
P450 inhibitor;
serotonin uptake inhibitor
trichostatin a[no description available]medium10antibiotic antifungal agent;
hydroxamic acid;
trichostatin		bacterial metabolite;
EC 3.5.1.98 (histone deacetylase) inhibitor;
geroprotector
diazepam[no description available]medium1101,4-benzodiazepinone;
organochlorine compound		anticonvulsant;
anxiolytic drug;
environmental contaminant;
sedative;
xenobiotic
4-amino-1-(6-chloro-2-pyridyl)piperidine hydrochloride[no description available]medium10
pindolol[no description available]medium122indoles;
secondary amine		antiglaucoma drug;
antihypertensive agent;
beta-adrenergic antagonist;
serotonergic antagonist;
vasodilator agent
tetradecanoylphorbol acetate[no description available]medium10acetate ester;
diester;
phorbol ester;
tertiary alpha-hydroxy ketone;
tetradecanoate ester		antineoplastic agent;
apoptosis inducer;
carcinogenic agent;
mitogen;
plant metabolite;
protein kinase C agonist;
reactive oxygen species generator
thiazoles[no description available]medium401,3-thiazoles;
mancude organic heteromonocyclic parent;
monocyclic heteroarene
ritanserin[no description available]medium51organofluorine compound;
piperidines;
thiazolopyrimidine		antidepressant;
antipsychotic agent;
anxiolytic drug;
dopaminergic antagonist;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
serotonergic antagonist
fenclonine[no description available]medium20phenylalanine derivative
1-(3-chlorophenyl)piperazine[no description available]medium41monochlorobenzenes;
N-arylpiperazine		drug metabolite;
environmental contaminant;
serotonergic agonist;
xenobiotic
slv 313[no description available]medium10
gepirone[no description available]medium20N-arylpiperazine
alpha-aminopyridine[no description available]medium10
7-hydroxy-2-n,n-dipropylaminotetralin[no description available]medium10tetralins
dextroamphetamine[no description available]medium101-phenylpropan-2-amineadrenergic agent;
adrenergic uptake inhibitor;
dopamine uptake inhibitor;
dopaminergic agent;
neurotoxin;
sympathomimetic agent
cycloserine[no description available]medium104-amino-1,2-oxazolidin-3-one;
organonitrogen heterocyclic antibiotic;
organooxygen heterocyclic antibiotic;
zwitterion		antiinfective agent;
antimetabolite;
antitubercular agent;
metabolite;
NMDA receptor agonist
gr 127935[no description available]medium101,2,4-oxadiazole;
benzamides;
N-alkylpiperazine;
N-arylpiperazine
oxadiazoles[no description available]medium20
alpha-methyltryptophan, (l)-isomer[no description available]medium10
tryptophan[no description available]medium10erythrose 4-phosphate/phosphoenolpyruvate family amino acid;
L-alpha-amino acid zwitterion;
L-alpha-amino acid;
proteinogenic amino acid;
tryptophan zwitterion;
tryptophan		antidepressant;
Escherichia coli metabolite;
human metabolite;
micronutrient;
mouse metabolite;
nutraceutical;
plant metabolite;
Saccharomyces cerevisiae metabolite
omega-n-methylarginine[no description available]medium21amino acid zwitterion;
arginine derivative;
guanidines;
L-arginine derivative;
non-proteinogenic L-alpha-amino acid
arginine[no description available]medium21arginine;
glutamine family amino acid;
L-alpha-amino acid;
proteinogenic amino acid		biomarker;
Escherichia coli metabolite;
micronutrient;
mouse metabolite;
nutraceutical
corticosterone[no description available]medium14011beta-hydroxy steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(4) steroid;
C21-steroid;
glucocorticoid;
primary alpha-hydroxy ketone		human metabolite;
mouse metabolite
sulpiride[no description available]medium11benzamides;
N-alkylpyrrolidine;
sulfonamide		antidepressant;
antiemetic;
antipsychotic agent;
dopaminergic antagonist
urapidil[no description available]medium60piperazines
methoxamine[no description available]medium10amphetaminesalpha-adrenergic agonist;
antihypotensive agent
doxazosin[no description available]medium20aromatic amine;
benzodioxine;
monocarboxylic acid amide;
N-acylpiperazine;
N-arylpiperazine;
quinazolines		alpha-adrenergic antagonist;
antihyperplasia drug;
antihypertensive agent;
antineoplastic agent;
vasodilator agent
prazosin[no description available]medium40aromatic ether;
furans;
monocarboxylic acid amide;
piperazines;
quinazolines		alpha-adrenergic antagonist;
antihypertensive agent;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor
ketanserin[no description available]medium10aromatic ketone;
organofluorine compound;
piperidines;
quinazolines		alpha-adrenergic antagonist;
antihypertensive agent;
cardiovascular drug;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
serotonergic antagonist
phenylephrine[no description available]medium20phenols;
phenylethanolamines;
secondary amino compound		alpha-adrenergic agonist;
cardiotonic drug;
mydriatic agent;
nasal decongestant;
protective agent;
sympathomimetic agent;
vasoconstrictor agent
5-methylurapidil[no description available]medium60
n,n-dipropylcarboxamidotryptamine[no description available]medium10indolecarboxamide
tetrodotoxin[no description available]medium30azatetracycloalkane;
oxatetracycloalkane;
quinazoline alkaloid		animal metabolite;
bacterial metabolite;
marine metabolite;
neurotoxin;
voltage-gated sodium channel blocker
xylazine[no description available]medium101,3-thiazine;
methylbenzene;
secondary amino compound		alpha-adrenergic agonist;
analgesic;
emetic;
muscle relaxant;
sedative
propranolol[no description available]medium10naphthalenes;
propanolamine;
secondary amine		anti-arrhythmia drug;
antihypertensive agent;
anxiolytic drug;
beta-adrenergic antagonist;
environmental contaminant;
human blood serum metabolite;
vasodilator agent;
xenobiotic
chlordiazepoxide[no description available]medium50benzodiazepine
hydralazine[no description available]medium10azaarene;
hydrazines;
ortho-fused heteroarene;
phthalazines		antihypertensive agent;
vasodilator agent
way 100135[no description available]medium10piperazines
3-hydroxybenzylhydrazine[no description available]medium10phenols
hydrazine[no description available]medium10azane;
hydrazines		EC 4.3.1.10 (serine-sulfate ammonia-lyase) inhibitor
colforsin[no description available]medium10acetate ester;
cyclic ketone;
labdane diterpenoid;
organic heterotricyclic compound;
tertiary alpha-hydroxy ketone;
triol		adenylate cyclase agonist;
anti-HIV agent;
antihypertensive agent;
plant metabolite;
platelet aggregation inhibitor;
protein kinase A agonist
lysergic acid diethylamide[no description available]medium20ergoline alkaloid;
monocarboxylic acid amide;
organic heterotetracyclic compound		dopamine agonist;
hallucinogen;
serotonergic agonist
clonidine[no description available]medium80clonidine;
imidazoline
yohimbine[no description available]medium40methyl 17-hydroxy-20xi-yohimban-16-carboxylatealpha-adrenergic antagonist;
dopamine receptor D2 antagonist;
serotonergic antagonist
fentanyl[no description available]medium10anilide;
monocarboxylic acid amide;
piperidines		adjuvant;
anaesthesia adjuvant;
anaesthetic;
intravenous anaesthetic;
mu-opioid receptor agonist;
opioid analgesic
methysergide[no description available]medium11ergoline alkaloid
u 93385[no description available]medium10
fluvoxamine[no description available]medium50(trifluoromethyl)benzenes;
5-methoxyvalerophenone O-(2-aminoethyl)oxime		antidepressant;
anxiolytic drug;
serotonin uptake inhibitor
oxazepam[no description available]medium101,4-benzodiazepinone;
organochlorine compound		anxiolytic drug;
environmental contaminant;
xenobiotic
midazolam[no description available]medium10imidazobenzodiazepine;
monofluorobenzenes;
organochlorine compound		anticonvulsant;
antineoplastic agent;
anxiolytic drug;
apoptosis inducer;
central nervous system depressant;
GABAA receptor agonist;
general anaesthetic;
muscle relaxant;
sedative
neuropeptide y[no description available]medium10
pituitrin[no description available]medium10
potassium chloride[no description available]medium20inorganic chloride;
inorganic potassium salt;
potassium salt		fertilizer
alprazolam[no description available]medium10organochlorine compound;
triazolobenzodiazepine		anticonvulsant;
anxiolytic drug;
GABA agonist;
muscle relaxant;
sedative;
xenobiotic
quinpirole[no description available]medium10pyrazoloquinolinedopamine agonist
1-(3-trifluoromethylphenyl)piperazine[no description available]medium10(trifluoromethyl)benzenes;
N-arylpiperazine		environmental contaminant;
psychotropic drug;
serotonergic agonist;
xenobiotic
4-(benzodioxan-5-yl)-1-(indan-2-yl)piperazine[no description available]medium20
amitriptyline[no description available]medium10carbotricyclic compound;
tertiary amine		adrenergic uptake inhibitor;
antidepressant;
environmental contaminant;
tropomyosin-related kinase B receptor agonist;
xenobiotic
guanosine 5'-o-(3-thiotriphosphate)[no description available]medium10nucleoside triphosphate analogue
l 694247[no description available]medium10tryptamines
fg 7142[no description available]medium10beta-carbolines
beta-carboline-3-carboxylic acid methyl ester[no description available]medium10beta-carbolines
mianserin[no description available]medium10dibenzoazepineadrenergic uptake inhibitor;
alpha-adrenergic antagonist;
antidepressant;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
geroprotector;
H1-receptor antagonist;
histamine agonist;
sedative;
serotonergic antagonist
hydroxyindoleacetic acid[no description available]medium10indole-3-acetic acidsdrug metabolite;
human metabolite;
mouse metabolite
anpirtoline[no description available]medium10aryl sulfide
saxitoxin[no description available]medium10alkaloid;
carbamate ester;
guanidines;
ketone hydrate;
paralytic shellfish toxin;
pyrrolopurine		cyanotoxin;
marine metabolite;
neurotoxin;
sodium channel blocker;
toxin
snx 230[no description available]medium10
batrachotoxinin a 20-alpha-benzoate[no description available]medium10
citalopram[no description available]medium102-benzofurans;
cyclic ether;
nitrile;
organofluorine compound;
tertiary amino compound
bicuculline[no description available]medium10benzylisoquinoline alkaloid;
isoquinoline alkaloid;
isoquinolines		agrochemical;
central nervous system stimulant;
GABA-gated chloride channel antagonist;
GABAA receptor antagonist;
neurotoxin
cirazoline[no description available]medium10aromatic ether
brl 44408[no description available]medium10
binospirone mesylate[no description available]medium10
bmy 7378[no description available]medium10
desipramine[no description available]medium10dibenzoazepine;
secondary amino compound		adrenergic uptake inhibitor;
alpha-adrenergic antagonist;
antidepressant;
cholinergic antagonist;
drug allergen;
EC 3.1.4.12 (sphingomyelin phosphodiesterase) inhibitor;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
H1-receptor antagonist;
serotonin uptake inhibitor
alpha-methylserotonin[no description available]medium10tryptaminesserotonergic agonist
phentolamine[no description available]medium10imidazoles;
phenols;
substituted aniline;
tertiary amino compound		alpha-adrenergic antagonist;
vasodilator agent
sumatriptan[no description available]medium10sulfonamide;
tryptamines		serotonergic agonist;
vasoconstrictor agent
glutamic acid[no description available]medium10glutamic acid;
glutamine family amino acid;
L-alpha-amino acid;
proteinogenic amino acid		Escherichia coli metabolite;
ferroptosis inducer;
micronutrient;
mouse metabolite;
neurotransmitter;
nutraceutical
pentobarbital[no description available]medium20barbituratesGABAA receptor agonist
morphine[no description available]medium20morphinane alkaloid;
organic heteropentacyclic compound;
tertiary amino compound		anaesthetic;
drug allergen;
environmental contaminant;
geroprotector;
mu-opioid receptor agonist;
opioid analgesic;
plant metabolite;
vasodilator agent;
xenobiotic
reserpine[no description available]medium10alkaloid ester;
methyl ester;
yohimban alkaloid		adrenergic uptake inhibitor;
antihypertensive agent;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
environmental contaminant;
first generation antipsychotic;
plant metabolite;
xenobiotic
dihydroxyphenylalanine[no description available]medium20hydroxyphenylalanine;
non-proteinogenic alpha-amino acid;
tyrosine derivative		human metabolite
5-hydroxytryptophan[no description available]medium20hydroxytryptophanhuman metabolite;
neurotransmitter
atropine[no description available]medium10
ondansetron[no description available]medium10carbazoles
methylatropine[no description available]medium10
cyanopindolol[no description available]medium10indoles
enflurane[no description available]medium10ether;
organochlorine compound;
organofluorine compound		anaesthetic
guanfacine[no description available]medium10acetamides
moxonidine[no description available]medium10organohalogen compound;
pyrimidines
ConditionIndicatedRelationship StrengthStudiesTrials
Aggression0low20
Aging0low10
Air Sickness0low10
Airsickness0low10
Alcohol Abuse0medium11
Alcohol Addiction0medium11
Alcohol Dependence0medium11
Alcohol Use Disorder0medium11
Alcoholic Intoxication, Chronic0medium11
Alcoholism0medium11
Anesthesia0low60
Anochlesia0low40
Anxiety0low70
Anxiety Disorders0low10
Anxiety Neuroses0low10
Anxiety States, Neurotic0low10
As If Personality0low20
Avoidant Personality Disorder0low20
Blood Pressure, High0low60
Body Weight0low10
Borderline Personality Disorder0low10
Car Sickness0low10
Carsickness0low10
Catalepsy0low40
Cerea Flexibilitas0low40
Decerebrate Posturing0low20
Decerebrate State0low20
Decorticate Rigidity0low20
Decorticate State0low20
Deficiency, Riboflavin0low10
Depression0low20
Depression, Endogenous0medium83
Depression, Involutional0medium31
Depression, Neurotic0medium83
Depression, Unipolar0medium83
Depressive Disorder0medium83
Depressive Disorder, Major0medium31
Depressive Syndrome0medium83
Disease Models, Animal0low100
Disorder, Borderline Personality0low10
Electrolytes0low20
Emesis0low10
Ethanol Abuse0medium11
Fever0low70
Flexibility, Waxy0low40
Hyperglycemia0low10
Hyperglycemia, Postprandial0low10
Hypertension0low60
Hypertension, Renal0low20
Hypothermia0low40
Hypothermia, Accidental0low40
Impulse-Ridden Personality0low20
Inadequate Personality0low20
Intraocular Pressure0low10
Major Depressive Disorder0medium31
Melancholia0medium83
Melancholia, Involutional0medium31
Motion Sickness0low10
Muscle Contraction0low10
Muscle Relaxation0low10
Narcissistic Personality Disorder0low20
Neuroses, Anxiety0low10
Neurosis, Depressive0medium83
Panic Attacks0medium11
Panic Disorder0medium11
Paraphrenia, Involutional0medium31
Personality Disorder, Borderline0low10
Personality Disorders0low20
Postprandial Hyperglycemia0low10
Psychosis, Involutional0medium31
Pyrexia0low70
Riboflavin Deficiency0low10
Rigidity, Decerebrate0low20
Rigidity, Decorticate0low20
Sea Sickness0low10
Seasickness0low10
Sensitivity and Specificity0low10
Tachyarrhythmia0low10
Tachycardia0low10
Unipolar Depression0medium83
Vomiting0low10

Research Highlights

Safety/Toxicity (1)

ArticleYear
Cardiovascular and side effects of flesinoxan in conscious hypertensive dogs. Modulation by prazosin.
European journal of pharmacology, Sep-04, Volume: 202, Issue: 1		1991
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Long-term Use (5)

ArticleYear
Flesinoxan challenge suggests that chronic treatment with paroxetine in rats does not desensitize receptors controlling 5-HT synthesis.
Neurochemistry international, Volume: 53, Issue: 6-8		2008
Rapid desensitization of somatodendritic 5-HT1A receptors by chronic administration of the high-efficacy 5-HT1A agonist, F13714: a microdialysis study in the rat.
British journal of pharmacology, Volume: 149, Issue: 2		2006
SLV313 (1-(2,3-dihydro-benzo[1,4]dioxin-5-yl)-4- [5-(4-fluoro-phenyl)-pyridin-3-ylmethyl]-piperazine monohydrochloride): a novel dopamine D2 receptor antagonist and 5-HT1A receptor agonist potential antipsychotic drug.
Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology, Volume: 32, Issue: 1		2007
Effect of chronic administration of flesinoxan and fluvoxamine on freezing behavior induced by conditioned fear.
European journal of pharmacology, Aug-03, Volume: 425, Issue: 1		2001
The effects of the 5-HT1A agonist flesinoxan, in three paradigms for assessing antidepressant potential in the rat.
European neuropsychopharmacology : the journal of the European College of Neuropsychopharmacology, Volume: 7, Issue: 2		1997
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Pharmacokinetics (2)

ArticleYear
Allometric scaling of pharmacodynamic responses: application to 5-Ht1A receptor mediated responses from rat to man.
Pharmaceutical research, Volume: 24, Issue: 11		2007
Pharmacokinetic-pharmacodynamic modelling of the hypothermic and corticosterone effects of the 5-HT1A receptor agonist flesinoxan.
European journal of pharmacology, Jun-07, Volume: 445, Issue: 1-2		2002
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Dosage (10)

ArticleYear
The rapid recovery of 5-HT cell firing induced by the antidepressant vortioxetine involves 5-HT(3) receptor antagonism.
The international journal of neuropsychopharmacology, Volume: 16, Issue: 5		2013
Effects of repeated testing in two inbred strains on flesinoxan dose-response curves in three mouse models for anxiety.
European journal of pharmacology, Jun-21, Volume: 494, Issue: 1		2004
Corticosterone responses in 5-HT1B receptor knockout mice to stress or 5-HT1A receptor activation are normal.
Psychopharmacology, Volume: 153, Issue: 4		2001
Effect of sustained administration of the 5-HT1A receptor agonist flesinoxan on rat 5-HT neurotransmission.
European neuropsychopharmacology : the journal of the European College of Neuropsychopharmacology, Volume: 9, Issue: 5		1999
Effects of 5-HT1A receptor ligands in a modified Geller-Seifter conflict model in the rat.
European journal of pharmacology, May-01, Volume: 325, Issue: 2-3		1997
Effects of the 5-HT1A receptor agonist flesinoxan in panic disorder.
Psychopharmacology, Volume: 127, Issue: 2		1996
Rapid and long duration tolerance to the vagal bradycardic effects of 5-HT1A receptor agonists.
Behavioural brain research, Volume: 73, Issue: 1-2		1996
Flesinoxan dose-dependently reduces extracellular 5-hydroxytryptamine (5-HT) in rat median raphe and dorsal hippocampus through activation of 5-HT1A receptors.
Journal of neurochemistry, Volume: 66, Issue: 6		1996
Evidence that different regional sympathetic outflows vary in their sensitivity to the sympathoinhibitory actions of putative 5-HT1A and alpha 2-adrenoceptor agonists in anaesthetized cats.
British journal of pharmacology, Volume: 98, Issue: 4		1989
8-OH-DPAT, flesinoxan and guanfacine: systemic and regional haemodynamic effects of centrally acting antihypertensive agents in anaesthetized rabbits.
British journal of pharmacology, Volume: 96, Issue: 4		1989
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]