Compounds > eltoprazine
Page last updated: 2024-11-06

eltoprazine

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

Eltoprazine is a potent and selective 5-HT1A receptor agonist that has been investigated for its potential therapeutic effects in a variety of neurological and psychiatric disorders. It is a synthetic compound that was developed in the 1980s. Eltoprazine's effects on the central nervous system include anxiolytic, antidepressant, and antipsychotic activity. It is studied for its potential to treat conditions such as anxiety, depression, and schizophrenia. Eltoprazine's selective affinity for the 5-HT1A receptor is believed to contribute to its therapeutic properties. Research suggests that it may modulate serotonin neurotransmission in the brain, leading to its observed effects. However, despite promising preclinical studies, eltoprazine has not been approved for clinical use, and its potential for treating psychiatric disorders remains under investigation.'

eltoprazine: RN given refers to parent cpd; suppresses hyperpolarizing responses to serotonin in rat hippocampus [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID65853
CHEMBL ID282614
SCHEMBL ID177715
MeSH IDM0176039

Synonyms (51)

Synonym
bdbm50035057
1-(2,3-dihydro-benzo[1,4]dioxin-5-yl)-piperazine
(eltoprazine)1-(2,3-dihydro-benzo[1,4]dioxin-5-yl)-piperazine
PDSP2_000559
NCGC00159533-01
eltoprazine
1-(2,3-dihydro-1,4-benzodioxin-5-yl)piperazine
eltoprazina [spanish]
1-(1,4-benzodioxan-5-yl)piperazine
eltoprazinum [latin]
eltoprazine [inn]
PDSP1_000561
CHEMBL282614 ,
L000982
FT-0667839
98206-09-8
98224-03-4
510m006ko6 ,
eltoprazinum
unii-510m006ko6
eltoprazina
1-(2,3-dihydrobenzo[b][1,4]dioxin-5-yl)piperazine
AKOS016007669
AM1234
piperazine, 1-(2,3-dihydro-1,4-benzodioxin-5-yl)-
CS-3216
HY-16687
1-(2,3-dihydrobenzo[1,4]dioxin-5-yl)-piperazine
4-(2,3-dihydrobenzo[1,4]dioxin-5-yl)piperazine
1-(2,3-dihydrobenzo[1,4]dioxin-5-yl)piperazine
4-(2,3-dihydro-benzo[1,4]dioxin-5-yl)-piperazine
(2,3-dihydro[1,4]benzodioxin-5-yl)piperazine
4-(2,3-dihydrobenzo[1,4]dioxin-5-yl)-piperazine
1-(1,4-benzodioxan-5-yl)-piperazine
1-(1,4-benzodioxan-5-yl)piperazin
n-(benzodioxan-5-yl)piperazine
SCHEMBL177715
eltoprazine [mi]
eltoprazine [mart.]
DTXSID5048425
mfcd00868056
DB12883
BCP19313
Q5367896
Z2044804716
BRD-K86171477-003-01-9
SB16767
H11026
1-(2,3-dihydrobenzo[b][1,4]dioxin-5-yl)piperazine hydrochloride hydrochloride
A902315
EN300-1839382

Research Excerpts

Effects

Eltoprazine has a weak antagonistic action (IC50 = 7 microM) on the 5-HT1C receptor as revealed by inhibition of the5-HT-induced accumulation of inositol phosphates in the choroid plexus of the pig.

ExcerptReferenceRelevance
"Eltoprazine has a weak antagonistic action (IC50 = 7 microM) on the 5-HT1C receptor as revealed by inhibition of the 5-HT-induced accumulation of inositol phosphates in the choroid plexus of the pig."( Neurochemical profile of eltoprazine.
Schipper, J; Sijbesma, H; Tulp, MT, 1990)		1.3
"Eltoprazine has potential clinical application for dyskinesia."( Eltoprazine modulated gamma oscillations on ameliorating L-dopa-induced dyskinesia in rats.
Bi, Y; Deng, Y; Guan, J; Wang, P; Wang, Z; Yang, H; Yu, J; Zhang, W, 2023)		3.07
"Eltoprazine has a weak antagonistic action (IC50 = 7 microM) on the 5-HT1C receptor as revealed by inhibition of the 5-HT-induced accumulation of inositol phosphates in the choroid plexus of the pig."( Neurochemical profile of eltoprazine.
Schipper, J; Sijbesma, H; Tulp, MT, 1990)		1.3

Treatment

ExcerptReferenceRelevance
"Treatment with eltoprazine (DU 28853) increased the number of entries by male mice into compartments containing the odors of male and female conspecifics. "( Effects of eltoprazine hydrochloride on reactivity to conspecific or novel odors and activity.
Kemble, ED; Ostrem, JL; Rawleigh, JM, 1992)		1.03

Pharmacokinetics

ExcerptReferenceRelevance
" The mean elimination half-life of eltoprazine in plasma was about 8 hours."( Pharmacokinetics of eltoprazine in healthy subjects.
Mathlener, IS; Raghoebar, M; van Harten, J, 1990)		0.88
" Values of tmax varied from 1 to 4 h after oral administration."( Pharmacokinetics of eltoprazine in healthy male subjects after single dose oral and intravenous administration.
Cournot, A; Mak, M; Pistorius, MC; Raghoebar, M; Roseboom, H; Van Harten, J, 1990)		0.6

Bioavailability

ExcerptReferenceRelevance
" Absolute bioavailability was 67% +/- 20%."( Pharmacokinetics of eltoprazine in the dog.
Lammers, R; van Harten, J, 1990)		0.6
" It was shown that the absorption of eltoprazine from the gastro-intestinal tract was complete, and that absolute bioavailability was 100%."( Pharmacokinetics of eltoprazine in healthy subjects.
Mathlener, IS; Raghoebar, M; van Harten, J, 1990)		0.88
" Absolute oral bioavailability was 110 +/- 32%."( Pharmacokinetics of eltoprazine in healthy male subjects after single dose oral and intravenous administration.
Cournot, A; Mak, M; Pistorius, MC; Raghoebar, M; Roseboom, H; Van Harten, J, 1990)		0.6

Dosage Studied

The pharmacokinetics of eltoprazine in healthy male subjects was investigated after intravenous and oral dosing. Dose-response curves for 5HT were shifted to the right in the presence of el toprazine.

ExcerptRelevanceReference
"To compare the metabolism of eltoprazine of dog, rat and rabbit with that in man, urine samples were collected after dosing with 14C-eltoprazine."( The metabolite patterns of eltoprazine in man, dog, rat and rabbit.
de Greef, L; Klerks, F; Koster, HJ; Raghoebar, M, 1990)		0.87
"The pharmacokinetics of eltoprazine in healthy male subjects was investigated after intravenous and oral dosing in one study, and after oral dosing of 14C-eltoprazine in a second study."( Pharmacokinetics of eltoprazine in healthy subjects.
Mathlener, IS; Raghoebar, M; van Harten, J, 1990)		0.91
" Dose-response curves for 5HT were shifted to the right in the presence of eltoprazine, while the maximal response was diminished."( Eltoprazine suppresses hyperpolarizing responses to serotonin in rat hippocampus.
Joëls, M; Pennartz, CM; Schipper, J; Sijbesma, H, 1990)		1.95
" They did not induce these responses alone, and in their presence, dose-response curves for 8-OH-DPAT were shifted in parallel to the right without loss of maximal effect."( Novel benzodioxopiperazines acting as antagonists at postsynaptic 5-HT1A receptors and as agonists at 5-HT1A autoreceptors: a comparative pharmacological characterization with proposed 5-HT1A antagonists.
Audinot, V; Bervoets, K; Brocco, M; Canton, H; Gobert, A; Lejeune, F; Mennini, T; Millan, MJ; Rivet, JM; Widdowson, P, 1994)		0.29
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (4)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)Ki0.02460.00010.739610.0000AID4411; AID4416
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)Ki0.05370.00031.29679.2440AID4718
D(2) dopamine receptorRattus norvegicus (Norway rat)Ki1.10000.00000.437510.0000AID65108
[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)
Beta-1 adrenergic receptorHomo sapiens (human)Kd15.92440.00010.803910.0000AID731818
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (14)

Processvia Protein(s)Taxonomy
positive regulation of heart rate by epinephrine-norepinephrineBeta-1 adrenergic receptorHomo sapiens (human)
positive regulation of the force of heart contraction by epinephrine-norepinephrineBeta-1 adrenergic receptorHomo sapiens (human)
diet induced thermogenesisBeta-1 adrenergic receptorHomo sapiens (human)
response to coldBeta-1 adrenergic receptorHomo sapiens (human)
heat generationBeta-1 adrenergic receptorHomo sapiens (human)
negative regulation of multicellular organism growthBeta-1 adrenergic receptorHomo sapiens (human)
fear responseBeta-1 adrenergic receptorHomo sapiens (human)
regulation of circadian sleep/wake cycle, sleepBeta-1 adrenergic receptorHomo sapiens (human)
brown fat cell differentiationBeta-1 adrenergic receptorHomo sapiens (human)
regulation of postsynaptic membrane potentialBeta-1 adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayBeta-1 adrenergic receptorHomo sapiens (human)
positive regulation of cold-induced thermogenesisBeta-1 adrenergic receptorHomo sapiens (human)
norepinephrine-epinephrine-mediated vasodilation involved in regulation of systemic arterial blood pressureBeta-1 adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeBeta-1 adrenergic receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (7)

Processvia Protein(s)Taxonomy
beta-adrenergic receptor activityBeta-1 adrenergic receptorHomo sapiens (human)
beta1-adrenergic receptor activityBeta-1 adrenergic receptorHomo sapiens (human)
protein bindingBeta-1 adrenergic receptorHomo sapiens (human)
PDZ domain bindingBeta-1 adrenergic receptorHomo sapiens (human)
alpha-2A adrenergic receptor bindingBeta-1 adrenergic receptorHomo sapiens (human)
protein heterodimerization activityBeta-1 adrenergic receptorHomo sapiens (human)
G protein-coupled neurotransmitter receptor activity involved in regulation of postsynaptic membrane potentialBeta-1 adrenergic receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (4)

Processvia Protein(s)Taxonomy
early endosomeBeta-1 adrenergic receptorHomo sapiens (human)
plasma membraneBeta-1 adrenergic receptorHomo sapiens (human)
Schaffer collateral - CA1 synapseBeta-1 adrenergic receptorHomo sapiens (human)
neuronal dense core vesicleBeta-1 adrenergic receptorHomo sapiens (human)
plasma membraneBeta-1 adrenergic receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (30)

Assay IDTitleYearJournalArticle
AID177450Compound was evaluated for the inhibition of quipazine-induced head twitches after 2 hr (administered subcutaneously); not tested1992Journal of medicinal chemistry, Dec-25, Volume: 35, Issue:26
Selective, centrally acting serotonin 5-HT2 antagonists. 1. 2- and 6-substituted 1-phenyl-3-(4-piperidinyl)-1H-indoles.
AID184856Minimum effective antagonist dose administered subcutaneously1995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
Characterization of potent and selective antagonists at postsynaptic 5-HT1A receptors in a series of N4-substituted arylpiperazines.
AID731818Binding affinity to His-tagged human beta1 adrenergic receptor expressed in HEK293 cell membranes by surface plasmon resonance analysis2013Journal of medicinal chemistry, May-09, Volume: 56, Issue:9
Biophysical fragment screening of the β1-adrenergic receptor: identification of high affinity arylpiperazine leads using structure-based drug design.
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.
AID182620Compound after subcutaneous administration was evaluated for antagonist activity against hypothermia induced by 8-hydroxy -DPAT in rat1995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
Characterization of potent and selective antagonists at postsynaptic 5-HT1A receptors in a series of N4-substituted arylpiperazines.
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.
AID127685Compound was evaluated for the inhibition of isolation-induced aggression at a threshold of, 90 seconds; 3.5-18.41992Journal of medicinal chemistry, Dec-25, Volume: 35, Issue:26
Selective, centrally acting serotonin 5-HT2 antagonists. 1. 2- and 6-substituted 1-phenyl-3-(4-piperidinyl)-1H-indoles.
AID177605Compound was evaluated for the inhibition of quipazine-induced head twitches after 24 hr (administered perorally); not tested1992Journal of medicinal chemistry, Dec-25, Volume: 35, Issue:26
Selective, centrally acting serotonin 5-HT2 antagonists. 1. 2- and 6-substituted 1-phenyl-3-(4-piperidinyl)-1H-indoles.
AID230050Ratio of MED (agonist) to that of MED (antagonist) values.1995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
Characterization of potent and selective antagonists at postsynaptic 5-HT1A receptors in a series of N4-substituted arylpiperazines.
AID17869Local inhibition constant was determined1993Journal of medicinal chemistry, Sep-17, Volume: 36, Issue:19
Structure-affinity relationship studies on 5-HT1A receptor ligands. 1. Heterobicyclic phenylpiperazines with N4-alkyl substituents.
AID185743Maximum antagonist effect (% effect) expressed relative to 8-hydroxy-DPAT (100%)1995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
Characterization of potent and selective antagonists at postsynaptic 5-HT1A receptors in a series of N4-substituted arylpiperazines.
AID4718Binding affinity at 5-hydroxytryptamine 1B receptor1995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
Characterization of potent and selective antagonists at postsynaptic 5-HT1A receptors in a series of N4-substituted arylpiperazines.
AID25073Ionization at 20 degree C1993Journal of medicinal chemistry, Sep-17, Volume: 36, Issue:19
Structure-affinity relationship studies on 5-HT1A receptor ligands. 1. Heterobicyclic phenylpiperazines with N4-alkyl substituents.
AID127679Compound was evaluated for the inhibition of isolation-induced aggression at a threshold of 180 seconds; 2.3-12.41992Journal of medicinal chemistry, Dec-25, Volume: 35, Issue:26
Selective, centrally acting serotonin 5-HT2 antagonists. 1. 2- and 6-substituted 1-phenyl-3-(4-piperidinyl)-1H-indoles.
AID330660Effect on life span of Caenorhabditis elegans at 100 uM2007Nature, Nov-22, Volume: 450, Issue:7169
An antidepressant that extends lifespan in adult Caenorhabditis elegans.
AID25074Ionization at 25 degree C1993Journal of medicinal chemistry, Sep-17, Volume: 36, Issue:19
Structure-affinity relationship studies on 5-HT1A receptor ligands. 1. Heterobicyclic phenylpiperazines with N4-alkyl substituents.
AID185742Maximum agonist effect (% effect) expressed relative to 8-hydroxy-DPAT (100%)1995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
Characterization of potent and selective antagonists at postsynaptic 5-HT1A receptors in a series of N4-substituted arylpiperazines.
AID25076Ionization at 37 degree C1993Journal of medicinal chemistry, Sep-17, Volume: 36, Issue:19
Structure-affinity relationship studies on 5-HT1A receptor ligands. 1. Heterobicyclic phenylpiperazines with N4-alkyl substituents.
AID184855Minimum effective agonist dose administered subcutaneously1995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
Characterization of potent and selective antagonists at postsynaptic 5-HT1A receptors in a series of N4-substituted arylpiperazines.
AID4416Binding affinity at 5-hydroxytryptamine 1A receptor1995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
Characterization of potent and selective antagonists at postsynaptic 5-HT1A receptors in a series of N4-substituted arylpiperazines.
AID177435Compound was evaluated for the inhibition of pergolide-induced reactions after 2 hr (administered subcutaneously); not tested1992Journal of medicinal chemistry, Dec-25, Volume: 35, Issue:26
Selective, centrally acting serotonin 5-HT2 antagonists. 1. 2- and 6-substituted 1-phenyl-3-(4-piperidinyl)-1H-indoles.
AID25077Ionization at 45 degree C1993Journal of medicinal chemistry, Sep-17, Volume: 36, Issue:19
Structure-affinity relationship studies on 5-HT1A receptor ligands. 1. Heterobicyclic phenylpiperazines with N4-alkyl substituents.
AID4411Binding affinity of a compound to rat brain 5-hydroxytryptamine 1A (serotonin) receptor assayed by radiolabeled [3H]-8-OH-DPAT ligand displacement1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
Binding of arylpiperazines, (aryloxy)propanolamines, and tetrahydropyridylindoles to the 5-HT1A receptor: contribution of the molecular lipophilicity potential to three-dimensional quantitative structure-affinity relationship models.
AID4091Displacement of [3H]2-(di-N-propylamino)-8-hydroxytetralin from central 5-hydroxytryptamine 1A receptor recognition sites in rat frontal cortex homogenates.1995Journal of medicinal chemistry, May-26, Volume: 38, Issue:11
N4-unsubstituted N1-arylpiperazines as high-affinity 5-HT1A receptor ligands.
AID25075Ionization at 30 degree C1993Journal of medicinal chemistry, Sep-17, Volume: 36, Issue:19
Structure-affinity relationship studies on 5-HT1A receptor ligands. 1. Heterobicyclic phenylpiperazines with N4-alkyl substituents.
AID330659Effect on life span of Caenorhabditis elegans at 50 uM2007Nature, Nov-22, Volume: 450, Issue:7169
An antidepressant that extends lifespan in adult Caenorhabditis elegans.
AID4092Displacement of radioligand [3H]2-(di-N-propylamino)-8-hydroxytetralin from 5-hydroxytryptamine 1A receptor in rat frontal cortex homogenate1993Journal of medicinal chemistry, Sep-17, Volume: 36, Issue:19
Structure-affinity relationship studies on 5-HT1A receptor ligands. 1. Heterobicyclic phenylpiperazines with N4-alkyl substituents.
AID177617Compound was evaluated for the inhibition of quipazine-induced head twitches after 24 h (administered subcutaneously); not tested1992Journal of medicinal chemistry, Dec-25, Volume: 35, Issue:26
Selective, centrally acting serotonin 5-HT2 antagonists. 1. 2- and 6-substituted 1-phenyl-3-(4-piperidinyl)-1H-indoles.
AID4344Binding affinity to displace [3H]2-(di-N-propylamino)-8-hydroxy-tetralin from 5-hydroxytryptamine 1A (5-HT1A) receptor in rat frontal cortex homogenates1994Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17
Structure-affinity relationship studies on 5-HT1A receptor ligands. 2. Heterobicyclic phenylpiperazines with N4-aralkyl substituents.
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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (69)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's51 (73.91)18.2507
2000's2 (2.90)29.6817
2010's14 (20.29)24.3611
2020's2 (2.90)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 30.17

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 moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index30.17 (24.57)
Research Supply Index4.34 (2.92)
Research Growth Index5.39 (4.65)
Search Engine Demand Index35.06 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (30.17)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials7 (10.14%)5.53%
Reviews4 (5.80%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other58 (84.06%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (2)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Randomized, Double-blind, Parallel Trial Comparing the Effects of Eltoprazine (Adjunct to Anti-psychotics) With Placebo in Adults With Schizophrenia, in Improving One or More Dimensions of Cognitive Impairment Associated With Schizophrenia [NCT01266174]Phase 231 participants (Actual)Interventional2011-08-31Completed
Phase 2, Multicenter, Randomized, Double-blind, Placebo-controlled, 4-way Crossover, Dose-finding Study, of Eltoprazine Safety, Tolerability and Efficacy in the Treatment of Levodopa-induced Dyskinesia in Patients With Parkinson's Disease [NCT02439125]Phase 260 participants (Anticipated)Interventional2015-05-31Active, not recruiting
[information is prepared from clinicaltrials.gov, extracted Sep-2024]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
gamma-aminobutyric acid
gamma-Aminobutyric Acid: The most common inhibitory neurotransmitter in the central nervous system.. gamma-aminobutyric acid : A gamma-amino acid that is butanoic acid with the amino substituent located at C-4.		2.1110amino acid zwitterion;
gamma-amino acid;
monocarboxylic acid		human metabolite;
neurotransmitter;
Saccharomyces cerevisiae metabolite;
signalling molecule
tryptamine
[no description available]		1.9910aminoalkylindole;
aralkylamino compound;
indole alkaloid;
tryptamines		human metabolite;
mouse metabolite;
plant metabolite
7-hydroxy-2-n,n-dipropylaminotetralin
7-hydroxy-2-N,N-dipropylaminotetralin: RN given refers to cpd without isomeric designation		2.0310tetralins
8-hydroxy-2-(di-n-propylamino)tetralin
8-Hydroxy-2-(di-n-propylamino)tetralin: A serotonin 1A-receptor agonist that is used experimentally to test the effects of serotonin.. 8-OH-DPAT : A tetralin substituted at positions 1 and 7 by hydroxy and dipropylamino groups respectively		9.06150phenols;
tertiary amino compound;
tetralins		serotonergic antagonist
4-iodo-2,5-dimethoxyphenylisopropylamine
4-iodo-2,5-dimethoxyphenylisopropylamine: RN given refers to unlabeled parent cpd without isomeric designation; a serotonin agonist. 2-(4-iodo-2,5-dimethoxyphenyl)-1-methylethylamine : An organoiodine compound that is amphetamine bearing two methoxy substituents at positions 2 and 5 as well as an iodo substituent at position 4.		1.9710amphetamines;
dimethoxybenzene;
organoiodine compound
1-(1-naphthyl)piperazine
1-(1-naphthyl)piperazine: serotonin agonist; structure given in first source		2.3920N-arylpiperazine
1-(2-methoxyphenyl)piperazine
1-(2-methoxyphenyl)piperazine: RN given refers to parent cpd		2.940piperazines
1-(3-chlorophenyl)piperazine
1-(3-chlorophenyl)piperazine: supposed metabolite of TRAZODONE; RN given refers to parent cpd; structure. 1-(3-chlorophenyl)piperazine : A N-arylpiperazine that is piperazine carrying a 3-chlorophenyl substituent at position 1. It is a metabolite of the antidepressant drug trazodone.		2.9140monochlorobenzenes;
N-arylpiperazine		drug metabolite;
environmental contaminant;
serotonergic agonist;
xenobiotic
2-methyl-5-ht
2-methyl-5-HT: M-receptor agonist		1.9910tryptaminesserotonergic agonist
5-carboxamidotryptamine
5-carboxamidotryptamine: agonist of 5-HT receptor; structure given in first source		1.9910tryptamines
methylbufotenin
5-methoxy-N,N-dimethyltryptamine : A tryptamine alkaloid that is N,N-dimethyltryptamine substituted by a methoxy group at position 5.		1.9910aromatic ether;
tertiary amino compound;
tryptamine alkaloid		hallucinogen;
plant metabolite
5-methoxytryptamine
5-Methoxytryptamine: Serotonin derivative proposed as potentiator for hypnotics and sedatives.. 5-methoxytryptamine : A member of the class of tryptamines that is the methyl ether derivative of serotonin.		1.9910aromatic ether;
primary amino compound;
tryptamines		5-hydroxytryptamine 2A receptor agonist;
5-hydroxytryptamine 2B receptor agonist;
5-hydroxytryptamine 2C receptor agonist;
antioxidant;
cardioprotective agent;
human metabolite;
mouse metabolite;
neuroprotective agent;
radiation protective agent;
serotonergic agonist
acebutolol
Acebutolol: A cardioselective beta-1 adrenergic antagonist with little effect on the bronchial receptors. The drug has stabilizing and quinidine-like effects on cardiac rhythm, as well as weak inherent sympathomimetic action.. acebutolol : An ether that is the 2-acetyl-4-(butanoylamino)phenyl ether of the primary hydroxy group of 3-(propan-2-ylamino)propane-1,2-diol.		1.9910aromatic amide;
ethanolamines;
ether;
monocarboxylic acid amide;
propanolamine;
secondary amino compound		anti-arrhythmia drug;
antihypertensive agent;
beta-adrenergic antagonist;
sympathomimetic agent
alpha-methylserotonin
alpha-methylserotonin: potent agonist at M & D receptors of serotonin; RN given refers to parent cpd		1.9910tryptaminesserotonergic agonist
alprenolol
Alprenolol: One of the ADRENERGIC BETA-ANTAGONISTS used as an antihypertensive, anti-anginal, and anti-arrhythmic agent.. alprenolol : A secondary alcohol that is propan-2-ol substituted by a 2-allylphenoxy group at position 1 and an isopropylamino group at position 3. It is a beta-adrenergic antagonist used as a antihypertensive, anti-arrhythmia and a sympatholytic agent.		1.9910secondary alcohol;
secondary amino compound		anti-arrhythmia drug;
antihypertensive agent;
beta-adrenergic antagonist;
sympatholytic agent
amantadine
amant: an antiviral compound consisting of an adamantane derivative chemically linked to a water-solube polyanioic matrix; structure in first source		2.0810adamantanes;
primary aliphatic amine		analgesic;
antiparkinson drug;
antiviral drug;
dopaminergic agent;
NMDA receptor antagonist;
non-narcotic analgesic
atenolol
Atenolol: A cardioselective beta-1 adrenergic blocker possessing properties and potency similar to PROPRANOLOL, but without a negative inotropic effect.. atenolol : An ethanolamine compound having a (4-carbamoylmethylphenoxy)methyl group at the 1-position and an N-isopropyl substituent.		1.9910ethanolamines;
monocarboxylic acid amide;
propanolamine		anti-arrhythmia drug;
antihypertensive agent;
beta-adrenergic antagonist;
environmental contaminant;
sympatholytic agent;
xenobiotic
bmy 7378
[no description available]		2.3920piperazines
buspirone
Buspirone: An anxiolytic agent and serotonin receptor agonist belonging to the azaspirodecanedione class of compounds. Its structure is unrelated to those of the BENZODIAZAPINES, but it has an efficacy comparable to DIAZEPAM.. buspirone : An azaspiro compound that is 8-azaspiro[4.5]decane-7,9-dione substituted at the nitrogen atom by a 4-(piperazin-1-yl)butyl group which in turn is substituted by a pyrimidin-2-yl group at the N(4) position.		7.940azaspiro compound;
N-alkylpiperazine;
N-arylpiperazine;
organic heteropolycyclic compound;
piperidones;
pyrimidines		anxiolytic drug;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
sedative;
serotonergic agonist
carvedilol
[no description available]		1.9910carbazoles;
secondary alcohol;
secondary amino compound		alpha-adrenergic antagonist;
antihypertensive agent;
beta-adrenergic antagonist;
cardiovascular drug;
vasodilator agent
celiprolol
Celiprolol: A cardioselective beta-1 adrenergic antagonist that has intrinsic sympathomimetic activity. It is used in the management of ANGINA PECTORIS and HYPERTENSION.		1.9910aromatic ketone
cgp 20712a
[no description available]		1.9910imidazoles
cgs 12066
4-(4-methylpiperazin-1-yl)-7-(trifluoromethyl)pyrrolo[1,2-a]quinoxaline : A pyrroloquinoxaline that is pyrrolo[1,2-a]quinoxaline bearing additional 4-methylpiperazin-1-yl and trifluoromethyl substituents at positions 4 and 7 respectively. A 5-hydroxytryptamine receptor 1B (5-HT1B) full agonist, 10-fold selective over 5-HT1A and 1000-fold selective over 5-HT2C receptors. Centrally active following systemic administration.		1.9910N-arylpiperazine;
organofluorine compound;
pyrroloquinoxaline		serotonergic agonist
citalopram
Citalopram: A furancarbonitrile that is one of the serotonin uptake inhibitors used as an antidepressant. The drug is also effective in reducing ethanol uptake in alcoholics and is used in depressed patients who also suffer from TARDIVE DYSKINESIA in preference to tricyclic antidepressants, which aggravate dyskinesia.. citalopram : A racemate comprising equimolar amounts of (R)-citalopram and its enantiomer, escitalopram. It is used as an antidepressant, although only escitalopram is active.. 1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-2-benzofuran-5-carbonitrile : A nitrile that is 1,3-dihydro-2-benzofuran-5-carbonitrile in which one of the hydrogens at position 1 is replaced by a p-fluorophenyl group, while the other is replaced by a 3-(dimethylamino)propyl group.		1.99102-benzofurans;
cyclic ether;
nitrile;
organofluorine compound;
tertiary amino compound
cyproheptadine
Cyproheptadine: A serotonin antagonist and a histamine H1 blocker used as antipruritic, appetite stimulant, antiallergic, and for the post-gastrectomy dumping syndrome, etc.. cyproheptadine : The product resulting from the formal oxidative coupling of position 5 of 5H-dibenzo[a,d]cycloheptene with position 4 of 1-methylpiperidine resulting in the formation of a double bond between the two fragments. It is a sedating antihistamine with antimuscarinic and calcium-channel blocking actions. It is used (particularly as the hydrochloride sesquihydrate) for the relief of allergic conditions including rhinitis, conjunctivitis due to inhalant allergens and foods, urticaria and angioedema, and in pruritic skin disorders. Unlike other antihistamines, it is also a seratonin receptor antagonist, making it useful in conditions such as vascular headache and anorexia.		2.0310piperidines;
tertiary amine		anti-allergic agent;
antipruritic drug;
gastrointestinal drug;
H1-receptor antagonist;
serotonergic antagonist
desipramine
Desipramine: A tricyclic dibenzazepine compound that potentiates neurotransmission. Desipramine selectively blocks reuptake of norepinephrine from the neural synapse, and also appears to impair serotonin transport. This compound also possesses minor anticholinergic activity, through its affinity to muscarinic receptors.. desipramine : A dibenzoazepine consisting of 10,11-dihydro-5H-dibenzo[b,f]azepine substituted on nitrogen with a 3-(methylamino)propyl group.		2.0310dibenzoazepine;
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
amphetamine
Amphetamine: A powerful central nervous system stimulant and sympathomimetic. Amphetamine has multiple mechanisms of action including blocking uptake of adrenergics and dopamine, stimulation of release of monamines, and inhibiting monoamine oxidase. Amphetamine is also a drug of abuse and a psychotomimetic. The l- and the d,l-forms are included here. The l-form has less central nervous system activity but stronger cardiovascular effects. The d-form is DEXTROAMPHETAMINE.. 1-phenylpropan-2-amine : A primary amine that is isopropylamine in which a hydrogen attached to one of the methyl groups has been replaced by a phenyl group.. amphetamine : A racemate comprising equimolar amounts of (R)-amphetamine (also known as levamphetamine or levoamphetamine) and (S)-amphetamine (also known as dexamfetamine or dextroamphetamine.		2.0810primary amine
diazepam
Diazepam: A benzodiazepine with anticonvulsant, anxiolytic, sedative, muscle relaxant, and amnesic properties and a long duration of action. Its actions are mediated by enhancement of GAMMA-AMINOBUTYRIC ACID activity.. diazepam : A 1,4-benzodiazepinone that is 1,3-dihydro-2H-1,4-benzodiazepin-2-one substituted by a chloro group at position 7, a methyl group at position 1 and a phenyl group at position 5.		1.99101,4-benzodiazepinone;
organochlorine compound		anticonvulsant;
anxiolytic drug;
environmental contaminant;
sedative;
xenobiotic
fluoxetine
Fluoxetine: The first highly specific serotonin uptake inhibitor. It is used as an antidepressant and often has a more acceptable side-effects profile than traditional antidepressants.. fluoxetine : A racemate comprising equimolar amounts of (R)- and (S)-fluoxetine. A selective serotonin reuptake inhibitor (SSRI), it is used (generally as the hydrochloride salt) for the treatment of depression (and the depressive phase of bipolar disorder), bullimia nervosa, and obsessive-compulsive disorder.. N-methyl-3-phenyl-3-[4-(trifluoromethyl)phenoxy]propan-1-amine : An aromatic ether consisting of 4-trifluoromethylphenol in which the hydrogen of the phenolic hydroxy group is replaced by a 3-(methylamino)-1-phenylpropyl group.		2.0310(trifluoromethyl)benzenes;
aromatic ether;
secondary amino compound
haloperidol
Haloperidol: A phenyl-piperidinyl-butyrophenone that is used primarily to treat SCHIZOPHRENIA and other PSYCHOSES. It is also used in schizoaffective disorder, DELUSIONAL DISORDERS, ballism, and TOURETTE SYNDROME (a drug of choice) and occasionally as adjunctive therapy in INTELLECTUAL DISABILITY and the chorea of HUNTINGTON DISEASE. It is a potent antiemetic and is used in the treatment of intractable HICCUPS. (From AMA Drug Evaluations Annual, 1994, p279). haloperidol : A compound composed of a central piperidine structure with hydroxy and p-chlorophenyl substituents at position 4 and an N-linked p-fluorobutyrophenone moiety.		7.6730aromatic ketone;
hydroxypiperidine;
monochlorobenzenes;
organofluorine compound;
tertiary alcohol		antidyskinesia agent;
antiemetic;
dopaminergic antagonist;
first generation antipsychotic;
serotonergic antagonist
imipramine
Imipramine: The prototypical tricyclic antidepressant. It has been used in major depression, dysthymia, bipolar depression, attention-deficit disorders, agoraphobia, and panic disorders. It has less sedative effect than some other members of this therapeutic group.. imipramine : A dibenzoazepine that is 5H-dibenzo[b,f]azepine substituted by a 3-(dimethylamino)propyl group at the nitrogen atom.		2.0310dibenzoazepineadrenergic uptake inhibitor;
antidepressant;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor
meperidine
Meperidine: A narcotic analgesic that can be used for the relief of most types of moderate to severe pain, including postoperative pain and the pain of labor. Prolonged use may lead to dependence of the morphine type; withdrawal symptoms appear more rapidly than with morphine and are of shorter duration.. pethidine : A piperidinecarboxylate ester that is piperidine which is substituted by a methyl group at position 1 and by phenyl and ethoxycarbonyl groups at position 4. It is an analgesic which is used for the treatment of moderate to severe pain, including postoperative pain and labour pain.		1.9810ethyl ester;
piperidinecarboxylate ester;
tertiary amino compound		antispasmodic drug;
kappa-opioid receptor agonist;
mu-opioid receptor agonist;
opioid analgesic
methiothepin
Methiothepin: A serotonin receptor antagonist in the CENTRAL NERVOUS SYSTEM used as an antipsychotic.. methiothepin : A dibenzothiepine that is 10,11-dihydrodibenzo[b,f]thiepine bearing additional methylthio and 4-methylpiperazin-1-yl substituents at positions 8 and 10 respectively. Potent 5-HT2 antagonist, also active as 5-HT1 antagonist. Differentiates 5-HT1D sub-types. Also displays affinity for rodent 5-HT5B, 5-HT5A, 5-HT7 and 5-HT6 receptors (pK1 values are 6.6, 7.0, 8.4 and 8.7 respectively).		2.0310aryl sulfide;
dibenzothiepine;
N-alkylpiperazine;
tertiary amino compound		antipsychotic agent;
dopaminergic antagonist;
geroprotector;
serotonergic antagonist
metoprolol
Metoprolol: A selective adrenergic beta-1 blocking agent that is commonly used to treat ANGINA PECTORIS; HYPERTENSION; and CARDIAC ARRHYTHMIAS.. metoprolol : A propanolamine that is 1-(propan-2-ylamino)propan-2-ol substituted by a 4-(2-methoxyethyl)phenoxy group at position 1.		1.9910aromatic ether;
propanolamine;
secondary alcohol;
secondary amino compound		antihypertensive agent;
beta-adrenergic antagonist;
environmental contaminant;
geroprotector;
xenobiotic
mianserin
Mianserin: A tetracyclic compound with antidepressant effects. It may cause drowsiness and hematological problems. Its mechanism of therapeutic action is not well understood, although it apparently blocks alpha-adrenergic, histamine H1, and some types of serotonin receptors.. mianserin : A dibenzoazepine (specifically 1,2,3,4,10,14b-hexahydrodibenzo[c,f]pyrazino[1,2-a]azepine) methyl-substituted on N-2. Closely related to (and now mostly superseded by) the tetracyclic antidepressant mirtazapinean, it is an atypical antidepressant used in the treatment of depression throughout Europe and elsewhere.		7.4120dibenzoazepineadrenergic uptake inhibitor;
alpha-adrenergic antagonist;
antidepressant;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
geroprotector;
H1-receptor antagonist;
histamine agonist;
sedative;
serotonergic antagonist
mirtazapine
Mirtazapine: A piperazinoazepine tetracyclic compound that enhances the release of NOREPINEPHRINE and SEROTONIN through blockage of presynaptic ALPHA-2 ADRENERGIC RECEPTORS. It also blocks both 5-HT2 and 5-HT3 serotonin receptors and is a potent HISTAMINE H1 RECEPTOR antagonist. It is used for the treatment of depression, and may also be useful for the treatment of anxiety disorders.		2.0310benzazepine;
tetracyclic antidepressant		alpha-adrenergic antagonist;
anxiolytic drug;
H1-receptor antagonist;
histamine antagonist;
oneirogen;
serotonergic antagonist
1-(3-trifluoromethylphenyl)piperazine
1-(3-trifluoromethylphenyl)piperazine: acts as serotonin agonist; structure. 1-(3-(trifluoromethyl)phenyl)piperazine : A N-arylpiperazine that is piperazine substituted by a 3-(trifluoromethyl)phenyl group at position 1. A serotonergic agonist used as a recreational drug.		8.2360(trifluoromethyl)benzenes;
N-arylpiperazine		environmental contaminant;
psychotropic drug;
serotonergic agonist;
xenobiotic
fg 7142
FG 7142: benzodiazepine receptor agonist		1.9810beta-carbolines
nan 190
1-(2-methoxyphenyl)-4-(4-(2-phthalimido)butyl)piperazine: RN from Toxlit. NAN 190 : An N-alkylpiperazine that consists of (2-methoxyphenyl)piperazine in which the amine hydrogen is substituted by a 4-(2-phthalimido)butyl group.		2.9140N-alkylpiperazine;
N-arylpiperazine;
phthalimides		serotonergic antagonist
octopamine
Octopamine: An alpha-adrenergic sympathomimetic amine, biosynthesized from tyramine in the CNS and platelets and also in invertebrate nervous systems. It is used to treat hypotension and as a cardiotonic. The natural D(-) form is more potent than the L(+) form in producing cardiovascular adrenergic responses. It is also a neurotransmitter in some invertebrates.. octopamine : A member of the class of phenylethanolamines that is phenol which is substituted at the para- position by a 2-amino-1-hydroxyethyl group. A biogenic phenylethanolamine which has been found to act as a neurotransmitter, neurohormone or neuromodulator in invertebrates.		2.0310phenylethanolamines;
tyramines		neurotransmitter
oxidopamine
Oxidopamine: A neurotransmitter analogue that depletes noradrenergic stores in nerve endings and induces a reduction of dopamine levels in the brain. Its mechanism of action is related to the production of cytolytic free-radicals.. oxidopamine : A benzenetriol that is phenethylamine in which the hydrogens at positions 2, 4, and 5 on the phenyl ring are replaced by hydroxy groups. It occurs naturally in human urine, but is also produced as a metabolite of the drug DOPA (used for the treatment of Parkinson's disease).		3.0540benzenetriol;
catecholamine;
primary amino compound		drug metabolite;
human metabolite;
neurotoxin
oxprenolol
Oxprenolol: A beta-adrenergic antagonist used in the treatment of hypertension, angina pectoris, arrhythmias, and anxiety.		1.9910aromatic ether
pindolol
Pindolol: A moderately lipophilic beta blocker (ADRENERGIC BETA-ANTAGONISTS). It is non-cardioselective and has intrinsic sympathomimetic actions, but little membrane-stabilizing activity. (From Martindale, The Extra Pharmocopoeia, 30th ed, p638). pindolol : A member of the class of indols which is the 2-hydroxy-3-(isopropylamino)propyl ether derivative of 1H-indol-4-ol.		2.940indoles;
secondary amine		antiglaucoma drug;
antihypertensive agent;
beta-adrenergic antagonist;
serotonergic antagonist;
vasodilator agent
prazosin
Prazosin: A selective adrenergic alpha-1 antagonist used in the treatment of HEART FAILURE; HYPERTENSION; PHEOCHROMOCYTOMA; RAYNAUD DISEASE; PROSTATIC HYPERTROPHY; and URINARY RETENTION.. prazosin : A member of the class of piperazines that is piperazine substituted by a furan-2-ylcarbonyl group and a 4-amino-6,7-dimethoxyquinazolin-2-yl group at positions 1 and 4 respectively.		2.3920aromatic ether;
furans;
monocarboxylic acid amide;
piperazines;
quinazolines		alpha-adrenergic antagonist;
antihypertensive agent;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor
quipazine
Quipazine: A pharmacologic congener of serotonin that contracts smooth muscle and has actions similar to those of tricyclic antidepressants. It has been proposed as an oxytocic.		2.0810piperazines;
pyridines
ritanserin
Ritanserin: A selective and potent serotonin-2 antagonist that is effective in the treatment of a variety of syndromes related to anxiety and depression. The drug also improves the subjective quality of sleep and decreases portal pressure.. ritanserin : A thiazolopyrimidine that is 5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one which is substituted at position 7 by a methyl group and at position 6 by a 2-{4-[bis(4-fluorophenyl)methylidene]piperidin-1-yl}ethyl group. A potent and long-acting seratonin (5-hydroxytryptamine, 5-HT) antagonist of the subtype 5-HT2 (Ki = 0.39 nM), it is used in the treatment of a variety of disorders including anxiety, depression and schizophrenia. It has little sedative action.		1.9810organofluorine compound;
piperidines;
thiazolopyrimidine		antidepressant;
antipsychotic agent;
anxiolytic drug;
dopaminergic antagonist;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
serotonergic antagonist
trazodone
Trazodone: A serotonin uptake inhibitor that is used as an antidepressive agent. It has been shown to be effective in patients with major depressive disorders and other subsets of depressive disorders. It is generally more useful in depressive disorders associated with insomnia and anxiety. This drug does not aggravate psychotic symptoms in patients with schizophrenia or schizoaffective disorders. (From AMA Drug Evaluations Annual, 1994, p309). trazodone : An N-arylpiperazine in which one nitrogen is substituted by a 3-chlorophenyl group, while the other is substituted by a 3-(3-oxo[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)propyl group.		1.9910monochlorobenzenes;
N-alkylpiperazine;
N-arylpiperazine;
triazolopyridine		adrenergic antagonist;
antidepressant;
anxiolytic drug;
H1-receptor antagonist;
sedative;
serotonin uptake inhibitor
tyramine
[no description available]		2.0310monoamine molecular messenger;
primary amino compound;
tyramines		EC 3.1.1.8 (cholinesterase) inhibitor;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
neurotransmitter
dextroamphetamine
Dextroamphetamine: The d-form of AMPHETAMINE. It is a central nervous system stimulant and a sympathomimetic. It has also been used in the treatment of narcolepsy and of attention deficit disorders and hyperactivity in children. Dextroamphetamine has multiple mechanisms of action including blocking uptake of adrenergics and dopamine, stimulating release of monamines, and inhibiting monoamine oxidase. It is also a drug of abuse and a psychotomimetic.. (S)-amphetamine : A 1-phenylpropan-2-amine that has S configuration.		2.03101-phenylpropan-2-amineadrenergic agent;
adrenergic uptake inhibitor;
dopamine uptake inhibitor;
dopaminergic agent;
neurotoxin;
sympathomimetic agent
apomorphine
Apomorphine: A derivative of morphine that is a dopamine D2 agonist. It is a powerful emetic and has been used for that effect in acute poisoning. It has also been used in the diagnosis and treatment of parkinsonism, but its adverse effects limit its use.		2.0810aporphine alkaloidalpha-adrenergic drug;
antidyskinesia agent;
antiparkinson drug;
dopamine agonist;
emetic;
serotonergic drug
levodopa
Levodopa: The naturally occurring form of DIHYDROXYPHENYLALANINE and the immediate precursor of DOPAMINE. Unlike dopamine itself, it can be taken orally and crosses the blood-brain barrier. It is rapidly taken up by dopaminergic neurons and converted to DOPAMINE. It is used for the treatment of PARKINSONIAN DISORDERS and is usually given with agents that inhibit its conversion to dopamine outside of the central nervous system.. L-dopa : An optically active form of dopa having L-configuration. Used to treat the stiffness, tremors, spasms, and poor muscle control of Parkinson's disease		6.24111amino acid zwitterion;
dopa;
L-tyrosine derivative;
non-proteinogenic L-alpha-amino acid		allelochemical;
antidyskinesia agent;
antiparkinson drug;
dopaminergic agent;
hapten;
human metabolite;
mouse metabolite;
neurotoxin;
plant growth retardant;
plant metabolite;
prodrug
phenylalanine
Phenylalanine: An essential aromatic amino acid that is a precursor of MELANIN; DOPAMINE; noradrenalin (NOREPINEPHRINE), and THYROXINE.. L-phenylalanine : The L-enantiomer of phenylalanine.. phenylalanine : An aromatic amino acid that is alanine in which one of the methyl hydrogens is substituted by a phenyl group.		2.0310amino acid zwitterion;
erythrose 4-phosphate/phosphoenolpyruvate family amino acid;
L-alpha-amino acid;
phenylalanine;
proteinogenic amino acid		algal metabolite;
EC 3.1.3.1 (alkaline phosphatase) inhibitor;
Escherichia coli metabolite;
human xenobiotic metabolite;
micronutrient;
mouse metabolite;
nutraceutical;
plant metabolite;
Saccharomyces cerevisiae metabolite
cycloserine
Cycloserine: Antibiotic substance produced by Streptomyces garyphalus.. D-cycloserine : A 4-amino-1,2-oxazolidin-3-one that has R configuration. It is an antibiotic produced by Streptomyces garyphalus or S. orchidaceus and is used as part of a multi-drug regimen for the treatment of tuberculosis when resistance to, or toxicity from, primary drugs has developed. An analogue of D-alanine, it interferes with bacterial cell wall synthesis in the cytoplasm by competitive inhibition of L-alanine racemase (which forms D-alanine from L-alanine) and D-alanine--D-alanine ligase (which incorporates D-alanine into the pentapeptide required for peptidoglycan formation and bacterial cell wall synthesis).		2.03104-amino-1,2-oxazolidin-3-one;
organonitrogen heterocyclic antibiotic;
organooxygen heterocyclic antibiotic;
zwitterion		antiinfective agent;
antimetabolite;
antitubercular agent;
metabolite;
NMDA receptor agonist
gramine
gramine : An aminoalkylindole that is indole carrying a dimethylaminomethyl substituent at postion 3.		2.0310aminoalkylindole;
indole alkaloid;
tertiary amino compound		antibacterial agent;
antiviral agent;
plant metabolite;
serotonergic antagonist
phenylpiperazine
phenylpiperazine: RN given refers to parent cpd		2.9240
yohimbine
Yohimbine: A plant alkaloid with alpha-2-adrenergic blocking activity. Yohimbine has been used as a mydriatic and in the treatment of ERECTILE DYSFUNCTION.. yohimbine : An indole alkaloid with alpha2-adrenoceptor antagonist activity. It is produced by Corynanthe johimbe and Rauwolfia serpentina.		1.9810methyl 17-hydroxy-20xi-yohimban-16-carboxylatealpha-adrenergic antagonist;
dopamine receptor D2 antagonist;
serotonergic antagonist
thiazoles
[no description available]		1.99101,3-thiazoles;
mancude organic heteromonocyclic parent;
monocyclic heteroarene
ketobemidone
ketobemidone: structure		1.9810piperidines
bufotenin
Bufotenin: A hallucinogenic serotonin analog found in frog or toad skins, mushrooms, higher plants, and mammals, especially in the brains, plasma, and urine of schizophrenics. Bufotenin has been used as a tool in CNS studies and misused as a psychedelic.. bufotenin : A tertiary amine that consists of N,N-dimethyltryptamine bearing an additional hydroxy substituent at position 5.		1.9910tertiary amine;
tryptamine alkaloid		coral metabolite;
hallucinogen
fluanisone
fluanisone: former provisional as haloanisone; structure; RN given refers to parent cpd		1.9910aromatic ketone
glutamic acid
Glutamic Acid: A non-essential amino acid naturally occurring in the L-form. Glutamic acid is the most common excitatory neurotransmitter in the CENTRAL NERVOUS SYSTEM.. glutamic acid : An alpha-amino acid that is glutaric acid bearing a single amino substituent at position 2.		2.4220glutamic acid;
glutamine family amino acid;
L-alpha-amino acid;
proteinogenic amino acid		Escherichia coli metabolite;
ferroptosis inducer;
micronutrient;
mouse metabolite;
neurotransmitter;
nutraceutical
timolol
(S)-timolol (anhydrous) : The (S)-(-) (more active) enantiomer of timolol. A beta-adrenergic antagonist, both the hemihydrate and the maleate salt are used in the mangement of glaucoma, hypertension, angina pectoris and myocardial infarction, and for the prevention of migraine.		1.9910timololanti-arrhythmia drug;
antiglaucoma drug;
antihypertensive agent;
beta-adrenergic antagonist
5,7-dihydroxytryptamine
5,7-Dihydroxytryptamine: Tryptamine substituted with two hydroxyl groups in positions 5 and 7. It is a neurotoxic serotonin analog that destroys serotonergic neurons preferentially and is used in neuropharmacology as a tool.		2.3920
tertatolol
tertatolol: RN given refers to parent cpd; structure given in first source		1.9910thiochromane
penbutolol
Penbutolol: A nonselective beta-blocker used as an antihypertensive and an antianginal agent.		1.9910ethanolamines
paroxetine
Paroxetine: A serotonin uptake inhibitor that is effective in the treatment of depression.. paroxetine : A benzodioxole that consists of piperidine bearing 1,3-benzodioxol-5-yloxy)methyl and 4-fluorophenyl substituents at positions 3 and 4 respectively; the (3S,4R)-diastereomer. Highly potent and selective 5-HT uptake inhibitor that binds with high affinity to the serotonin transporter (Ki = 0.05 nM). Ki values are 1.1, 350 and 1100 nM for inhibition of [3H]-5-HT, [3H]-l-NA and [3H]-DA uptake respectively. Displays minimal affinity for alpha1-, alpha2- or beta-adrenoceptors, 5-HT2A, 5-HT1A, D2 or H1 receptors at concentrations below 1000 nM, however displays weak affinity for muscarinic ACh receptors (Ki = 42 nM). Antidepressant and anxiolytic in vivo.		7.420aromatic ether;
benzodioxoles;
organofluorine compound;
piperidines		antidepressant;
anxiolytic drug;
hepatotoxic agent;
P450 inhibitor;
serotonin uptake inhibitor
ipsapirone
[no description available]		8.3870N-arylpiperazine
flesinoxan
[no description available]		3.150
sertindole
sertindole : A phenylindole that is 1H-indole which is substituted on the nitrogen by a p-chlorophenyl group, at position 5 by chlorine, and at position 3 by a piperidin-4-yl group, which is itself substituted on the nitrogen by a 2-(2-oxoimidazolidin-1-yl)ethyl group.		1.9810heteroarylpiperidine;
imidazolidinone;
organochlorine compound;
organofluorine compound;
phenylindole		alpha-adrenergic antagonist;
H1-receptor antagonist;
second generation antipsychotic;
serotonergic antagonist
triazoles
Triazoles: Heterocyclic compounds containing a five-membered ring with two carbon atoms and three nitrogen atoms with the molecular formula C2H3N3.. triazoles : An azole in which the five-membered heterocyclic aromatic skeleton contains three N atoms and two C atoms.		2.59201,2,3-triazole
sertraline
Sertraline: A selective serotonin uptake inhibitor that is used in the treatment of depression.. sertraline : A member of the class of tetralins that is tetralin which is substituted at positions 1 and 4 by a methylamino and a 3,4-dichlorophenyl group, respectively (the S,S diastereoisomer). A selective serotonin-reuptake inhibitor (SSRI), it is administered orally as the hydrochloride salt as an antidepressant for the treatment of depression, obsessive-compulsive disorder, panic disorder and post-traumatic stress disorder.		2.0310dichlorobenzene;
secondary amino compound;
tetralins		antidepressant;
serotonin uptake inhibitor
fluprazine
fluprazine: anti-aggressive agent in rats; RN given refers to parent cpd		7.3820
kampirone
1-(2-pyrimidinyl)piperazine: metabolite of buspirone; structure given in first source		1.9910N-arylpiperazine
n,n-dipropyl-2-aminotetralin
N,N-dipropyl-2-aminotetralin: RN given refers to parent cpd		1.9910
gr 127935
GR 127935: a 5-HT 1D receptor antagonist. GR 127935 : A member of the class of benzamides obtained by formal condensation of the carboxy group of 2'-methyl-4'-(5-methyl-1,2,4-oxadiazol-3-yl)biphenyl-4-carboxylic acid and the anilino group of 4-methoxy-3-(4-methylpiperazin-1-yl)aniline. Potent and selective 5-HT1B/1D receptor antagonist (pKi values are 8.5 for both guinea pig 5-HT1D and rat 5-HT1B receptors). Displays > 100-fold selectivity over 5HT1A, 5-HT2A, 5-HT2C receptors and other receptor types. Centrally active following oral administration.		2.03101,2,4-oxadiazole;
benzamides;
N-alkylpiperazine;
N-arylpiperazine
5-methoxy 3-(1,2,3,6-tetrahydro-4-pyridinyl)1h indole
[no description available]		2.940indoles
3-propylamino-5-hydroxychroman
[no description available]		1.9910
s 14671
S 14671: serotonin receptor agonist; RN from toxlit		1.9910
4-(benzodioxan-5-yl)-1-(indan-2-yl)piperazine
[no description available]		2.6830
dilevalol
(R,R)-labetalol : A 2-hydroxy-5-{1-hydroxy-2-[(4-phenylbutan-2-yl)amino]ethyl}benzamide that has 1R,2R-configuration.		1.99102-hydroxy-5-{1-hydroxy-2-[(4-phenylbutan-2-yl)amino]ethyl}benzamide
n-methylserotonin
N-methylserotonin: RN given refers to parent cpd. N-methylserotonin : A member of the class of tryptamines that is serotonin in which one of the hydrogens attached to the primary amino group is replaced by a methyl group.		1.9910phenols;
tryptamines		human metabolite;
plant metabolite
3-(1-methyl-1,2,3,6-tetrahydropyrid-4-yl)indole
3-(1-methyl-1,2,3,6-tetrahydropyrid-4-yl)indole: structure given in first source		1.9910
6-hydroxytryptamine
6-hydroxytryptamine: RN given refers to parent cpd		1.9910
alnespirone
alnespirone: S 20499 is the (+)-enantiomer; S 20500 is the (-)-enantiomer		710
8-methoxy-2-(di-n-propylamino)tetralin
8-methoxy-2-(di-n-propylamino)tetralin: RN given refers to parent cpd without isomeric designation		1.9910
bmy 7378
[no description available]		1.9810
1-(4-methoxyphenyl)piperazine
1-(4-methoxyphenyl)piperazine: a designer drug; structure in first source		1.9810
4,4-dicarboxy-5-pyridoxylproline
[no description available]		2.0810
femoxetine
femoxetine: serotonin uptake inhibitor; RN given refers to (3R-trans)-isomer		6.9810piperidines
5-methoxy-3-(di-n-propylamino)chroman
5-methoxy-3-(di-n-propylamino)chroman: labels central 5-HT receptor binding sites		1.9910
mm 77
[no description available]		2.0310piperazines
fluvoxamine
Fluvoxamine: A selective serotonin reuptake inhibitor that is used in the treatment of DEPRESSION and a variety of ANXIETY DISORDERS.. fluvoxamine : An oxime O-ether that is benzene substituted by a (1E)-N-(2-aminoethoxy)-5-methoxypentanimidoyl group at position 1 and a trifluoromethyl group at position 4. It is a selective serotonin reuptake inhibitor that is used for the treatment of obsessive-compulsive disorder.		1.9910(trifluoromethyl)benzenes;
5-methoxyvalerophenone O-(2-aminoethyl)oxime		antidepressant;
anxiolytic drug;
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
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: 5-HT(1A) receptor antagonist; structure in first source		1.9910
oxadiazoles
Oxadiazoles: Compounds containing five-membered heteroaromatic rings containing two carbons, two nitrogens, and one oxygen atom which exist in various regioisomeric forms.		2.0310
scopolamine hydrobromide
[no description available]		1.9810
piperidines
Piperidines: A family of hexahydropyridines.		1.9810
guanosine triphosphate
Guanosine Triphosphate: Guanosine 5'-(tetrahydrogen triphosphate). A guanine nucleotide containing three phosphate groups esterified to the sugar moiety.		1.9710guanosine 5'-phosphate;
purine ribonucleoside 5'-triphosphate		Escherichia coli metabolite;
mouse metabolite;
uncoupling protein inhibitor
guanylyl imidodiphosphate
Guanylyl Imidodiphosphate: A non-hydrolyzable analog of GTP, in which the oxygen atom bridging the beta to the gamma phosphate is replaced by a nitrogen atom. It binds tightly to G-protein in the presence of Mg2+. The nucleotide is a potent stimulator of ADENYLYL CYCLASES.. guanosine 5'-[beta,gamma-imido]triphosphate : A nucleoside triphosphate analogue that is GTP in which the oxygen atom bridging the beta- to the gamma- phosphate is replaced by a nitrogen atom A non-hydrolyzable analog of GTP, it binds tightly to G-protein in the presence of Mg(2+).		1.9710nucleoside triphosphate analogue
ConditionIndicatedRelationship StrengthStudiesTrials
Starvation
Lengthy and continuous deprivation of food. (Stedman, 25th ed)		02.0310
Aging
The gradual irreversible changes in structure and function of an organism that occur as a result of the passage of time.		02.0310
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		03.3960
Dyskinesia, Medication-Induced
[description not available]		06.24111
Dyskinesia, Drug-Induced
Abnormal movements, including HYPERKINESIS; HYPOKINESIA; TREMOR; and DYSTONIA, associated with the use of certain medications or drugs. Muscles of the face, trunk, neck, and extremities are most commonly affected. Tardive dyskinesia refers to abnormal hyperkinetic movements of the muscles of the face, tongue, and neck associated with the use of neuroleptic agents (see ANTIPSYCHOTIC AGENTS). (Adams et al., Principles of Neurology, 6th ed, p1199)		06.24111
Autosomal Dominant Juvenile Parkinson Disease
[description not available]		02.8330
Parkinsonian Disorders
A group of disorders which feature impaired motor control characterized by bradykinesia, MUSCLE RIGIDITY; TREMOR; and postural instability. Parkinsonian diseases are generally divided into primary parkinsonism (see PARKINSON DISEASE), secondary parkinsonism (see PARKINSON DISEASE, SECONDARY) and inherited forms. These conditions are associated with dysfunction of dopaminergic or closely related motor integration neuronal pathways in the BASAL GANGLIA.		02.8330
Body Weight
The mass or quantity of heaviness of an individual. It is expressed by units of pounds or kilograms.		02.1510
Anxiety
Feelings or emotions of dread, apprehension, and impending disaster but not disabling as with ANXIETY DISORDERS.		02.4320
Idiopathic Parkinson Disease
[description not available]		05.871
Parkinson Disease
A progressive, degenerative neurologic disease characterized by a TREMOR that is maximal at rest, retropulsion (i.e. a tendency to fall backwards), rigidity, stooped posture, slowness of voluntary movements, and a masklike facial expression. Pathologic features include loss of melanin containing neurons in the substantia nigra and other pigmented nuclei of the brainstem. LEWY BODIES are present in the substantia nigra and locus coeruleus but may also be found in a related condition (LEWY BODY DISEASE, DIFFUSE) characterized by dementia in combination with varying degrees of parkinsonism. (Adams et al., Principles of Neurology, 6th ed, p1059, pp1067-75)		05.871
ADDH
[description not available]		02.9810
Attention Deficit Disorder with Hyperactivity
A behavior disorder originating in childhood in which the essential features are signs of developmentally inappropriate inattention, impulsivity, and hyperactivity. Although most individuals have symptoms of both inattention and hyperactivity-impulsivity, one or the other pattern may be predominant. The disorder is more frequent in males than females. Onset is in childhood. Symptoms often attenuate during late adolescence although a minority experience the full complement of symptoms into mid-adulthood. (From DSM-V)		02.9810
Deficiency, Mental
[description not available]		04.9733
Aggression
Behavior which may be manifested by destructive and attacking action which is verbal or physical, by covert attitudes of hostility or by obstructionism.		07.39173
Intellectual Disability
Subnormal intellectual functioning which originates during the developmental period. This has multiple potential etiologies, including genetic defects and perinatal insults. Intelligence quotient (IQ) scores are commonly used to determine whether an individual has an intellectual disability. IQ scores between 70 and 79 are in the borderline range. Scores below 67 are in the disabled range. (from Joynt, Clinical Neurology, 1992, Ch55, p28)		04.9733
Dementia Praecox
[description not available]		03.3711
Schizophrenia
A severe emotional disorder of psychotic depth characteristically marked by a retreat from reality with delusion formation, HALLUCINATIONS, emotional disharmony, and regressive behavior.		08.3711
Behavior Disorders
[description not available]		03.3711
Mental Disorders
Psychiatric illness or diseases manifested by breakdowns in the adaptational process expressed primarily as abnormalities of thought, feeling, and behavior producing either distress or impairment of function.		03.3711
Inadequate Sleep
[description not available]		01.9810
Hypothermia, Accidental
[description not available]		0210
Hypothermia
Lower than normal body temperature, especially in warm-blooded animals.		0210
Claustrophobia
[description not available]		01.9710
Phobic Disorders
Anxiety disorders in which the essential feature is persistent and irrational fear of a specific object, activity, or situation that the individual feels compelled to avoid. The individual recognizes the fear as excessive or unreasonable.		01.9710