Compounds > tiospirone
Page last updated: 2024-12-06

tiospirone

Description

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

Cross-References

ID SourceID
PubMed CID55752
CHEMBL ID35057
SCHEMBL ID78696
MeSH IDM0125991

Synonyms (30)

Synonym
gtpl101
tiospyrone
bmy-13859
PDSP2_000472
PDSP1_000474
PDSP2_000471
tiospirone
PDSP1_000473
tiospironum [latin]
tiospirone [inn]
tiospirona [spanish]
8-azaspiro(4,5)decane-7,9-dione, 8-(4-(4-(1,2-benzisothiazol-3-yl)-1-piperazinyl)butyl)-
CHEMBL35057 ,
L000720
bdbm50007692
8-[4-(4-benzo[d]isothiazol-3-yl-piperazin-1-yl)-butyl]-8-aza-spiro[4.5]decane-7,9-dione
tiosperone
8-[4-[4-(1,2-benzothiazol-3-yl)piperazin-1-yl]butyl]-8-azaspiro[4.5]decane-7,9-dione
35c6umo5sr ,
tiospironum
tiospirona
87691-91-6
unii-35c6umo5sr
SCHEMBL78696
ZFZPJDFBJFHYIV-UHFFFAOYSA-N
8-[4-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]butyl]-8-azaspiro[4.5]decane-7,9-dione
DTXSID90236558
Q13415380
mj 13859; nih 10766
AKOS040746412

Research Excerpts

Overview

Tiospirone (TSP) is an atypical antipsychotic drug. It can decrease consumption of ethanol while increasing food intake.

ExcerptReferenceRelevance
"Tiospirone (TSP) is a 5-HT2 receptor antagonist with affinity for D2, 5-HT1a, and 5-HT7, and sigma receptors, which can decrease consumption of ethanol while increasing food intake."( Effects of amperozide and tiospirone, atypical antipsychotic 5-HT2 drugs, on food-reinforced behavior in rats.
Arolfo, MP; McMillen, BA, )		1.15
"Tiospirone (TSP) is an atypical antipsychotic drug. "( Tiospirone and the reinforcing effects of cocaine in the conditioned place preference paradigm in rats.
Arolfo, MP; McMillen, BA, 2000)		3.19

Effects

ExcerptReferenceRelevance
"Tiospirone has demonstrated preclinical activities that predict utility as an antipsychotic drug which lacks the potential to produce extrapyramidal side effects. "( Radioreceptor assay of dopamine binding activity in human serum after tiospirone administration.
Hyslop, DK; Shukla, UA; Taylor, DP; Westrick, ML, 1989)		1.95

Dosage Studied

ExcerptRelevanceReference
" A comparison of levels of dopamine binding activity present in serum samples taken immediately prior to dosing on various days during the course of the study suggested that steady-state was achieved within seven days with repeated administration."( Radioreceptor assay of dopamine binding activity in human serum after tiospirone administration.
Hyslop, DK; Shukla, UA; Taylor, DP; Westrick, ML, 1989)		0.51
" The dissociation constant (K(B)) and relative intrinsic efficacy (E(r)) for each partial agonist were calculated using a partial agonist interaction null model in which the effects of fixed concentrations of each partial agonist on the dopamine dose-response curve were evaluated."( Nonlinear analysis of partial dopamine agonist effects on cAMP in C6 glioma cells.
Abell, C; Avalos, M; Kwan, SW; Mak, C; Randall, PK; Trzeciakowski, JP; Wilcox, RE, )		0.13
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (7)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
5-hydroxytryptamine receptor 2CRattus norvegicus (Norway rat)IC50 (µMol)0.00200.00040.629810.0000AID4803
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)IC50 (µMol)0.00200.00040.908610.0000AID4803
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)Ki0.00060.00010.601710.0000AID5328
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)Ki0.00150.00010.949010.0000AID36016
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)Ki0.00150.00000.575110.0000AID36016
5-hydroxytryptamine receptor 2BRattus norvegicus (Norway rat)IC50 (µMol)0.00200.00040.615610.0000AID4803
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)Ki0.00150.00000.965010.0000AID36016
D(2) dopamine receptorRattus norvegicus (Norway rat)IC50 (µMol)0.00840.00010.54948.4000AID61404
D(2) dopamine receptorRattus norvegicus (Norway rat)Ki0.00210.00000.437510.0000AID63811; AID65713
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (58)

Assay IDTitleYearJournalArticle
AID177499In vivo inhibition of amphetamine induced stereotypy in rat by the compound administered intraperitoneally; nt=Not tested1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Synthesis and biological evaluation of a series of substituted N-alkoxyimides and -amides as potential atypical antipsychotic agents.
AID176804In vivo activity administered intraperitoneally was determined by pole climb avoidance in rat1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Synthesis and biological evaluation of a series of substituted N-alkoxyimides and -amides as potential atypical antipsychotic agents.
AID176744Dose inhibiting conditioned avoidance response in rats after oral administration1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID227559Relative binding affinity for dopamine D2 and alpha receptors1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID184033In vivo activity administered intraperitoneally was determined by induction of catalepsy in rat at 20 uM1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Synthesis and biological evaluation of a series of substituted N-alkoxyimides and -amides as potential atypical antipsychotic agents.
AID35277Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in rat brain1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents.
AID3720Binding affinity against 5-hydroxytryptamine 1A receptor of rat hippocampal tissue with [3H]8-OH-DPAT1991Journal of medicinal chemistry, Nov, Volume: 34, Issue:11
Synthesis and biological activity of the putative metabolites of the atypical antipsychotic agent tiospirone.
AID63811Displacement of [3H]NPA from rat brain Dopamine receptor D21996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID177516In vivo inhibition of conditional avoidance response in rats(CAR), after po administration1991Journal of medicinal chemistry, Nov, Volume: 34, Issue:11
Synthesis and biological activity of the putative metabolites of the atypical antipsychotic agent tiospirone.
AID176803In vivo activity administered intraperitoneally was determined by intracranial self stimulation in rat1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Synthesis and biological evaluation of a series of substituted N-alkoxyimides and -amides as potential atypical antipsychotic agents.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' 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
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]
AID176735Dose (administered orally) inhibiting spontaneous locomotor behavior in rats1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents.
AID176734Dose (administered orally) inhibiting apomorphine-induced stereotypy in rats1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents.
AID4803Compound was measured for affinity at 5-hydroxytryptamine 2 receptor in rat cortical by [3H]spiroperidol displacement.1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Synthesis and biological evaluation of a series of substituted N-alkoxyimides and -amides as potential atypical antipsychotic agents.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID184034In vivo activity administered intraperitoneally was determined by social interaction of rat at 1.0 uM1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Synthesis and biological evaluation of a series of substituted N-alkoxyimides and -amides as potential atypical antipsychotic agents.
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]
AID227557In vitro ability to displace [3H]ketanserin from 5-hydroxytryptamine 2A receptor in rat brain1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents.
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]
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]
AID61562Compound was measured for affinity at dopamine receptor D2 labeled with [3H]spiroperidol radioligand in striatum tissue1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Synthesis and biological evaluation of a series of substituted N-alkoxyimides and -amides as potential atypical antipsychotic agents.
AID36708Binding affinity against Alpha-1 adrenergic receptor of rat cerebral cortex with [3H]WB-41011991Journal of medicinal chemistry, Nov, Volume: 34, Issue:11
Synthesis and biological activity of the putative metabolites of the atypical antipsychotic agent tiospirone.
AID231370Ratio representing inhibitory activity against spontaneous locomotor behavior to inhibitory activity against amphetamine-induced stereotypy in rats1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents.
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]
AID61404Binding affinity against Dopamine receptor D2 receptor of rat corpus striatal tissue with [3H]spiperone1991Journal of medicinal chemistry, Nov, Volume: 34, Issue:11
Synthesis and biological activity of the putative metabolites of the atypical antipsychotic agent tiospirone.
AID36016Displacement of [3H]prazosin from rat brain Alpha-1 adrenergic receptor1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents.
AID231369Ratio representing inhibitory activity against catalepsy to inhibitory activity against amphetamine-induced locomotor behavior in rats1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents.
AID177515In vivo inhibition of conditional avoidance response in rats(CAR), after im administration1991Journal of medicinal chemistry, Nov, Volume: 34, Issue:11
Synthesis and biological activity of the putative metabolites of the atypical antipsychotic agent tiospirone.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID176805In vivo activity administered intraperitoneally was determined by pole climb escape failures in rat1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Synthesis and biological evaluation of a series of substituted N-alkoxyimides and -amides as potential atypical antipsychotic agents.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID176743Dose inducing catalepsy in rats after oral administration1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents.
AID63640Selectivity ratio of IC50 for dopamine receptor and Alpha-1 receptor1991Journal of medicinal chemistry, Nov, Volume: 34, Issue:11
Synthesis and biological activity of the putative metabolites of the atypical antipsychotic agent tiospirone.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID176733Dose (administered orally) inhibiting amphetamine-induced locomotor behavior in rats1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents.
AID65713Displacement of [3H]NPA from rat brain Dopamine receptor D21996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents.
AID3743Affinity for 5-hydroxytryptamine 1A receptor labeled with [3H]8-OH-DPAT radioligand in hippocampus tissue1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Synthesis and biological evaluation of a series of substituted N-alkoxyimides and -amides as potential atypical antipsychotic agents.
AID5573Relative binding affinity for D2 receptor and 5-hydroxytryptamine 2A receptor, ratio of Ki1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents.
AID5102Binding affinity against rat 5-hydroxytryptamine 2 receptor in rat cerebral cortex tissue using [3H]spiperone as radioligand1991Journal of medicinal chemistry, Nov, Volume: 34, Issue:11
Synthesis and biological activity of the putative metabolites of the atypical antipsychotic agent tiospirone.
AID5328Displacement of [3H]-ketanserin from rat brain 5-hydroxytryptamine 2A receptor1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents.
AID130881Inhibition of apomorphine induced mouse climbing, administered intraperitoneally1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Synthesis and biological evaluation of a series of substituted N-alkoxyimides and -amides as potential atypical antipsychotic agents.
AID177506In vivo inhibition of apomorphine induced stereotypy in rat by the compound administered intraperitoneally1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Synthesis and biological evaluation of a series of substituted N-alkoxyimides and -amides as potential atypical antipsychotic agents.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1345154Rat 5-HT6 receptor (5-Hydroxytryptamine receptors)1994The Journal of pharmacology and experimental therapeutics, Mar, Volume: 268, Issue:3
Binding of typical and atypical antipsychotic agents to 5-hydroxytryptamine-6 and 5-hydroxytryptamine-7 receptors.
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.
AID1346893Human 5-HT2C receptor (5-Hydroxytryptamine receptors)2000The Journal of pharmacology and experimental therapeutics, Oct, Volume: 295, Issue:1
Inverse agonist activity of atypical antipsychotic drugs at human 5-hydroxytryptamine2C receptors.
AID624215Antagonists 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.
AID1345235Rat 5-HT7 receptor (5-Hydroxytryptamine receptors)1994The Journal of pharmacology and experimental therapeutics, Mar, Volume: 268, Issue:3
Binding of typical and atypical antipsychotic agents to 5-hydroxytryptamine-6 and 5-hydroxytryptamine-7 receptors.
AID1345170Human 5-HT6 receptor (5-Hydroxytryptamine receptors)1996Journal of neurochemistry, Jan, Volume: 66, Issue:1
Cloning, characterization, and chromosomal localization of a human 5-HT6 serotonin receptor.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (23)

TimeframeStudies, This Drug (%)All Drugs %
pre-199011 (47.83)18.7374
1990's10 (43.48)18.2507
2000's2 (8.70)29.6817
2010's0 (0.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 20.36

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 Index20.36 (24.57)
Research Supply Index3.40 (2.92)
Research Growth Index4.47 (4.65)
Search Engine Demand Index18.60 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (20.36)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials2 (7.41%)5.53%
Reviews1 (3.70%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other24 (88.89%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
choline
[no description available]		1.9710cholinesallergen;
Daphnia magna metabolite;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
neurotransmitter;
nutrient;
plant metabolite;
Saccharomyces cerevisiae metabolite
3,4-dihydroxyphenylacetic acid
3,4-Dihydroxyphenylacetic Acid: A deaminated metabolite of LEVODOPA.. (3,4-dihydroxyphenyl)acetic acid : A dihydroxyphenylacetic acid having the two hydroxy substituents located at the 3- and 4-positions. It is a metabolite of dopamine.. dihydroxyphenylacetic acid : A dihydroxy monocarboxylic acid consisting of phenylacetic acid having two phenolic hydroxy substituents.		1.9810catechols;
dihydroxyphenylacetic acid		human metabolite
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		1.9910phenols;
tertiary amino compound;
tetralins		serotonergic antagonist
sk&f-38393
2,3,4,5-Tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepine: A selective D1 dopamine receptor agonist used primarily as a research tool.. 1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine-7,8-diol : A benzazepine that is 2,3,4,5-tetrahydro-3-benzazepine bearing a phenyl substituent at position 1 and two hydroxy substituents at positions 7 and 8.. SKF 38393 : A racemate comprising equimolar amounts of (R)- and (S)-SKF 38393		1.9710benzazepine;
catechols;
secondary amino compound
5-carboxamidotryptamine
5-carboxamidotryptamine: agonist of 5-HT receptor; structure given in first source		2.420tryptamines
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
amitriptyline
Amitriptyline: Tricyclic antidepressant with anticholinergic and sedative properties. It appears to prevent the re-uptake of norepinephrine and serotonin at nerve terminals, thus potentiating the action of these neurotransmitters. Amitriptyline also appears to antagonize cholinergic and alpha-1 adrenergic responses to bioactive amines.. amitriptyline : An organic tricyclic compound that is 10,11-dihydro-5H-dibenzo[a,d][7]annulene substituted by a 3-(dimethylamino)propylidene group at position 5.		1.9910carbotricyclic compound;
tertiary amine		adrenergic uptake inhibitor;
antidepressant;
environmental contaminant;
tropomyosin-related kinase B receptor agonist;
xenobiotic
amoxapine
Amoxapine: The N-demethylated derivative of the antipsychotic agent LOXAPINE that works by blocking the reuptake of norepinephrine, serotonin, or both; it also blocks dopamine receptors. Amoxapine is used for the treatment of depression.. amoxapine : A dibenzooxazepine compound having a chloro substituent at the 2-position and a piperazin-1-yl group at the 11-position.		2.3920dibenzooxazepineadrenergic uptake inhibitor;
antidepressant;
dopaminergic antagonist;
geroprotector;
serotonin uptake inhibitor
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.		1.9910azaspiro compound;
N-alkylpiperazine;
N-arylpiperazine;
organic heteropolycyclic compound;
piperidones;
pyrimidines		anxiolytic drug;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
sedative;
serotonergic agonist
chlorpromazine
Chlorpromazine: The prototypical phenothiazine antipsychotic drug. Like the other drugs in this class chlorpromazine's antipsychotic actions are thought to be due to long-term adaptation by the brain to blocking DOPAMINE RECEPTORS. Chlorpromazine has several other actions and therapeutic uses, including as an antiemetic and in the treatment of intractable hiccup.. chlorpromazine : A substituted phenothiazine in which the ring nitrogen at position 10 is attached to C-3 of an N,N-dimethylpropanamine moiety.		3.2360organochlorine compound;
phenothiazines;
tertiary amine		anticoronaviral agent;
antiemetic;
dopaminergic antagonist;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
phenothiazine antipsychotic drug
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.		1.9910piperidines;
tertiary amine		anti-allergic agent;
antipruritic drug;
gastrointestinal drug;
H1-receptor antagonist;
serotonergic antagonist
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.		1.9610primary amine
fluphenazine
[no description available]		2.3820N-alkylpiperazine;
organofluorine compound;
phenothiazines		anticoronaviral agent;
dopaminergic antagonist;
phenothiazine antipsychotic drug
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.		3.5990aromatic ketone;
hydroxypiperidine;
monochlorobenzenes;
organofluorine compound;
tertiary alcohol		antidyskinesia agent;
antiemetic;
dopaminergic antagonist;
first generation antipsychotic;
serotonergic antagonist
ketanserin
Ketanserin: A selective serotonin receptor antagonist with weak adrenergic receptor blocking properties. The drug is effective in lowering blood pressure in essential hypertension. It also inhibits platelet aggregation. It is well tolerated and is particularly effective in older patients.. ketanserin : A member of the class of quinazolines that is quinazoline-2,4(1H,3H)-dione which is substituted at position 3 by a 2-[4-(p-fluorobenzoyl)piperidin-1-yl]ethyl group.		1.9810aromatic ketone;
organofluorine compound;
piperidines;
quinazolines		alpha-adrenergic antagonist;
antihypertensive agent;
cardiovascular drug;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
serotonergic antagonist
loxapine
Loxapine: An antipsychotic agent used in SCHIZOPHRENIA.		2.940dibenzooxazepineantipsychotic agent;
dopaminergic antagonist
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).		2.420aryl sulfide;
dibenzothiepine;
N-alkylpiperazine;
tertiary amino compound		antipsychotic agent;
dopaminergic antagonist;
geroprotector;
serotonergic antagonist
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.		1.9910dibenzoazepineadrenergic uptake inhibitor;
alpha-adrenergic antagonist;
antidepressant;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
geroprotector;
H1-receptor antagonist;
histamine agonist;
sedative;
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.		1.9910(trifluoromethyl)benzenes;
N-arylpiperazine		environmental contaminant;
psychotropic drug;
serotonergic agonist;
xenobiotic
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.		1.9910N-alkylpiperazine;
N-arylpiperazine;
phthalimides		serotonergic antagonist
perphenazine
Perphenazine: An antipsychotic phenothiazine derivative with actions and uses similar to those of CHLORPROMAZINE.. perphenazine : A phenothiazine derivative in which the phenothiazine tricycle carries a chloro substituent at the 2-position and a 3-[4-(2-hydroxyethyl)piperazin-1-yl]propyl group at N-10.		1.9810N-(2-hydroxyethyl)piperazine;
N-alkylpiperazine;
organochlorine compound;
phenothiazines		antiemetic;
dopaminergic antagonist;
phenothiazine antipsychotic drug
quetiapine
[no description available]		1.9910dibenzothiazepine;
N-alkylpiperazine;
N-arylpiperazine		adrenergic antagonist;
dopaminergic antagonist;
histamine antagonist;
second generation antipsychotic;
serotonergic antagonist
risperidone
Risperidone: A selective blocker of DOPAMINE D2 RECEPTORS and SEROTONIN 5-HT2 RECEPTORS that acts as an atypical antipsychotic agent. It has been shown to improve both positive and negative symptoms in the treatment of SCHIZOPHRENIA.. risperidone : A member of the class of pyridopyrimidines that is 2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one carrying an additional 2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl group at position 2.		3.37701,2-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
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.		1.9910organofluorine compound;
piperidines;
thiazolopyrimidine		antidepressant;
antipsychotic agent;
anxiolytic drug;
dopaminergic antagonist;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
serotonergic antagonist
spiperone
Spiperone: A spiro butyrophenone analog similar to HALOPERIDOL and other related compounds. It has been recommended in the treatment of SCHIZOPHRENIA.. spiperone : An azaspiro compound that is 1,3,8-triazaspiro[4.5]decane which is substituted at positions 1, 4, and 8 by phenyl, oxo, and 4-(p-fluorophenyl)-4-oxobutyl groups, respectively.		3.0850aromatic ketone;
azaspiro compound;
organofluorine compound;
piperidines;
tertiary amino compound		alpha-adrenergic antagonist;
antipsychotic agent;
dopaminergic antagonist;
psychotropic drug;
serotonergic antagonist
spiroxatrine
spiroxatrine: structure		1.9910imidazolidines
sumatriptan
Sumatriptan: A serotonin agonist that acts selectively at 5HT1 receptors. It is used in the treatment of MIGRAINE DISORDERS.. sumatriptan : A sulfonamide that consists of N,N-dimethyltryptamine bearing an additional (N-methylsulfamoyl)methyl substituent at position 5. Selective agonist for a vascular 5-HT1 receptor subtype (probably a member of the 5-HT1D family). Used (in the form of its succinate salt) for the acute treatment of migraine with or without aura in adults.		1.9910sulfonamide;
tryptamines		serotonergic agonist;
vasoconstrictor agent
thioridazine
Thioridazine: A phenothiazine antipsychotic used in the management of PHYCOSES, including SCHIZOPHRENIA.. thioridazine : A phenothiazine derivative having a methylsulfanyl subsitituent at the 2-position and a (1-methylpiperidin-2-yl)ethyl] group at the N-10 position.		2.940phenothiazines;
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]		1.9910piperazines
zotepine
zotepine: structure		2.420dibenzothiepine;
tertiary amino compound		alpha-adrenergic drug;
second generation antipsychotic;
serotonergic drug
corticosterone
[no description available]		1.981011beta-hydroxy steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(4) steroid;
C21-steroid;
glucocorticoid;
primary alpha-hydroxy ketone		human metabolite;
mouse metabolite
physostigmine
Physostigmine: A cholinesterase inhibitor that is rapidly absorbed through membranes. It can be applied topically to the conjunctiva. It also can cross the blood-brain barrier and is used when central nervous system effects are desired, as in the treatment of severe anticholinergic toxicity.		1.9610carbamate ester;
indole alkaloid		antidote to curare poisoning;
EC 3.1.1.8 (cholinesterase) inhibitor;
miotic
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.		1.9610aporphine alkaloidalpha-adrenergic drug;
antidyskinesia agent;
antiparkinson drug;
dopamine agonist;
emetic;
serotonergic drug
n,n-dimethyltryptamine
N,N-Dimethyltryptamine: An N-methylated indoleamine derivative and serotonergic hallucinogen which occurs naturally and ubiquitously in several plant species including Psychotria veridis. It also occurs in trace amounts in mammalian brain, blood, and urine, and is known to act as an agonist or antagonist of certain SEROTONIN RECEPTORS.. N,N-dimethyltryptamine : A tryptamine derivative having two N-methyl substituents on the side-chain.		1.9910tryptamine alkaloid;
tryptamines
isoxazoles
Isoxazoles: Azoles with an OXYGEN and a NITROGEN next to each other at the 1,2 positions, in contrast to OXAZOLES that have nitrogens at the 1,3 positions.. isoxazole : A monocyclic heteroarene with a structure consisting of a 5-membered ring containing three carbon atoms and an oxygen and nitrogen atom adjacent to each other. It is the parent of the class of isoxazoles.. isoxazoles : Oxazoles in which the N and O atoms are adjacent.		2.3820isoxazoles;
mancude organic heteromonocyclic parent;
monocyclic heteroarene
oxazoles
Oxazoles: Five-membered heterocyclic ring structures containing an oxygen in the 1-position and a nitrogen in the 3-position, in distinction from ISOXAZOLES where they are at the 1,2 positions.. 1,3-oxazole : A five-membered monocyclic heteroarene that is an analogue of cyclopentadiene with O in place of CH2 at position 1 and N in place of CH at position 3.. oxazole : An azole based on a five-membered heterocyclic aromatic skeleton containing one N and one O atom.		1.96101,3-oxazoles;
mancude organic heteromonocyclic parent;
monocyclic heteroarene
thiazoles
[no description available]		2.38201,3-thiazoles;
mancude organic heteromonocyclic parent;
monocyclic heteroarene
methysergide
Methysergide: An ergot derivative that is a congener of LYSERGIC ACID DIETHYLAMIDE. It antagonizes the effects of serotonin in blood vessels and gastrointestinal smooth muscle, but has few of the properties of other ergot alkaloids. Methysergide is used prophylactically in migraine and other vascular headaches and to antagonize serotonin in the carcinoid syndrome.. methysergide : A synthetic ergot alkaloid, structurally related to the oxytocic agent methylergonovine and to the potent hallucinogen LSD and used prophylactically to reduce the frequency and intensity of severe vascular headaches.		1.9910ergoline alkaloid
metylperon
metylperon: RN given refers to parent cpd		1.9710aromatic ketone
pimozide
Pimozide: A diphenylbutylpiperidine that is effective as an antipsychotic agent and as an alternative to HALOPERIDOL for the suppression of vocal and motor tics in patients with Tourette syndrome. Although the precise mechanism of action is unknown, blockade of postsynaptic dopamine receptors has been postulated. (From AMA Drug Evaluations Annual, 1994, p403). pimozide : A member of the class of benzimidazoles that is 1,3-dihydro-2H-benzimidazol-2-one in which one of the nitrogens is substituted by a piperidin-4-yl group, which in turn is substituted on the nitrogen by a 4,4-bis(p-fluorophenyl)butyl group.		2.3920benzimidazoles;
heteroarylpiperidine;
organofluorine compound		antidyskinesia agent;
dopaminergic antagonist;
first generation antipsychotic;
H1-receptor antagonist;
serotonergic antagonist
flupenthixol
Flupenthixol: A thioxanthene neuroleptic that, unlike CHLORPROMAZINE, is claimed to have CNS-activating properties. It is used in the treatment of psychoses although not in excited or manic patients. (From Martindale, The Extra Pharmacopoeia, 30th ed, p595). flupenthixol : A thioxanthene derivative having a trifluoromethyl substituent at the 2-position and a 3-(4-(2-hydroxyethyl)piperazin-1-yl)propylidene group at the 10-position with undefined double bond stereochemistry.		1.9710thioxanthenes
metergoline
Metergoline: A dopamine agonist and serotonin antagonist. It has been used similarly to BROMOCRIPTINE as a dopamine agonist and also for MIGRAINE DISORDERS therapy.. metergoline : An ergoline alkaloid that is the N-benzyloxycarbonyl derivative of lysergamine. A 5-HT2 antagonist. Also 5-HT1 antagonist and 5-HT1D ligand. Has moderate affinity for 5-HT6 and high affinity for 5-HT7.		1.9910carbamate ester;
ergoline alkaloid		dopamine agonist;
geroprotector;
serotonergic antagonist
bromocriptine
Bromocriptine: A semisynthetic ergotamine alkaloid that is a dopamine D2 agonist. It suppresses prolactin secretion.		1.9910indole alkaloidantidyskinesia agent;
antiparkinson drug;
dopamine agonist;
hormone antagonist
butaclamol
(+)-butaclamol : An organic heteropentacyclic compound that is 2,3,4,4a,8,9,13b,14-octahydro-1H-benzo[6,7]cyclohepta[1,2,3-de]pyrido[2,1-a]isoquinoline substituted at position 3 by both hydroxy and tert-butyl groups.		1.9910organic heteropentacyclic compound
fluperlapine
fluperlapine: structure given in first source		2.6730benzazepine
rimcazole
rimcazole: RN given refers to (cis)-isomer; structure given in first source		3.0710carbazoles
remoxipride
Remoxipride: An antipsychotic agent that is specific for dopamine D2 receptors. It has been shown to be effective in the treatment of schizophrenia.		3.4820dimethoxybenzene
ipsapirone
[no description available]		1.9910N-arylpiperazine
flesinoxan
[no description available]		1.9910
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.		2.420heteroarylpiperidine;
imidazolidinone;
organochlorine compound;
organofluorine compound;
phenylindole		alpha-adrenergic antagonist;
H1-receptor antagonist;
second generation antipsychotic;
serotonergic antagonist
ziprasidone
ziprasidone: a benzisothiazoylpiperazine derivative; has combined dopamine and serotonin receptor antagonist activity; structurally related to tiospirone. ziprasidone : A piperazine compound having 1,2-benzothiazol-3-yl- and 2-(6-chloro-1,3-dihydro-2-oxindol-5-yl)ethyl substituents attached to the nitrogen atoms.		2.69301,2-benzisothiazole;
indolones;
organochlorine compound;
piperazines		antipsychotic agent;
dopaminergic antagonist;
histamine antagonist;
muscarinic antagonist;
psychotropic drug;
serotonergic antagonist
setoperone
[no description available]		1.9710
mesulergine
mesulergine: RN given refers to parent cpd; CU 32-085 is synonymous to mono-HCl; metabolized into dopaminergic agonists; structure given in first source. mesulergine : A member of the class of ergot alkaloids that is known to act on serotonin and dopamine receptors.		1.9910ergot alkaloid;
sulfamides		antiparkinson drug;
dopamine agonist;
serotonergic antagonist
tandospirone
tandospirone: structure given in first source. tandospirone : A dicarboximide that is (3aR,4S,7R,7aS)-hexahydro-1H-4,7-methanoisoindole-1,3(2H)-dione which is substituted by a 4-[4-(pyrimidin-2-yl)piperazin-1-yl]butyl group at position 2. It is a potent and selective 5-HT1A receptor partial agonist (Ki = 27 nM).		1.9910bridged 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]		2.420indoles
alpha-(4-fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazine butanol
alpha-(4-fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazine butanol: NM refers to free form; BMY 14802-1 is the HCl; structure given in first source		3.7730N-arylpiperazine
perospirone
perospirone: structure given in first source		1.9810N-arylpiperazine
1-(2-(4-aminophenyl)ethyl)-4-(3-trifluoromethylphenyl)piperazine
LY 165163: structure given in first source; a serotonin agonist. LY-165163 : A N-arylpiperazine that is piperazine substituted by 2-(4-aminophenyl)ethyl and 3-(trifluoromethyl)phenyl groups at positions 1 and 4, respectively. It is a selective 5-HT1A serotonin receptor agonist and 5-HT1D serotonin receptor antagonist.		1.9910(trifluoromethyl)benzenes;
N-alkylpiperazine;
N-arylpiperazine;
primary arylamine;
substituted aniline		geroprotector;
serotonergic agonist
uh 301
UH 301: structure given in first source		1.9910
ici 169369
2-((2-(dimethylamino)ethyl)thio)-3-phenylquinoline: structure & RN given in first source		1.9910
fg 5893
FG 5893: a mixed serotonin agonist & antagonist; attenuates alcohol drinking in rats		1.9910
s 14671
S 14671: serotonin receptor agonist; RN from toxlit		1.9910
asenapine
asenapine : A racemate consisting of equal amounts of (R,R)- and (S,S)-asenapine. Used as its maleate salt for the acute treatment of schizophrenia and acute treatment of manic or mixed episodes associated with bipolar I disorder with or without psychotic features.. (S,S)-asenapine : A 5-chloro-2-methyl-2,3,3a,12b-tetrahydrodibenzo[2,3:6,7]oxepino[4,5-c]pyrrole in which both of the stereocentres have S configuration.		1.99105-chloro-2-methyl-2,3,3a,12b-tetrahydrodibenzo[2,3:6,7]oxepino[4,5-c]pyrrole
zalospirone
zalospirone: a partial 5-HT1A receptor agonist; RN given refers to (3aalpha,4alpha,4abeta,6abeta,7alpha,7aalpha)-isomer; RN for cpd without isomeric designation not available 4/91		1.9910
cocaine
Cocaine: An alkaloid ester extracted from the leaves of plants including coca. It is a local anesthetic and vasoconstrictor and is clinically used for that purpose, particularly in the eye, ear, nose, and throat. It also has powerful central nervous system effects similar to the amphetamines and is a drug of abuse. Cocaine, like amphetamines, acts by multiple mechanisms on brain catecholaminergic neurons; the mechanism of its reinforcing effects is thought to involve inhibition of dopamine uptake.. cocaine : A tropane alkaloid obtained from leaves of the South American shrub Erythroxylon coca.		710benzoate ester;
methyl ester;
tertiary amino compound;
tropane alkaloid		adrenergic uptake inhibitor;
central nervous system stimulant;
dopamine uptake inhibitor;
environmental contaminant;
local anaesthetic;
mouse metabolite;
plant metabolite;
serotonin uptake inhibitor;
sodium channel blocker;
sympathomimetic agent;
vasoconstrictor agent;
xenobiotic
raclopride
Raclopride: A substituted benzamide that has antipsychotic properties. It is a dopamine D2 receptor (see RECEPTORS, DOPAMINE D2) antagonist.		1.9910salicylamides
nafadotride
nafadotride: structure given in first source. nafadotride : A naphthalenecarboxamide resulting from the formal condensation of the carboxylic acid group of 4-cyano-1-methoxynaphthalene-2-carboxylic acid with the primary amino group of 1-(1-butylpyrrolidin-2-yl]methanamine. It is a highly potent, competitive, preferential dopamine D3 receptor antagonist, centrally active upon systemic administration.		1.9910aromatic ether;
naphthalenecarboxamide;
nitrile;
pyrrolidines;
tertiary amino compound		dopaminergic antagonist
piperidines
Piperidines: A family of hexahydropyridines.		1.9810
clozapine
Clozapine: A tricylic dibenzodiazepine, classified as an atypical antipsychotic agent. It binds several types of central nervous system receptors, and displays a unique pharmacological profile. Clozapine is a serotonin antagonist, with strong binding to 5-HT 2A/2C receptor subtype. It also displays strong affinity to several dopaminergic receptors, but shows only weak antagonism at the dopamine D2 receptor, a receptor commonly thought to modulate neuroleptic activity. Agranulocytosis is a major adverse effect associated with administration of this agent.. clozapine : A benzodiazepine that is 5H-dibenzo[b,e][1,4]diazepine substituted by a chloro group at position 8 and a 4-methylpiperazin-1-yl group at position 11. It is a second generation antipsychotic used in the treatment of psychiatric disorders like schizophrenia.		3.4980benzodiazepine;
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
Olanzapine: A benzodiazepine derivative that binds SEROTONIN RECEPTORS; MUSCARINIC RECEPTORS; HISTAMINE H1 RECEPTORS; ADRENERGIC ALPHA-1 RECEPTORS; and DOPAMINE RECEPTORS. It is an antipsychotic agent used in the treatment of SCHIZOPHRENIA; BIPOLAR DISORDER; and MAJOR DEPRESSIVE DISORDER; it may also reduce nausea and vomiting in patients undergoing chemotherapy.. olanzapine : A benzodiazepine that is 10H-thieno[2,3-b][1,5]benzodiazepine substituted by a methyl group at position 2 and a 4-methylpiperazin-1-yl group at position 4.		2.9140benzodiazepine;
N-arylpiperazine;
N-methylpiperazine		antiemetic;
dopaminergic antagonist;
histamine antagonist;
muscarinic antagonist;
second generation antipsychotic;
serotonergic antagonist;
serotonin uptake inhibitor
pyrimidinones
Pyrimidinones: Heterocyclic compounds known as 2-pyrimidones (or 2-hydroxypyrimidines) and 4-pyrimidones (or 4-hydroxypyrimidines) with the general formula C4H4N2O.		1.9710
ConditionIndicatedRelationship StrengthStudiesTrials
Anochlesia
[description not available]		02.8940
Alcohol Drinking
Behaviors associated with the ingesting of ALCOHOLIC BEVERAGES, including social drinking.		0210
Dementia Praecox
[description not available]		05.5232
Schizophrenia
A severe emotional disorder of psychotic depth characteristically marked by a retreat from reality with delusion formation, HALLUCINATIONS, emotional disharmony, and regressive behavior.		05.5232
Dyskinesia, Medication-Induced
[description not available]		01.9610
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)		01.9610
Hypotension, Postural
[description not available]		03.3511
Hypotension, Orthostatic
A significant drop in BLOOD PRESSURE after assuming a standing position. Orthostatic hypotension is a finding, and defined as a 20-mm Hg decrease in systolic pressure or a 10-mm Hg decrease in diastolic pressure 3 minutes after the person has risen from supine to standing. Symptoms generally include DIZZINESS, blurred vision, and SYNCOPE.		03.3511
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