Compounds > lr 511
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lr 511

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Description

LR 511: structure [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID68696
CHEMBL ID72400
SCHEMBL ID2109741
MeSH IDM0064991

Synonyms (23)

Synonym
zoloperone
zoloperona [inn-spanish]
4-(p-fluorophenyl)-5-(2-(4-(o-methoxyphenyl)-1-piperazinyl)ethyl)-4-oxazolin-2-one
2(3h)-oxazolone, 4-(4-fluorophenyl)-5-(2-(4-(2-methoxyphenyl)-1-piperazinyl)ethyl)-
brn 1182380
4-(4-fluorophenyl)-5-(2-(4-(2-methoxyphenyl)-1-piperazinyl)ethyl)-2(3h)-oxazolone
lr 511
zoloperone [inn]
zoloperonum [inn-latin]
lr-511
52867-74-0
CHEMBL72400
4-(4-fluorophenyl)-5-[2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl]-3h-1,3-oxazol-2-one
4-4-fluorophenyl-5-n-(n'-o-methoxyphenyl)piperazinoethyl-4-oxazolin-2-one
unii-3yu9tet43b
zoloperonum
3yu9tet43b ,
zoloperona
SCHEMBL2109741
DTXSID80200889
bdbm50227900
Q27258220
AKOS040754577
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (48)

Assay IDTitleYearJournalArticle
AID128816Antagonistic activity against amphetamine-induced hypermotility, after 1 hour of peroral administration in mouse1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID177739Activity to evoke catalepsy in rats, by administering perorally1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID131419Potentiation against pentobarbital-induced sleeping, after 1 hour of peroral administration in mouse1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID178997Inhibitory activity against norepinephrine-induced lethality, after 1 hour of peroral administration in rat1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID131205Contractile activity in skeletal muscles, after 1 hour of peroral administration in mouse at dose of 0 mg/kg1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID131206Contractile activity in skeletal muscles, after 5 hour of peroral administration in mouse1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID63327Antagonistic activity against apomorphine-induced emesis, after 5 hour of peroral administration in dogs1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID130871Inhibition against apomorphine-induced climbing, after 1 hour of peroral administration in mouse1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID128815Antagonistic activity against amphetamine-induced Hypermobility in mouse by administering perorally1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID128986Anticonvulsant activity against tryptamine-induced convulsions, after 1 hour of peroral administration in mouse1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID177732Inhibition against conditioned avoidance response, after 5 hour of peroral administration in rats1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID178998Inhibitory activity against norepinephrine-induced lethality, after 5 hour of peroral administration in rat1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID177946Antagonistic activity against amphetamine-induced stereotypy, after 1 hour of peroral administration in rats1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID130876Inhibition against apomorphine-induced turning, after 5 hour of peroral administration in mouse1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID130875Inhibition against apomorphine-induced turning, after 1 hr of peroral administration in mouse1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID133842Anticonvulsant activity against electroshock-induced convulsions, after 5 hour of peroral administration in mouse at dose of 100 mg/kg1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID133862Anticonvulsant activity against tryptamine-induced convulsions, after 5 hour of peroral administration in mouse at dose of 40 mg/kg1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID62726Binding affinity against rat striatal membranes using [3H]spiroperidol as the radioligand, after 15 min of incubation in vitro at 37 degree C1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID134580Lethal dose in mice (LD50) following i.p. dosing1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID177741Activity to evoke catalepsy, after 1 hour of peroral administration in rats1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID131365Effect on skeletal muscle tone, after 5 hour of peroral administration in mouse1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID131420Potentiation against pentobarbital-induced sleeping, after 5 hour of peroral administration in mouse1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID128817Antagonistic activity against amphetamine-induced hypermotility, after 5 hour of peroral administration in mouse1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID133851Anticonvulsant activity against pentylenetetrazole-induced convulsions, after 5 hour of peroral administration in mouse at dose of 100 mg/kg1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID177950Antagonistic activity against apomorphine-induced stereotypy, after 1 hour of peroral administration in rats1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID130872Inhibition against apomorphine-induced climbing, after 5 hour of peroral administration in mouse1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID135367Inhibitory activity against tremorine-induced tremors, after 1 hour of peroral administration in mouse at dose of 60 mg/kg1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID133682Activity of inclined screen in mouse, after 5 hour of peroral administration in mouse at dose of 100 mg/kg1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID131046Inhibition of spontaneous motor activity, after 5 hour of peroral administration in mouse1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID131045Inhibition of spontaneous motor activity, after 1 hour of peroral administration in mouse1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID177952Antagonistic activity against apomorphine-induced stereotypy in rats, by administering perorally1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID128162Activity of inclined screen in mouse, after 1 hour of peroral administration in mouse1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID177947Antagonistic activity against amphetamine-induced stereotypy, after 5 hour of peroral administration in rats1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID130911Inhibition of spontaneous motor activity in mouse, by administering perorally1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID134521Effect on skeletal muscle tone, after 1 hour of peroral administration in mouse at dose of 200 mg/kg1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID63326Antagonistic activity against apomorphine-induced emesis, after 1 hr of peroral administration in dogs1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID135363Inhibitory activity against tremorine-induced salivation, after 5 hour of peroral administration in mouse at dose of 60 mg/kg1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID177951Antagonistic activity against apomorphine-induced stereotypy, after 5 hour of peroral administration in rats1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID135370Inhibitory activity against tremorine-induced tremors, after 5 hour of peroral administration in mouse at dose of 60 mg/kg1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID135223Inhibitory activity against tremorine-induced salivation, after 1 hour of peroral administration in mouse at dose of 60 mg/kg1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID177742Activity to evoke catalepsy, after 5 hour of peroral administration in rats1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID131588Suppression of aggressive behavior, after 1 hour of peroral administration in mouse1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID133840Anticonvulsant activity against electroshock-induced convulsions, after 1 hour of peroral administration in mouse at dose of 100 mg/kg1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID176328Body weight gain, after 5 hour of peroral administration in rats1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID176327Body weight gain, after 2 hour period of conditioned feeding in rats1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID133849Anticonvulsant activity against pentylenetetrazole-induced convulsions, after 1 hour of peroral administration in mouse at dose of 100 mg/kg1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID177731Inhibition against conditioned avoidance response, after 1 hour of peroral administration in rats1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID131589Suppression of aggressive behavior, after 5 hour of peroral administration in mouse1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (6)

TimeframeStudies, This Drug (%)All Drugs %
pre-19906 (100.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)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: 32.29

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 Index32.29 (24.57)
Research Supply Index1.95 (2.92)
Research Growth Index4.45 (4.65)
Search Engine Demand Index70.29 (26.88)
Search Engine Supply Index3.80 (0.95)

This Compound (32.29)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other6 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
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.		2.3720organochlorine compound;
phenothiazines;
tertiary amine		anticoronaviral agent;
antiemetic;
dopaminergic antagonist;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
phenothiazine antipsychotic drug
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.		1.9510primary 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.		1.95101,4-benzodiazepinone;
organochlorine compound		anticonvulsant;
anxiolytic drug;
environmental contaminant;
sedative;
xenobiotic
diphenhydramine
Diphenhydramine: A histamine H1 antagonist used as an antiemetic, antitussive, for dermatoses and pruritus, for hypersensitivity reactions, as a hypnotic, an antiparkinson, and as an ingredient in common cold preparations. It has some undesired antimuscarinic and sedative effects.. diphenhydramine : An ether that is the benzhydryl ether of 2-(dimethylamino)ethanol. It is a H1-receptor antagonist used as a antipruritic and antitussive drug.. antitussive : An agent that suppresses cough. Antitussives have a central or a peripheral action on the cough reflex, or a combination of both. Compare with expectorants, which are considered to increase the volume of secretions in the respiratory tract, so facilitating their removal by ciliary action and coughing, and mucolytics, which decrease the viscosity of mucus, facilitating its removal by ciliary action and expectoration.		1.9510ether;
tertiary amino compound		anti-allergic agent;
antidyskinesia agent;
antiemetic;
antiparkinson drug;
antipruritic drug;
antitussive;
H1-receptor antagonist;
local anaesthetic;
muscarinic antagonist;
oneirogen;
sedative
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.		2.8740aromatic ketone;
hydroxypiperidine;
monochlorobenzenes;
organofluorine compound;
tertiary alcohol		antidyskinesia agent;
antiemetic;
dopaminergic antagonist;
first generation antipsychotic;
serotonergic antagonist
muscimol
Muscimol: A neurotoxic isoxazole isolated from species of AMANITA. It is obtained by decarboxylation of IBOTENIC ACID. Muscimol is a potent agonist of GABA-A RECEPTORS and is used mainly as an experimental tool in animal and tissue studies.. muscimol : A member of the class of isoxazoles that is 1,2-oxazol-3(2H)-one substituted by an aminomethyl group at position 5. It has been isolated from mushrooms of the genus Amanita.		1.9510alkaloid;
isoxazoles;
primary amino compound		fungal metabolite;
GABA agonist;
oneirogen;
psychotropic drug
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.		2.3620aporphine alkaloidalpha-adrenergic drug;
antidyskinesia agent;
antiparkinson drug;
dopamine agonist;
emetic;
serotonergic drug
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.		3.05501,3-oxazoles;
mancude organic heteromonocyclic parent;
monocyclic heteroarene
fluanisone
fluanisone: former provisional as haloanisone; structure; RN given refers to parent cpd		1.9710aromatic ketone
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.		1.9510carbamate ester;
ergoline alkaloid		dopamine agonist;
geroprotector;
serotonergic antagonist
2-phenyloxazolone
2-phenyloxazolone: RN given refers to 2-phenyl-5-oxazolone. 2-phenyloxazol-5(4H)-one : A 1,3-oxazole having a phenyl substituent at the 2-position and an oxo group at the 5-position. Note that phenyloxazolone is commonly used as a synonym for 4-(ethoxymethylene)-2-phenyloxazol-5-one (PhOx).		1.96101,3-oxazoles
oxazolone
Oxazolone: Immunologic adjuvant and sensitizing agent.		1.9610
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.		2.3720benzodiazepine;
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
ConditionIndicatedRelationship StrengthStudiesTrials
Anochlesia
[description not available]		02.3620
Contact Dermatitis
[description not available]		01.9610
Delayed Hypersensitivity
[description not available]		01.9610
Dermatitis, Contact
A type of acute or chronic skin reaction in which sensitivity is manifested by reactivity to materials or substances coming in contact with the skin. It may involve allergic or non-allergic mechanisms.		01.9610
Aggression
Behavior which may be manifested by destructive and attacking action which is verbal or physical, by covert attitudes of hostility or by obstructionism.		01.9510
Muscle Contraction
A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments.		01.9510