Perlapine (original) (raw)

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Perlapine, sold under the brand names Hypnodine and Pipnodine, is a hypnotic and sedative of the tricyclic group which is marketed in Japan. It acts primarily as a potent antihistamine, and also has anticholinergic, antiserotonergic, antiadrenergic, and some antidopaminergic activity. The drug has relatively weak affinity for the dopamine D2 receptor (IC50 = 1,803 nM) and, in accordance, is said to be ineffective as an antipsychotic. However, it retains higher affinity for the dopamine D1 receptor (IC50 = 198 nM). Its IC50 values are 19 nM for the α1-adrenergic receptor, 4,945 nM for the α2-adrenergic receptor, and 70 nM for the serotonin 5-HT2A receptor. Perlapine is closely related to clotiapine, clozapine, fluperlapine, loxapine, and .

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dbo:abstract Perlapine, sold under the brand names Hypnodine and Pipnodine, is a hypnotic and sedative of the tricyclic group which is marketed in Japan. It acts primarily as a potent antihistamine, and also has anticholinergic, antiserotonergic, antiadrenergic, and some antidopaminergic activity. The drug has relatively weak affinity for the dopamine D2 receptor (IC50 = 1,803 nM) and, in accordance, is said to be ineffective as an antipsychotic. However, it retains higher affinity for the dopamine D1 receptor (IC50 = 198 nM). Its IC50 values are 19 nM for the α1-adrenergic receptor, 4,945 nM for the α2-adrenergic receptor, and 70 nM for the serotonin 5-HT2A receptor. Perlapine is closely related to clotiapine, clozapine, fluperlapine, loxapine, and . Perlapine has been suggested as a potential ligand for certain DREADDs. (en)
dbo:alternativeName Hypnodine, Pipnodine (en)
dbo:casNumber 1977-11-3
dbo:chEBI 31983
dbo:chEMBL 340801
dbo:fdaUniiCode 4N8UJJ27IM
dbo:kegg D01438
dbo:pubchem 16106
dbo:thumbnail wiki-commons:Special:FilePath/Perlapine.svg?width=300
dbo:wikiPageExternalLink https://pubchem.ncbi.nlm.nih.gov/compound/21862004 https://pharmaceutical-substances.thieme.com/ps/search-results%3FdocUri=KD-16-0056
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dbo:wikiPageRevisionID 1120352117 (xsd:integer)
dbo:wikiPageWikiLink dbr:Potency_(pharmacology) dbc:Piperazines dbr:Clotiapine dbr:Clozapine dbr:Epinastine dbr:Anticholinergic dbr:Antihistamine dbr:Antipsychotic dbr:Loxapine dbc:Dibenzodiazepines dbr:Pharmacodynamics dbr:5-HT2A_receptor dbc:5-HT2A_antagonists dbc:H1_receptor_antagonists dbc:Muscarinic_antagonists dbr:Alpha-1_adrenergic_receptor dbr:Alpha-2_adrenergic_receptor dbr:Fluperlapine dbc:Serotonin_receptor_antagonists dbr:Japan dbr:Hypnotic dbc:Dopamine_antagonists dbc:Alpha-1_blockers dbr:Affinity_(pharmacology) dbr:Dopamine dbr:Antiserotonergic dbr:D1_receptor dbr:D2_receptor dbr:DREADD dbr:Sedative dbr:Serotonin dbr:Tricyclic_compound dbr:Antiadrenergic dbr:Antidopaminergic dbr:File:Perlapine_synthesis.svg dbr:Tilozepine
dbp:c 19 (xsd:integer)
dbp:casNumber 1977-11-03 (xsd:date)
dbp:chebi 31983 (xsd:integer)
dbp:chembl 340801 (xsd:integer)
dbp:chemspiderid 15291 (xsd:integer)
dbp:h 21 (xsd:integer)
dbp:iupacName 6 (xsd:integer)
dbp:kegg D01438 (en)
dbp:n 3 (xsd:integer)
dbp:pubchem 16106 (xsd:integer)
dbp:smiles CN1CCNC2=NC3=CC=CC=C3CC4=CC=CC=C42 (en)
dbp:stdinchi 1 (xsd:integer)
dbp:stdinchikey PWRPUAKXMQAFCJ-UHFFFAOYSA-N (en)
dbp:synonyms AW-14233; HF-2333; MP-11; PLP 100-127; 6-morphanthridine (en)
dbp:title dbr:Pharmacodynamics
dbp:titlestyle background:#ccccff (en)
dbp:tradename Hypnodine, Pipnodine (en)
dbp:unii 4 (xsd:integer)
dbp:wikiPageUsesTemplate dbt:Tricyclics dbt:Abbr dbt:Adrenergic_receptor_modulators dbt:Drugbox dbt:Navboxes dbt:Reflist dbt:Sedatives dbt:Serotonin_receptor_modulators dbt:Short_description dbt:Abbrlink dbt:Dopamine_receptor_modulators dbt:Histamine_receptor_modulators dbt:Muscarinic_acetylcholine_receptor_modulators dbt:Sedative-stub dbt:Antihistamines
dcterms:subject dbc:Piperazines dbc:Dibenzodiazepines dbc:5-HT2A_antagonists dbc:H1_receptor_antagonists dbc:Muscarinic_antagonists dbc:Serotonin_receptor_antagonists dbc:Dopamine_antagonists dbc:Alpha-1_blockers
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rdfs:comment Perlapine, sold under the brand names Hypnodine and Pipnodine, is a hypnotic and sedative of the tricyclic group which is marketed in Japan. It acts primarily as a potent antihistamine, and also has anticholinergic, antiserotonergic, antiadrenergic, and some antidopaminergic activity. The drug has relatively weak affinity for the dopamine D2 receptor (IC50 = 1,803 nM) and, in accordance, is said to be ineffective as an antipsychotic. However, it retains higher affinity for the dopamine D1 receptor (IC50 = 198 nM). Its IC50 values are 19 nM for the α1-adrenergic receptor, 4,945 nM for the α2-adrenergic receptor, and 70 nM for the serotonin 5-HT2A receptor. Perlapine is closely related to clotiapine, clozapine, fluperlapine, loxapine, and . (en)
rdfs:label Perlapine (en)
owl:sameAs wikidata:Perlapine dbpedia-fa:Perlapine https://global.dbpedia.org/id/2YYQG
prov:wasDerivedFrom wikipedia-en:Perlapine?oldid=1120352117&ns=0
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foaf:isPrimaryTopicOf wikipedia-en:Perlapine
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is foaf:primaryTopic of wikipedia-en:Perlapine