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 |
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https://pubchem.ncbi.nlm.nih.gov/compound/21862004 https://pharmaceutical-substances.thieme.com/ps/search-results%3FdocUri=KD-16-0056 |
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D01438 (en) |
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CN1CCNC2=NC3=CC=CC=C3CC4=CC=CC=C42 (en) |
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PWRPUAKXMQAFCJ-UHFFFAOYSA-N (en) |
dbp:synonyms |
AW-14233; HF-2333; MP-11; PLP 100-127; 6-morphanthridine (en) |
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dbr:Pharmacodynamics |
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background:#ccccff (en) |
dbp:tradename |
Hypnodine, Pipnodine (en) |
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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 . (en) |
rdfs:label |
Perlapine (en) |
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wikidata:Perlapine dbpedia-fa:Perlapine https://global.dbpedia.org/id/2YYQG |
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wikipedia-en:Perlapine?oldid=1120352117&ns=0 |
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