| 词条 | Perlapine |
| 释义 |
| Verifiedfields = | Watchedfields = | verifiedrevid = | IUPAC_name = 6-(4-Methylpiperazin-1-yl)-11H-benzo[c][1]benzazepine | image = Perlapine.svg | width = | tradename = Hypnodine, Pipnodine | pregnancy_AU = | pregnancy_US = | pregnancy_category = | legal_AU = | legal_CA = | legal_UK = | legal_US = | legal_status = | routes_of_administration = | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion = | CAS_number_Ref = | CAS_number = 1977-11-3 | CAS_supplemental = | class = | ATC_prefix = | ATC_suffix = | ATC_supplemental = | PubChem = 16106 | IUPHAR_ligand = | DrugBank_Ref = | DrugBank = | ChemSpiderID_Ref = | ChemSpiderID = 15291 | UNII = 4N8UJJ27IM | KEGG = D01438 | ChEBI = 31983 | ChEMBL = 340801 | synonyms = AW-14233; HF-2333; MP-11; PLP 100-127; 6-(4-Methyl-1-piperazinyl)morphanthridine | C=19 | H=21 | N=3 | molecular_weight = 291.398 g/mol | SMILES = CN1CCN(CC1)C2=NC3=CC=CC=C3CC4=CC=CC=C42 | StdInChI_Ref = | StdInChI = 1S/C19H21N3/c1-21-10-12-22(13-11-21)19-17-8-4-2-6-15(17)14-16-7-3-5-9-18(16)20-19/h2-9H,10-14H2,1H3 | StdInChIKey_Ref = | StdInChIKey = PWRPUAKXMQAFCJ-UHFFFAOYSA-N }}Perlapine, sold under the brand names Hypnodine and Pipnodine, is a hypnotic and sedative of the tricyclic group which is marketed in Japan.[1] It acts primarily as a potent antihistamine,[2] and also has anticholinergic,[2] antiserotonergic,[3] antiadrenergic, and some antidopaminergic activity.[3][4][5][6] The drug has relatively weak affinity for the dopamine D2 receptor ({{abbrlink|IC50|Half-maximal inhibitory concentration}} = 1,803 nM) and, in accordance, is said to be ineffective as an antipsychotic.[6][7] However, it retains higher affinity for the dopamine D1 receptor ({{abbr|IC50|Half-maximal inhibitory concentration}} = 198 nM).[6] Its {{abbr|IC50|Half-maximal inhibitory concentration}} values are 19 nM for the α1-adrenergic receptor, 4,945 nM for the α2-adrenergic recpetor, and 70 nM for the serotonin 5-HT2A receptor.[6] Perlapine is closely related to clotiapine, clozapine, fluperlapine, loxapine, and tilozepine.[6] References1. ^{{cite book|title=Index Nominum 2000: International Drug Directory|url=https://books.google.com/books?id=5GpcTQD_L2oC&pg=PA811|year=2000|publisher=Taylor & Francis|isbn=978-3-88763-075-1|pages=811–}} {{Antihistamines}}{{Sedatives}}{{Navboxes2. ^1 {{cite book|author=Abel Lajtha|title=Alterations of Metabolites in the Nervous System|url=https://books.google.com/books?id=dYnSBwAAQBAJ&pg=PA352|date=11 November 2013|publisher=Springer Science & Business Media|isbn=978-1-4757-6740-7|pages=352–}} 3. ^1 {{cite book|title=Progress in Medicinal Chemistry|url=https://books.google.com/books?id=SDaZ4qcemf8C&pg=PA226|date=24 April 1996|publisher=Elsevier|isbn=978-0-08-086281-1|pages=226–}} 4. ^{{cite book|author=D E Hathway|title=Foreign Compound Metabolism in Mammals|url=https://books.google.com/books?id=UHAoDwAAQBAJ&pg=PA302|date=31 October 2007|publisher=Royal Society of Chemistry|isbn=978-1-84755-608-0|pages=302–}} 5. ^{{cite book|author=Bentham Science Publishers|title=Current Medicinal Chemistry|url=https://books.google.com/books?id=eMw2LsjQ5PQC&pg=PA489|date=April 1995|publisher=Bentham Science Publishers|pages=489–}} 6. ^1 2 3 4 {{cite book|author=Thomas R.E. Barnes|title=Antipsychotic Drugs and Their Side-Effects|url=https://books.google.com/books?id=IT2OAgAAQBAJ&pg=PA34|date=22 October 2013|publisher=Elsevier Science|isbn=978-1-4832-8810-9|pages=28,34}} 7. ^{{cite book|author=American College of Neuropsychopharmacology|title=Psychopharmacology: a generation of progress|url=https://books.google.com/books?id=c-RsAAAAMAAJ|year=1978|publisher=Raven Press|isbn=978-0-89004-191-8|page=514}} | title = Pharmacodynamics | titlestyle = background:#ccccff | list1 ={{Adrenergic receptor modulators}}{{Dopamine receptor modulators}}{{Histamine receptor modulators}}{{Muscarinic acetylcholine receptor modulators}}{{Serotonin receptor modulators}} }}{{Tricyclics}}{{sedative-stub}} 7 : Alpha-1 blockers|Dibenzodiazepines|Dopamine antagonists|H1 receptor antagonists|Muscarinic antagonists|Piperazines|Serotonin antagonists |
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