Chemistry:Perlapine

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Short description: Sedative and hypnotic medication
Perlapine
Perlapine.svg
Clinical data
Trade namesHypnodine, Pipnodine
Other namesAW-14233; HF-2333; MP-11; PLP 100-127; 6-(4-Methyl-1-piperazinyl)morphanthridine
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
Chemical and physical data
FormulaC19H21N3
Molar mass291.398 g·mol−1
3D model (JSmol)

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 (IC50 = 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 (IC50 = 198 nM).[6] 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.[6] Perlapine is closely related to clotiapine, clozapine, fluperlapine, loxapine, and tilozepine.[6]

Perlapine has been suggested as a potential ligand for certain DREADDs.[8][9]

References

  1. ↑ Index Nominum 2000: International Drug Directory. Taylor & Francis. 2000. pp. 811–. ISBN 978-3-88763-075-1. https://books.google.com/books?id=5GpcTQD_L2oC&pg=PA811. 
  2. ↑ 2.0 2.1 "Neuroleptics". Alterations of Metabolites in the Nervous System. Boston, MA.: Springer Science & Business Media. 1985. pp. 331–361. ISBN 978-1-4757-6740-7. https://books.google.com/books?id=dYnSBwAAQBAJ&pg=PA352. 
  3. ↑ 3.0 3.1 "Risperidone and related 5HT2/D2 antagonists: a new type of antipsychotic agent?". Progress in Medicinal Chemistry 33: 185–232. 1996. doi:10.1016/s0079-6468(08)70306-0. ISBN 9780444823106. PMID 8776944. 
  4. ↑ Foreign Compound Metabolism in Mammals. Royal Society of Chemistry. 31 October 2007. pp. 302–. ISBN 978-1-84755-608-0. https://books.google.com/books?id=UHAoDwAAQBAJ&pg=PA302. 
  5. ↑ "Diarylazepine derivatives as potent atypical neuroleptic drugs: recent advances.". Current Medicinal Chemistry (Bentham Science Publishers) 1 (6): 471–501. April 1995. doi:10.2174/092986730106220216114910. https://books.google.com/books?id=eMw2LsjQ5PQC&pg=PA489. 
  6. ↑ 6.0 6.1 6.2 6.3 6.4 Antipsychotic Drugs and Their Side-Effects. Elsevier Science. 22 October 2013. pp. 28, 34. ISBN 978-1-4832-8810-9. https://books.google.com/books?id=IT2OAgAAQBAJ&pg=PA34. 
  7. ↑ American College of Neuropsychopharmacology (1978). Psychopharmacology: a generation of progress. Raven Press. p. 514. ISBN 978-0-89004-191-8. https://books.google.com/books?id=c-RsAAAAMAAJ. 
  8. ↑ "DREADD Agonist 21 Is an Effective Agonist for Muscarinic-Based DREADDs in Vitro and in Vivo". ACS Pharmacology & Translational Science 1 (1): 61–72. September 2018. doi:10.1021/acsptsci.8b00012. PMID 30868140. 
  9. ↑ "The first structure-activity relationship studies for designer receptors exclusively activated by designer drugs". ACS Chemical Neuroscience 6 (3): 476–484. March 2015. doi:10.1021/cn500325v. PMID 25587888. 




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