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Perlapine









Perlapine


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Perlapine
Perlapine.svg
Clinical data
Trade names Hypnodine, Pipnodine
Synonyms AW-14233; HF-2333; MP-11; PLP 100-127; 6-(4-Methyl-1-piperazinyl)morphanthridine
Identifiers
CAS Number
  • 1977-11-3

PubChem CID
  • 16106
ChemSpider
  • 15291
UNII
  • 4N8UJJ27IM
KEGG
  • D01438
ChEBI
  • CHEBI:31983
ChEMBL
  • ChEMBL340801
Chemical and physical data
Formula
C19H21N3
Molar mass 291.398 g/mol
3D model (JSmol)
  • Interactive image

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 recpetor, and 70 nM for the serotonin 5-HT2A receptor.[6] Perlapine is closely related to clotiapine, clozapine, fluperlapine, loxapine, and tilozepine.[6]



References[edit]





  1. ^ Index Nominum 2000: International Drug Directory. Taylor & Francis. 2000. pp. 811–. ISBN 978-3-88763-075-1..mw-parser-output cite.citation{font-style:inherit}.mw-parser-output q{quotes:"""""""'""'"}.mw-parser-output code.cs1-code{color:inherit;background:inherit;border:inherit;padding:inherit}.mw-parser-output .cs1-lock-free a{background:url("//upload.wikimedia.org/wikipedia/commons/thumb/6/65/Lock-green.svg/9px-Lock-green.svg.png")no-repeat;background-position:right .1em center}.mw-parser-output .cs1-lock-limited a,.mw-parser-output .cs1-lock-registration a{background:url("//upload.wikimedia.org/wikipedia/commons/thumb/d/d6/Lock-gray-alt-2.svg/9px-Lock-gray-alt-2.svg.png")no-repeat;background-position:right .1em center}.mw-parser-output .cs1-lock-subscription a{background:url("//upload.wikimedia.org/wikipedia/commons/thumb/a/aa/Lock-red-alt-2.svg/9px-Lock-red-alt-2.svg.png")no-repeat;background-position:right .1em center}.mw-parser-output .cs1-subscription,.mw-parser-output .cs1-registration{color:#555}.mw-parser-output .cs1-subscription span,.mw-parser-output .cs1-registration span{border-bottom:1px dotted;cursor:help}.mw-parser-output .cs1-hidden-error{display:none;font-size:100%}.mw-parser-output .cs1-visible-error{font-size:100%}.mw-parser-output .cs1-subscription,.mw-parser-output .cs1-registration,.mw-parser-output .cs1-format{font-size:95%}.mw-parser-output .cs1-kern-left,.mw-parser-output .cs1-kern-wl-left{padding-left:0.2em}.mw-parser-output .cs1-kern-right,.mw-parser-output .cs1-kern-wl-right{padding-right:0.2em}


  2. ^ ab Abel Lajtha (11 November 2013). Alterations of Metabolites in the Nervous System. Springer Science & Business Media. pp. 352–. ISBN 978-1-4757-6740-7.


  3. ^ ab Progress in Medicinal Chemistry. Elsevier. 24 April 1996. pp. 226–. ISBN 978-0-08-086281-1.


  4. ^ D E Hathway (31 October 2007). Foreign Compound Metabolism in Mammals. Royal Society of Chemistry. pp. 302–. ISBN 978-1-84755-608-0.


  5. ^ Bentham Science Publishers (April 1995). Current Medicinal Chemistry. Bentham Science Publishers. pp. 489–.


  6. ^ abcde Thomas R.E. Barnes (22 October 2013). Antipsychotic Drugs and Their Side-Effects. Elsevier Science. pp. 28, 34. ISBN 978-1-4832-8810-9.


  7. ^ American College of Neuropsychopharmacology (1978). Psychopharmacology: a generation of progress. Raven Press. p. 514. ISBN 978-0-89004-191-8.



















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