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Pirenperone

From Wikipedia, the free encyclopedia
Chemical compound
Not to be confused withPipamperone.
Pharmaceutical compound
Pirenperone
Clinical data
Other namesR-47456; R-50656; Pirenpirone
Identifiers
  • 3-[2-[4-(4-Fluorobenzoyl)piperidin-1-yl]ethyl]-2-methylpyrido[1,2-a]pyrimidin-4-one
CAS Number
PubChemCID
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard(EPA)
ECHA InfoCard100.071.081Edit this at Wikidata
Chemical and physical data
FormulaC23H24FN3O2
Molar mass393.462 g·mol−1
3D model (JSmol)
  • CC1=C(C(=O)N2C=CC=CC2=N1)CCN3CCC(CC3)C(=O)C4=CC=C(C=C4)F
  • InChI=1S/C23H24FN3O2/c1-16-20(23(29)27-12-3-2-4-21(27)25-16)11-15-26-13-9-18(10-14-26)22(28)17-5-7-19(24)8-6-17/h2-8,12,18H,9-11,13-15H2,1H3
  • Key:HXCNRYXBZNHDNE-UHFFFAOYSA-N

Pirenperone (INNTooltip International Nonproprietary Name,USANTooltip United States Adopted Name,BANTooltip British Approved Name; developmental code namesR-47456,R-50656) is aserotonin receptor antagonist closely related toketanserin andrisperidone which is described as anantipsychotic andtranquilizer and was never marketed.[1][2]

It is a relativelyselectiveantagonist of theserotonin5-HT2A receptor and has been used inscientific research to study theserotonin system.[3][2][4][5] Itsaffinities (Ki) for serotonin and other receptors have been reported to be 0.3 to 1.1 nM for the serotonin 5-HT2A receptor, 6.5 nM for the serotonin5-HT7 receptor, 20 nM for theα1B-adrenergic receptor, 20 nM for theα2B-adrenergic receptor, 61 nM for the serotonin5-HT2B receptor, 60 to 77 nM for the serotonin5-HT2C receptor, 485 to 1,700 nM for the serotonin5-HT1A receptor, and >1,000 or 6,600 nM for the serotonin5-HT1B receptor, whereas other receptors were not reported.[3][5]

In the 1980s, the drug was found to block the effects of thelysergic acid diethylamide (LSD) in animals, and, along withketanserin, led to the elucidation of the5-HT2A receptor as thebiological mediator of the effects of serotonergic psychedelics.[6]

See also

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References

[edit]
  1. ^Elks J (14 November 2014).The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies. Springer. pp. 994–.ISBN 978-1-4757-2085-3.
  2. ^abMorton IK, Hall JM (31 October 1999).Concise Dictionary of Pharmacological Agents: Properties and Synonyms. Springer Science & Business Media. pp. 223–.ISBN 978-0-7514-0499-9.
  3. ^abCasey AB, Cui M, Booth RG, Canal CE (June 2022).""Selective" serotonin 5-HT2A receptor antagonists".Biochem Pharmacol.200 115028.doi:10.1016/j.bcp.2022.115028.PMC 9252399.PMID 35381208.
  4. ^Colpaert FC, Balster R (6 December 2012).Transduction Mechanisms of Drug Stimuli. Springer Science & Business Media. pp. 29–.ISBN 978-3-642-73223-2.
  5. ^abGlennon RA (January 1987). "Central serotonin receptors as targets for drug research".J Med Chem.30 (1):1–12.doi:10.1021/jm00384a001.PMID 3543362.Table II. Affinities of Selected Phenalkylamines for 5-HT1 and 5-HT2 Binding Sites
  6. ^Nichols DE (April 2016)."Psychedelics".Pharmacological Reviews.68 (2):264–355.doi:10.1124/pr.115.011478.PMC 4813425.PMID 26841800.
5-HT1
5-HT1A
5-HT1B
5-HT1D
5-HT1E
5-HT1F
5-HT2
5-HT2A
5-HT2B
5-HT2C
5-HT3–7
5-HT3
5-HT4
5-HT5A
5-HT6
5-HT7
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