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EZS-8

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(Redirected fromQuinazolinylethylamine)

Pharmaceutical compound
EZS-8
Clinical data
Other names3-(2-Aminoethyl)quinazoline-2,4-dione
Drug classSerotonin5-HT2A receptorpartial agonist
ATC code
  • None
Identifiers
  • 3-(2-aminoethyl)-1H-quinazoline-2,4-dione
CAS Number
PubChemCID
ChemSpider
ChEMBL
Chemical and physical data
FormulaC10H11N3O2
Molar mass205.217 g·mol−1
3D model (JSmol)
  • C1=CC=C2C(=C1)C(=O)N(C(=O)N2)CCN
  • InChI=1S/C10H11N3O2/c11-5-6-13-9(14)7-3-1-2-4-8(7)12-10(13)15/h1-4H,5-6,11H2,(H,12,15)
  • Key:NTAUXYQQSCPGHT-UHFFFAOYSA-N

EZS-8, also known as3-(2-aminoethyl)quinazoline-2,4-dione, is a very-low-potencyserotonin5-HT2A receptorpartial agonist related toketanserin.[1][2][3][4] It has about 0.15% of the potency (EC50Tooltip half-maximal effective concentration = 66,000 nM) and 46% of theefficacy (EmaxTooltip maximal efficacy) of serotonin as a serotonin 5-HT2A receptor agonistin vitro.[1][2][3][4] TheN-(2-methoxy)benzylanalogue of EZS-8,RH-34, has 250-fold greater potency as a serotonin 5-HT2A receptor agonist in comparison.[2][3][4] EZS-8 was first described in thescientific literature by 1999.[1]N-Benzylderivatives of EZS-8 like RH-34 had been described as early as 1996 or 1998.[5][6]

References

[edit]
  1. ^abcHeim R, Pertz HH, Elz S (1999)."Preparation and in vitro pharmacology of novel secondary amine-type 5-HT2A receptor agonists: from submillimolar to subnanomolar activity".Arch. Pharm. Pharm. Med. Chem.332: 34.
  2. ^abcElz S, Klass T, Heim R, Warnke U, Pertz HH (2002)."Development of highly potent partial agonists and chiral antagonists as tools for the study of 5-HT2A-receptor mediated function".Naunyn-Schmiedeberg's Archives of Pharmacology.365 (1 Suppl):R21 –R40.doi:10.1007/s00210-002-0604-4.
  3. ^abcSilva M (2009).Theoretical study of the interaction of agonists with the 5-HT2A receptor (PhD.). Universität Regensburg.Table 5.1: Agonistic potency (pEC50) and intrinsic activity (Emax) of 5-HT2AR partial agonistic arylethylamines (indole, methoxybenzene and quinazolinedione derivatives) used in the study. [...]
  4. ^abcSilva ME, Heim R, Strasser A, Elz S, Dove S (January 2011)."Theoretical studies on the interaction of partial agonists with the 5-HT2A receptor".Journal of Computer-Aided Molecular Design.25 (1):51–66.Bibcode:2011JCAMD..25...51S.doi:10.1007/s10822-010-9400-2.PMID 21088982.
  5. ^Heim R, Pertz H, Walther I, Elz S (January 1998)."P 8.10. Congeners of 3-(2-benzylaminoethyl)-2, 4-quinazolinedione: Partial agonists for rat vascular 5-HT2A receptors".Naunyn-Schmiedebergs Archives of Pharmacology.358 (1): R105.
  6. ^"Abstracts: 331: Characterization of the Partial Agonism of Ergoline Reverse Esters, Indolyltetrahydropyridines, and Quinazolinediones at 5-HT2A receptors in Rat Tail Artery".Naunyn-Schmiedeberg's Archives of Pharmacology.353 (S4): R1–R166 (R90–R91). 1996.doi:10.1007/BF00625102.ISSN 0028-1298.The aim of the study was to characterize the partial agonism of congeners of well-established 5-HT2A receptor ligands, identified in a series of ergot alkaloids (so-called ergoline reverse esters with lysergol and dihydrolysergol-I as alcoholic component), indolyltetrahydropyridines (RU 24969 and two derivatives), and quinazolinediones (derivatives of ketanserin), at 5-HT2A receptors in rat tail artery. [...] Quinazolinediones (derivatives of ketanserin) showed weak agonist activity (pKp = 3.83 - 4.66, α = 0.17 - 0,46) and antagonized contractile responses to 5-HT with calculated pKp values of 3.52 - 5.12.

External links

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5-HT2C
5-HT3–7
5-HT3
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5-HT5A
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