Specific binding of racemic oxazepam esters to rat brain synaptosomes and the influence of bioactivation by esterases

G. Maksay, J. Kardos, M. Simonyi, Z. Tegyey, L. Otvös

Research output: Contribution to journalArticle

9 Citations (Scopus)

Abstract

Six aliphatic esters of oxazepam were investigated for 3H-diazepam displacing activity and hyrolysis in rat brain synaptosomal preparations. IC 50 values were measured in the brain P 2-fraction treated with diisopropylfluorophosphate. The esters are prodrugs in relation to oxazepam. Increasing size of the 3-substituent and steric hindrance increased the value of IC 50. Controversial reports on oxazepam hemisuccinate could be explained by its stereoselective hydrolysis in vitro.

Original languageEnglish
Pages (from-to)979-981
Number of pages3
JournalArzneimittel-Forschung
Volume31
Issue number6
Publication statusPublished - 1981

Fingerprint

Oxazepam
Synaptosomes
Esterases
Rats
Brain
Esters
Isoflurophate
Prodrugs
Diazepam
Hydrolysis
In Vitro Techniques
oxazepam hemisuccinate

ASJC Scopus subject areas

  • Drug Discovery
  • Organic Chemistry
  • Chemistry(all)
  • Pharmacology

Cite this

Specific binding of racemic oxazepam esters to rat brain synaptosomes and the influence of bioactivation by esterases. / Maksay, G.; Kardos, J.; Simonyi, M.; Tegyey, Z.; Otvös, L.

In: Arzneimittel-Forschung, Vol. 31, No. 6, 1981, p. 979-981.

Research output: Contribution to journalArticle

@article{9baffd6c5b744d19b2b733de15fb0a7e,
title = "Specific binding of racemic oxazepam esters to rat brain synaptosomes and the influence of bioactivation by esterases",
abstract = "Six aliphatic esters of oxazepam were investigated for 3H-diazepam displacing activity and hyrolysis in rat brain synaptosomal preparations. IC 50 values were measured in the brain P 2-fraction treated with diisopropylfluorophosphate. The esters are prodrugs in relation to oxazepam. Increasing size of the 3-substituent and steric hindrance increased the value of IC 50. Controversial reports on oxazepam hemisuccinate could be explained by its stereoselective hydrolysis in vitro.",
author = "G. Maksay and J. Kardos and M. Simonyi and Z. Tegyey and L. Otv{\"o}s",
year = "1981",
language = "English",
volume = "31",
pages = "979--981",
journal = "Drug Research",
issn = "2194-9379",
publisher = "Thieme",
number = "6",

}

TY - JOUR

T1 - Specific binding of racemic oxazepam esters to rat brain synaptosomes and the influence of bioactivation by esterases

AU - Maksay, G.

AU - Kardos, J.

AU - Simonyi, M.

AU - Tegyey, Z.

AU - Otvös, L.

PY - 1981

Y1 - 1981

N2 - Six aliphatic esters of oxazepam were investigated for 3H-diazepam displacing activity and hyrolysis in rat brain synaptosomal preparations. IC 50 values were measured in the brain P 2-fraction treated with diisopropylfluorophosphate. The esters are prodrugs in relation to oxazepam. Increasing size of the 3-substituent and steric hindrance increased the value of IC 50. Controversial reports on oxazepam hemisuccinate could be explained by its stereoselective hydrolysis in vitro.

AB - Six aliphatic esters of oxazepam were investigated for 3H-diazepam displacing activity and hyrolysis in rat brain synaptosomal preparations. IC 50 values were measured in the brain P 2-fraction treated with diisopropylfluorophosphate. The esters are prodrugs in relation to oxazepam. Increasing size of the 3-substituent and steric hindrance increased the value of IC 50. Controversial reports on oxazepam hemisuccinate could be explained by its stereoselective hydrolysis in vitro.

UR - http://www.scopus.com/inward/record.url?scp=0019435953&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=0019435953&partnerID=8YFLogxK

M3 - Article

C2 - 7196245

AN - SCOPUS:0019435953

VL - 31

SP - 979

EP - 981

JO - Drug Research

JF - Drug Research

SN - 2194-9379

IS - 6

ER -