Modulation of benzodiazepine receptor binding: Insight into pharmacological efficacy

Frederick J. Ehlert, Paul Ragan, Andrew Chen, William R. Roeske, Henry I. Yamamura

Research output: Contribution to journalArticle

47 Citations (Scopus)

Abstract

The effects of GABA on the binding of analogues of benzodiazepine, triazolopyridazines, β-carbolines and imidazodiazepines were examined in ligand/[3H]flunitrazepan competition experiments. GABA increased the potency of anxiolytics, like flunitrazepam, whereas the potency of benzodiazepine antagonists, like Ro15-1788, was largely insensitive to the influence of GABA. Several other agents including pyrazolopyridines, barbiturates and etomidate caused a chloride dependent enhancement of [3H]flunitrazepam binding but not an enhancement of [3H]propyl-β-carboline-3-carboxylate binding.

Original languageEnglish (US)
Pages (from-to)249-253
Number of pages5
JournalEuropean Journal of Pharmacology
Volume78
Issue number2
DOIs
StatePublished - Feb 26 1982
Externally publishedYes

Fingerprint

GABA-A Receptors
gamma-Aminobutyric Acid
Flunitrazepam
Carbolines
Pharmacology
Benzodiazepines
Etomidate
Barbiturates
Anti-Anxiety Agents
Chlorides
Ligands

Keywords

  • Barbiturates
  • Benzodiazepine receptor agonists and antagonists
  • Etomidate
  • GABA
  • Pyrazolopyridines

ASJC Scopus subject areas

  • Cellular and Molecular Neuroscience
  • Pharmacology

Cite this

Modulation of benzodiazepine receptor binding : Insight into pharmacological efficacy. / Ehlert, Frederick J.; Ragan, Paul; Chen, Andrew; Roeske, William R.; Yamamura, Henry I.

In: European Journal of Pharmacology, Vol. 78, No. 2, 26.02.1982, p. 249-253.

Research output: Contribution to journalArticle

Ehlert, Frederick J. ; Ragan, Paul ; Chen, Andrew ; Roeske, William R. ; Yamamura, Henry I. / Modulation of benzodiazepine receptor binding : Insight into pharmacological efficacy. In: European Journal of Pharmacology. 1982 ; Vol. 78, No. 2. pp. 249-253.
@article{155b9b21a81341b4acad132c9f060aac,
title = "Modulation of benzodiazepine receptor binding: Insight into pharmacological efficacy",
abstract = "The effects of GABA on the binding of analogues of benzodiazepine, triazolopyridazines, β-carbolines and imidazodiazepines were examined in ligand/[3H]flunitrazepan competition experiments. GABA increased the potency of anxiolytics, like flunitrazepam, whereas the potency of benzodiazepine antagonists, like Ro15-1788, was largely insensitive to the influence of GABA. Several other agents including pyrazolopyridines, barbiturates and etomidate caused a chloride dependent enhancement of [3H]flunitrazepam binding but not an enhancement of [3H]propyl-β-carboline-3-carboxylate binding.",
keywords = "Barbiturates, Benzodiazepine receptor agonists and antagonists, Etomidate, GABA, Pyrazolopyridines",
author = "Ehlert, {Frederick J.} and Paul Ragan and Andrew Chen and Roeske, {William R.} and Yamamura, {Henry I.}",
year = "1982",
month = "2",
day = "26",
doi = "10.1016/0014-2999(82)90246-1",
language = "English (US)",
volume = "78",
pages = "249--253",
journal = "European Journal of Pharmacology",
issn = "0014-2999",
publisher = "Elsevier",
number = "2",

}

TY - JOUR

T1 - Modulation of benzodiazepine receptor binding

T2 - Insight into pharmacological efficacy

AU - Ehlert, Frederick J.

AU - Ragan, Paul

AU - Chen, Andrew

AU - Roeske, William R.

AU - Yamamura, Henry I.

PY - 1982/2/26

Y1 - 1982/2/26

N2 - The effects of GABA on the binding of analogues of benzodiazepine, triazolopyridazines, β-carbolines and imidazodiazepines were examined in ligand/[3H]flunitrazepan competition experiments. GABA increased the potency of anxiolytics, like flunitrazepam, whereas the potency of benzodiazepine antagonists, like Ro15-1788, was largely insensitive to the influence of GABA. Several other agents including pyrazolopyridines, barbiturates and etomidate caused a chloride dependent enhancement of [3H]flunitrazepam binding but not an enhancement of [3H]propyl-β-carboline-3-carboxylate binding.

AB - The effects of GABA on the binding of analogues of benzodiazepine, triazolopyridazines, β-carbolines and imidazodiazepines were examined in ligand/[3H]flunitrazepan competition experiments. GABA increased the potency of anxiolytics, like flunitrazepam, whereas the potency of benzodiazepine antagonists, like Ro15-1788, was largely insensitive to the influence of GABA. Several other agents including pyrazolopyridines, barbiturates and etomidate caused a chloride dependent enhancement of [3H]flunitrazepam binding but not an enhancement of [3H]propyl-β-carboline-3-carboxylate binding.

KW - Barbiturates

KW - Benzodiazepine receptor agonists and antagonists

KW - Etomidate

KW - GABA

KW - Pyrazolopyridines

UR - http://www.scopus.com/inward/record.url?scp=0020081045&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=0020081045&partnerID=8YFLogxK

U2 - 10.1016/0014-2999(82)90246-1

DO - 10.1016/0014-2999(82)90246-1

M3 - Article

C2 - 6281035

AN - SCOPUS:0020081045

VL - 78

SP - 249

EP - 253

JO - European Journal of Pharmacology

JF - European Journal of Pharmacology

SN - 0014-2999

IS - 2

ER -