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.
N1 - Funding Information:
The authors thank Dr. William Haefely of Hoffman-LaRoehc, Basle, Switzerland, for providing the Ro-15-1788, Dr. Josee Leysen of Janssen Pharmaceuticals for providing the enantiomers of e\[omidatc and Dr. Jeffrey Malick of ICI Pharmaceuticals for providing tracazolate. We also thank Susan Yamamura for computer programming assistance. Part of this work was supported by Public Health Service Grants MH-27257, MH-30626, HL-21486 and Program Project Grant HL-20984 and the Arizona Committee to Combat Huntington's Disease.H .I.Y. is a recipient of a USPHS Research Scientist Development Award, Type II (MH-00095), from the National Institute of mental Health, and W.I~.R. is a recipient of a usPHS R.esearch Career Development Award (HL-00776) from the National Heart Lung and Blood Institute.
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 -