The Pharmacology of the Benzodiazepine Site of the GABA-A Receptor is Dependent on the Type of γ-Subunit Present

1995 ◽  
Vol 15 (1-4) ◽  
pp. 173-183 ◽  
Author(s):  
R. M. McKernan ◽  
K. Wafford ◽  
K. Quirk ◽  
K. L. Hadingham ◽  
E. A. Harley ◽  
...  
Keyword(s):  
Gaba A ◽  
Γ Subunit ◽  
Benzodiazepine Site

scholarly journals Flavones-bound in benzodiazepine site on GABA A receptor: Concomitant anxiolytic-like and cognitive-enhancing effects produced by Isovitexin and 6-C-glycoside-Diosmetin

2018 ◽  
Vol 831 ◽  
pp. 77-86 ◽  
Author(s):  
Daniela Rodrigues de Oliveira ◽  
Andréia Hatsue Todo ◽  
Gizelda Maia Rêgo ◽  
Janete Maria Cerutti ◽  
Alberto José Cavalheiro ◽  
...  
Keyword(s):  
Gaba A ◽  
Benzodiazepine Site

Key Amino Acids in the γ Subunit of the γ-Aminobutyric AcidA Receptor that Determine Ligand Binding and Modulation at the Benzodiazepine Site

1997 ◽  
Vol 52 (5) ◽  
pp. 874-881 ◽  
Author(s):  
Peter B. Wingrove ◽  
Sally A. Thompson ◽  
Keith A. Wafford ◽  
Paul J. Whiting
Keyword(s):  
Amino Acids ◽  
Ligand Binding ◽  
Γ Subunit ◽  
Benzodiazepine Site

GABA A Receptor Subtypes Differentiated by their γ-Subunit Variants: Prevalence, Pharmacology and Subunit Architecture

1996 ◽  
Vol 35 (9-10) ◽  
pp. 1413-1423 ◽  
Author(s):  
D. BENKE ◽  
M. HONER ◽  
C. MICHEL ◽  
H. MOHLER
Keyword(s):  
Receptor Subtypes ◽  
Gaba A ◽  
Γ Subunit

scholarly journals Anticonvulsant profile of 2-ethylthio-7-methyl-4-(4-methylphenyl)pyrazolo[1,5-a][1,3,5]triazine

2014 ◽  
Vol 50 (1) ◽  
pp. 73-81
Author(s):  
Martín Hermógenes Estrada ◽  
Henry Insuasty ◽  
Luis Enrique Cuca ◽  
Mariel Marder ◽  
Angélica Fierro ◽  
...  
Keyword(s):  
Maximal Electroshock ◽  
Dependent Manner ◽  
Maximal Electroshock Seizure ◽  
Gaba A ◽  
Mao B ◽  
Plus Maze ◽  
Marble Burying ◽  
One Step ◽  
Dose Dependent ◽  
Benzodiazepine Site

This work evaluates the central nervous effects in ICR strain mice of 2-ethylthio-7-methyl-4-(4-methylphenyl)pyrazolo[1,5-a][1,3,5]triazine (MH4b1), a compound obtained by an efficient one-step reaction of S,S-diethyl 4-methylbenzoylimidodithiocarbonate with 5-amino-3-methyl-1H-pyrazole, in order to assess its neuro-pharmacological profile. The tests applied were: maximal electroshock seizure (MES), pentylenetetrazole (PTZ) seizures, forced swimming, plus maze, marble burying, sleeping time, rota-rod and catalepsy. In addition, MH4b1 binding to the benzodiazepine site of the GABA-A receptor and MH4b1 inhibition of monoamine oxidase (MAO) subtypes A and B were evaluated. MH4b1 showed anticonvulsant effects in a dose dependent manner (30-300 mg/kg, p.o.) against MES and inhibition of MAO-B (IC50: 24.5 µM) without activity at the benzodiazepine site. These data suggest that MH4b1 has anticonvulsant properties related to MAO-B inhibition.

scholarly journals From the Behavioral Pharmacology of Beta-Carbolines to Seizures, Anxiety, and Memory

2007 ◽  
Vol 7 ◽  
pp. 204-223 ◽  
Author(s):  
Patrice Venault ◽  
Georges Chapouthier
Keyword(s):  
Epileptic Seizures ◽  
Behavioral Pharmacology ◽  
Mouse Strains ◽  
Receptor Complex ◽  
Low Doses ◽  
Learning Abilities ◽  
Gaba A ◽  
High Doses ◽  
Benzodiazepine Site ◽  
Receptor Channel

A number of beta-carbolines are inverse agonists of the GABA-A receptor complex, acting on the benzodiazepine site. They show convulsive properties when administered at high doses, anxiogenic properties at moderate doses, and learning-enhancing effects at low doses. These data suggest a possible physiological relationship, through the GABA-A receptor channel, between memory processes, anxiety, and ultimately, in pathological states, epileptic seizures. This relationship seems to be confirmed partially by experiments on mouse strains selected for their resistance (BR) and sensitivity (BS) to a single convulsive dose of a beta-carboline. These two strains also show differences in anxiety and learning abilities. However, some opposite results found while observing the behavior of the two strains suggest that in addition to pharmacologically induced anxiety, there is spontaneous anxiety, no doubt involving other brain mechanisms.

scholarly journals Experiment‐guided virtual screening provides new high affinity ligands for the benzodiazepine site on GABA‐A receptors (654.4)

2014 ◽  
Vol 28 (S1) ◽  
Author(s):  
Erwin Sigel ◽  
Simon Middendorp ◽  
Roland Baur ◽  
Roshan Puthenkalam ◽  
Margot Ernst
Keyword(s):  
Virtual Screening ◽  
Gaba A ◽  
Affinity Ligands ◽  
High Affinity ◽  
Benzodiazepine Site

[ 3 H]L-655,708, a Novel Ligand Selective for the Benzodiazepine Site of GABA A Receptors which Contain the α5 Subunit

1996 ◽  
Vol 35 (9-10) ◽  
pp. 1331-1335 ◽  
Author(s):  
K. QUIRK ◽  
P. BLURTON ◽  
S. FLETCHER ◽  
P. LEESON ◽  
F. TANG ◽  
...  
Keyword(s):  
Gaba A ◽  
Benzodiazepine Site

Cinnamamides from Piper capense with affinity to the benzodiazepine site on the GABAA receptor

Planta Medica ◽  
2008 ◽  
Vol 74 (09) ◽  
Author(s):  
ME Pedersen ◽  
HB Rasmussen ◽  
B Metzler ◽  
GI Stafford ◽  
J van Staden ◽  
...  
Keyword(s):  
Gabaa Receptor ◽  
Benzodiazepine Site
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