Quantitative analysis of drug-receptor interactions: I. Determination of kinetic and equilibrium properties

GA Weiland, PB Molinoff - Life sciences, 1981 - Elsevier
It has recently become possible to characterize a variety of different receptors by studying
the binding of appropriate drugs labelled with 3 H or 125 I. The goal of this review is to …

Positive allosteric modulation of GABAA receptors by a novel antiepileptic drug cenobamate

R Sharma, M Nakamura, C Neupane, BH Jeon… - European journal of …, 2020 - Elsevier
Cenobamate is a novel antiepileptic drug under investigation for use in patients with focal
(partial-onset) seizures. To understand its potential molecular mechanism of action, the …

Inhibition of phosphodiesterase 2 increases neuronal cGMP, synaptic plasticity and memory performance

FG Boess, M Hendrix, FJ van der Staay, C Erb… - …, 2004 - Elsevier
An essential element of the signalling cascade leading to synaptic plasticity is the
intracellular second messenger molecule guanosine 3′, 5′-cyclic monophosphate …

Differentiation between two ligands for peripheral benzodiazepine binding sites,[3H] R05-4864 and [3H] PK 11195, by thermodynamic studies

G Le Fur, N Vaucher, ML Perrier, A Flamier… - Life sciences, 1983 - Elsevier
Abstract The [3 H] PK 11195, 1-(2-chlorophenyl)-N-methyl-N-(1-methylpropyl)-3-
isoquinolinecarboxamide, binding sites in rat cardiac membranes are saturable, with high …

ICA-17043, a novel Gardos channel blocker, prevents sickled red blood cell dehydration in vitro and in vivo in SAD mice

JW Stocker, L De Franceschi… - Blood, The Journal …, 2003 - ashpublications.org
A prominent feature of sickle cell anemia is the presence of dehydrated red blood cells
(RBCs) in circulation. Loss of potassium (K+), chloride (Cl−), and water from RBCs is thought …

Electrophysiology of benzodiazepine receptor ligands: multiple mechanisms and sites of action

P Polc - Progress in neurobiology, 1988 - Elsevier
Electrophysiology of BZR ligands has been reviewed from different points of view. A great
effort was made to critically discuss the arguments for and against the temporarily leading …

Immunohistochemical mapping of vitamin D-dependent calcium-binding protein in brain

SS Jande, L Maler, DEM Lawson - Nature, 1981 - nature.com
Abstract The steroid hormone, 1, 25-dihydroxycholecalciferol (1, 25-(OH) 2D3) causes the
de novo synthesis of a calcium-binding protein (D-CaBP) 1, 2. This protein is present in …

Agonist and antagonist benzodiazepine receptor interaction in vitro

H Möhler, JG Richards - Nature, 1981 - nature.com
A representative of a novel series of imidazodiazepines, Ro 15-1788, selectively
antagonizes all major central actions of benzodiazepines by competitive, high-affinity …

Resolution of two biochemically and pharmacologically distinct benzodiazepine receptors

CA Klepner, AS Lippa, DI Benson, MC Sano… - Pharmacology …, 1979 - Elsevier
Brain-specific binding sites have been isolated on synaptosomal membrane fragments
which recognize pharmacologically active benzodiazepine (BDZ's) and triazolopyridazines …

Modulation of GABAergic synaptic transmission by the non-benzodiazepine anxiolytic etifoxine

R Schlichter, V Rybalchenko, P Poisbeau, M Verleye… - …, 2000 - Elsevier
We have investigated the effects of 2-ethylamino-6-chloro-4-methyl-4-phenyl-4H-3, 1-
benzoxazine hydrochloride (etifoxine) on GABAA receptor function. Etifoxine displaced [35S] …