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Advancements in the use of xenopus oocytes for modelling neurological disease for novel drug discovery. , O'Connor EC., Expert Opin Drug Discov. February 1, 2024; 19 (2): 173-187.
GABAergic Neurotransmission in Human Tissues Is Modulated by Cannabidiol. , Ruffolo G., Life (Basel). December 6, 2022; 12 (12):
GABAA receptor function is enhanced by Interleukin-10 in human epileptogenic gangliogliomas and its effect is counteracted by Interleukin-1β. , Ruffolo G., Sci Rep. October 26, 2022; 12 (1): 17956.
Unexpected Effect of IL-1β on the Function of GABAA Receptors in Pediatric Focal Cortical Dysplasia. , Alfano V., Brain Sci. June 19, 2022; 12 (6):
Basmisanil, a highly selective GABAA-α5 negative allosteric modulator: preclinical pharmacology and demonstration of functional target engagement in man. , Hipp JF., Sci Rep. April 8, 2021; 11 (1): 7700.
Dissecting the Molecular Determinants of GABAA Receptors Current Rundown, a Hallmark of Refractory Human Epilepsy. , Cifelli P., Brain Sci. March 30, 2021; 11 (4):
GABAA Receptors Expressed in Oligodendrocytes Cultured from the Neonatal Rat Contain α3 and γ1 Subunits and Present Differential Functional and Pharmacological Properties. , Ordaz RP., Mol Pharmacol. February 1, 2021; 99 (2): 133-146.
GABAA Receptor Subunit Composition Drives Its Sensitivity to the Insecticide Fipronil. , Soualah Z., Front Neurosci. January 1, 2021; 15 768466.
In vitro and in vivo characterization of Lu AA41178: A novel, brain penetrant, pan-selective Kv7 potassium channel opener with efficacy in preclinical models of epileptic seizures and psychiatric disorders. , Grupe M., Eur J Pharmacol. November 15, 2020; 887 173440.
PNU-120596, a positive allosteric modulator of mammalian α7 nicotinic acetylcholine receptor, is a negative modulator of ligand-gated chloride-selective channels of the gastropod Lymnaea stagnalis. , Vulfius CA., J Neurochem. November 1, 2020; 155 (3): 274-284.
The desensitization pathway of GABAA receptors, one subunit at a time. , Gielen M., Nat Commun. October 23, 2020; 11 (1): 5369.
Analysis of Modulation of the ρ1 GABAA Receptor by Combinations of Inhibitory and Potentiating Neurosteroids Reveals Shared and Distinct Binding Sites. , Germann AL., Mol Pharmacol. October 1, 2020; 98 (4): 280-291.
Erythropoietin Increases GABAA Currents in Human Cortex from TLE Patients. , Roseti C., Neuroscience. July 15, 2020; 439 153-162.
Differential Coassembly of α1-GABAARs Associated with Epileptic Encephalopathy. , Hannan S., J Neurosci. July 15, 2020; 40 (29): 5518-5530.
Functional characterization of the antiepileptic drug candidate, padsevonil, on GABAA receptors. , Niespodziany I., Epilepsia. May 1, 2020; 61 (5): 914-923.
Reduced neurosteroid potentiation of GABAA receptors in epilepsy and depolarized hippocampal neurons. , Joshi S., Ann Clin Transl Neurol. April 1, 2020; 7 (4): 527-542.
Cloning and Expression of Cockroach α7 Nicotinic Acetylcholine Receptor Subunit. , Cartereau A., Front Physiol. January 1, 2020; 11 418.
Steady-state activation of the high-affinity isoform of the α4β2δ GABAA receptor. , Pierce SR., Sci Rep. November 5, 2019; 9 (1): 15997.
Coadministered cannabidiol and clobazam: Preclinical evidence for both pharmacodynamic and pharmacokinetic interactions. , Anderson LL., Epilepsia. November 1, 2019; 60 (11): 2224-2234.
Natural product incarvillateine aggravates epileptic seizures by inhibiting GABAA currents. , Bian X., Eur J Pharmacol. September 5, 2019; 858 172496.
Involvement of the GABAA receptor α subunit in the mode of action of etifoxine. , Mattei C., Pharmacol Res. July 1, 2019; 145 104250.
Multiple actions of fenamates and other nonsteroidal anti-inflammatory drugs on GABAA receptors. , Mansikkamäki S., Eur J Pharmacol. June 15, 2019; 853 247-255.
Ketone body modulation of ligand-gated ion channels. , Pflanz NC., Neuropharmacology. April 1, 2019; 148 21-30.
Design and Synthesis of Novel Positive Allosteric Modulators of α7 Nicotinic Acetylcholine Receptors with the Ability To Rescue Auditory Gating Deficit in Mice. , Li Y., J Med Chem. January 10, 2019; 62 (1): 159-173.
A novel GABAergic dysfunction in human Dravet syndrome. , Ruffolo G., Epilepsia. November 1, 2018; 59 (11): 2106-2117.
Suramin is a novel competitive antagonist selective to α1β2γ2 GABAA over ρ1 GABAC receptors. , Luo H., Neuropharmacology. October 1, 2018; 141 148-157.
Structural basis of neurosteroid anesthetic action on GABAA receptors. , Chen Q., Nat Commun. September 28, 2018; 9 (1): 3972.
Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission. , Knoflach F., J Vis Exp. August 16, 2018; (138):
A novel action of lacosamide on GABAA currents sets the ground for a synergic interaction with levetiracetam in treatment of epilepsy. , Ruffolo G., Neurobiol Dis. July 1, 2018; 115 59-68.
Direct neurotransmitter activation of voltage-gated potassium channels. , Manville RW., Nat Commun. May 10, 2018; 9 (1): 1847.
Direct intertectal inputs are an integral component of the bilateral sensorimotor circuit for behavior in Xenopus tadpoles. , Gambrill AC., J Neurophysiol. May 1, 2018; 119 (5): 1947-1961.
Assembly rules for GABAA receptor complexes in the brain. , Martenson JS., Elife. August 17, 2017; 6
Novel Molecule Exhibiting Selective Affinity for GABAA Receptor Subtypes. , Borghese CM., Sci Rep. July 24, 2017; 7 (1): 6230.
HPLC-Based Activity Profiling for GABAA Receptor Modulators in Extracts: Validation of an Approach Utilizing a Larval Zebrafish Locomotor Assay. , Moradi-Afrapoli F., J Nat Prod. May 26, 2017; 80 (5): 1548-1557.
GABAB receptor attenuation of GABAA currents in neurons of the mammalian central nervous system. , Shen W., Physiol Rep. March 1, 2017; 5 (6):
Low Expression in Xenopus Oocytes and Unusual Functional Properties of α1β2γ2 GABAA Receptors with Non-Conventional Subunit Arrangement. , Baur R., PLoS One. January 3, 2017; 12 (1): e0170572.
Ester to amide substitution improves selectivity, efficacy and kinetic behavior of a benzodiazepine positive modulator of GABAA receptors containing the α5 subunit. , Stamenić TT., Eur J Pharmacol. November 15, 2016; 791 433-443.
Functional aspects of early brain development are preserved in tuberous sclerosis complex (TSC) epileptogenic lesions. , Ruffolo G., Neurobiol Dis. November 1, 2016; 95 93-101.
Molecular mode of action of CGS 9895 at α1 β2 γ2 GABAA receptors. , Maldifassi MC., J Neurochem. September 1, 2016; 138 (5): 722-30.
A pharmacological assessment of agonists and modulators at α4β2γ2 and α4β2δ GABAA receptors: The challenge in comparing apples with oranges. , Ahring PK., Pharmacol Res. September 1, 2016; 111 563-576.
Toward Understanding Functional Properties and Subunit Arrangement of α4β2δ γ-Aminobutyric Acid, Type A (GABAA) Receptors. , Wongsamitkul N., J Biol Chem. August 26, 2016; 291 (35): 18474-83.
Zolpidem is a potent stoichiometry-selective modulator of α1β3 GABAA receptors: evidence of a novel benzodiazepine site in the α1-α1 interface. , Che Has AT., Sci Rep. June 27, 2016; 6 28674.
Functional sites involved in modulation of the GABAA receptor channel by the intravenous anesthetics propofol, etomidate and pentobarbital. , Maldifassi MC., Neuropharmacology. June 1, 2016; 105 207-214.
Novel positive allosteric modulators of GABAA receptors with anesthetic activity. , Maldifassi MC., Sci Rep. May 20, 2016; 6 25943.
Potentiating effect of glabridin from Glycyrrhiza glabra on GABAA receptors. , Hoffmann KM., Biochem Biophys Rep. March 31, 2016; 6 197-202.
Pharmacological induction of skin pigmentation unveils the neuroendocrine circuit regulated by light. , Bertolesi GE ., Pigment Cell Melanoma Res. March 1, 2016; 29 (2): 186-98.
Propofol and AZD3043 Inhibit Adult Muscle and Neuronal Nicotinic Acetylcholine Receptors Expressed in Xenopus Oocytes. , Jonsson Fagerlund M., Pharmaceuticals (Basel). February 6, 2016; 9 (1):
A Cysteine Substitution Probes β3H267 Interactions with Propofol and Other Potent Anesthetics in α1β3γ2L γ-Aminobutyric Acid Type A Receptors. , Stern AT., Anesthesiology. January 1, 2016; 124 (1): 89-100.
Structure-dependent inhibition of the human α1β2γ2 GABAA receptor by piperazine derivatives: A novel mode of action. , Hondebrink L., Neurotoxicology. December 1, 2015; 51 1-9.
A novel GABA(A) alpha 5 receptor inhibitor with therapeutic potential. , Ling I., Eur J Pharmacol. October 5, 2015; 764 497-507.