Published in Anesthesiology on December 01, 2011
Etomidate produces similar allosteric modulation in α1β3δ and α1β3γ2L GABA(A) receptors. Br J Pharmacol (2014) 0.83
Caenorhabditis elegans neuromuscular junction: GABA receptors and ivermectin action. PLoS One (2014) 0.79
Modulation of the human ρ1 GABAA receptor by inhibitory steroids. Psychopharmacology (Berl) (2013) 0.76
Mutational Analysis at Intersubunit Interfaces of an Anionic Glutamate Receptor Reveals a Key Interaction Important for Channel Gating by Ivermectin. Front Mol Neurosci (2017) 0.75
Trapping of ivermectin by a pentameric ligand-gated ion channel upon open-to-closed isomerization. Sci Rep (2017) 0.75
Direct physical measure of conformational rearrangement underlying potassium channel gating. Science (1996) 6.31
General anaesthesia: from molecular targets to neuronal pathways of sleep and arousal. Nat Rev Neurosci (2008) 6.05
Substituted-cysteine accessibility method. Methods Enzymol (1998) 5.57
Sequence and functional expression of the GABA A receptor shows a ligand-gated receptor super-family. Nature (1987) 5.12
Endogenous neurosteroids regulate GABAA receptors through two discrete transmembrane sites. Nature (2006) 4.33
Recent advances in Cys-loop receptor structure and function. Nature (2006) 4.20
Nicotinic receptors at the amino acid level. Annu Rev Pharmacol Toxicol (2000) 4.04
GABA A receptors: subtypes provide diversity of function and pharmacology. Neuropharmacology (2008) 3.49
Identification of a GABAA receptor anesthetic binding site at subunit interfaces by photolabeling with an etomidate analog. J Neurosci (2006) 3.42
Electrostatic potential of the acetylcholine binding sites in the nicotinic receptor probed by reactions of binding-site cysteines with charged methanethiosulfonates. Biochemistry (1994) 3.02
The benzodiazepine binding site of GABAA receptors. Trends Pharmacol Sci (1997) 2.26
Reactivity of small thiolate anions and cysteine-25 in papain toward methyl methanethiosulfonate. Biochemistry (1986) 2.20
An open-channel blocker interacts with adjacent turns of alpha-helices in the nicotinic acetylcholine receptor. Neuron (1990) 2.06
GABAA receptor subunit gamma2 and delta subtypes confer unique kinetic properties on recombinant GABAA receptor currents in mouse fibroblasts. J Physiol (1999) 2.02
Evidence for a common binding cavity for three general anesthetics within the GABAA receptor. J Neurosci (2001) 2.00
Identification of channel-lining residues in the M2 membrane-spanning segment of the GABA(A) receptor alpha1 subunit. J Gen Physiol (1996) 1.85
The actions of propofol on inhibitory amino acid receptors of bovine adrenomedullary chromaffin cells and rodent central neurones. Br J Pharmacol (1991) 1.81
Dependence of the GABAA receptor gating kinetics on the alpha-subunit isoform: implications for structure-function relations and synaptic transmission. J Physiol (1995) 1.64
Interaction of picrotoxin with GABAA receptor channel-lining residues probed in cysteine mutants. Biophys J (1995) 1.56
Clinical and molecular pharmacology of etomidate. Anesthesiology (2011) 1.55
Benzodiazepine and beta-carboline regulation of single GABAA receptor channels of mouse spinal neurones in culture. J Physiol (1994) 1.50
Benzodiazepines act on GABAA receptors via two distinct and separable mechanisms. Nat Neurosci (2000) 1.49
Neuroactive steroids have multiple actions to potentiate GABAA receptors. J Physiol (2004) 1.47
Multiple mechanisms of picrotoxin block of GABA-induced currents in rat hippocampal neurons. J Physiol (1993) 1.39
A fluorophore attached to nicotinic acetylcholine receptor beta M2 detects productive binding of agonist to the alpha delta site. Proc Natl Acad Sci U S A (2004) 1.34
Site-specific fluorescence reveals distinct structural changes with GABA receptor activation and antagonism. Nat Neurosci (2002) 1.31
Conformational variability of the glycine receptor M2 domain in response to activation by different agonists. J Biol Chem (2007) 1.31
A single hydrophobic residue confers barbiturate sensitivity to gamma-aminobutyric acid type C receptor. Mol Pharmacol (1999) 1.26
Effect of the alpha subunit subtype on the macroscopic kinetic properties of recombinant GABA(A) receptors. Brain Res (2007) 1.24
Agonist-, antagonist-, and benzodiazepine-induced structural changes in the alpha1 Met113-Leu132 region of the GABAA receptor. Mol Pharmacol (2006) 1.24
Structural domains of the human GABAA receptor 3 subunit involved in the actions of pentobarbital. J Physiol (2000) 1.23
GABA(A) receptor beta 2 Tyr97 and Leu99 line the GABA-binding site. Insights into mechanisms of agonist and antagonist actions. J Biol Chem (2001) 1.23
Distinct deactivation and desensitization kinetics of recombinant GABAA receptors. Neuropharmacology (1996) 1.21
Activation and block of recombinant GABA(A) receptors by pentobarbitone: a single-channel study. Br J Pharmacol (2000) 1.19
Biophysical and pharmacological properties of cloned GABAA receptor subunits expressed in Xenopus oocytes. Neuron (1988) 1.18
Local and global ligand-induced changes in the structure of the GABA(A) receptor. Biochemistry (2006) 1.14
GABA(A) receptor subtypes underlying general anesthesia. Pharmacol Biochem Behav (2008) 1.13
Ligand-specific conformational changes in the alpha1 glycine receptor ligand-binding domain. J Biol Chem (2009) 1.08
Distinct structural changes in the GABAA receptor elicited by pentobarbital and GABA. Biophys J (2009) 1.07
Structural rearrangements in loop F of the GABA receptor signal ligand binding, not channel activation. Biophys J (2009) 1.03
Structural elements involved in activation of the gamma-aminobutyric acid type A (GABAA) receptor. Biochem Soc Trans (2004) 1.03
Gamma-aminobutyric acid (GABA) and pentobarbital induce different conformational rearrangements in the GABA A receptor alpha1 and beta2 pre-M1 regions. J Biol Chem (2008) 1.02
Chemical modification of the active site of the acetylcholine receptor. J Gen Physiol (1969) 1.00
Neuroactive steroids and human recombinant rho1 GABAC receptors. J Pharmacol Exp Ther (2007) 1.00
Agonist- and competitive antagonist-induced movement of loop 5 on the alpha subunit of the neuronal alpha4beta4 nicotinic acetylcholine receptor. J Neurochem (2007) 0.97
Channel opening by anesthetics and GABA induces similar changes in the GABAA receptor M2 segment. Biophys J (2007) 0.97
GABA(A) receptor function and pharmacology in epilepsy and status epilepticus. Curr Opin Pharmacol (2003) 0.97
Agonist- and antagonist-induced conformational changes of loop F and their contributions to the rho1 GABA receptor function. J Physiol (2008) 0.96
Augmentation of GABA-induced current in frog sensory neurons by pentobarbital. Am J Physiol (1990) 0.93
Kinetic and structural determinants for GABA-A receptor potentiation by neuroactive steroids. Curr Neuropharmacol (2010) 0.90
Ligand- and subunit-specific conformational changes in the ligand-binding domain and the TM2-TM3 linker of {alpha}1 {beta}2 {gamma}2 GABAA receptors. J Biol Chem (2010) 0.90
Site-specific fluorescence reveals distinct structural changes induced in the human rho 1 GABA receptor by inhibitory neurosteroids. Mol Pharmacol (2010) 0.84
Pharmacology of structural changes at the GABA(A) receptor transmitter binding site. Br J Pharmacol (2011) 0.83
Context dependent benzodiazepine modulation of GABA(A) receptor opening frequency. Curr Neuropharmacol (2010) 0.79
Neurosteroid access to the GABAA receptor. J Neurosci (2005) 1.95
Mechanisms of neurosteroid interactions with GABA(A) receptors. Pharmacol Ther (2007) 1.60
Neuroactive steroids have multiple actions to potentiate GABAA receptors. J Physiol (2004) 1.47
Mutations of the GABA-A receptor alpha1 subunit M1 domain reveal unexpected complexity for modulation by neuroactive steroids. Mol Pharmacol (2008) 1.46
Nicotine is highly effective at producing desensitization of rat alpha4beta2 neuronal nicotinic receptors. J Physiol (2003) 1.38
Natural and enantiomeric etiocholanolone interact with distinct sites on the rat alpha1beta2gamma2L GABAA receptor. Mol Pharmacol (2007) 1.33
Dual potentiating and inhibitory actions of a benz[e]indene neurosteroid analog on recombinant alpha1beta2gamma2 GABAA receptors. Mol Pharmacol (2006) 1.31
3beta -hydroxypregnane steroids are pregnenolone sulfate-like GABA(A) receptor antagonists. J Neurosci (2002) 1.18
Activation of GABA(A) receptors containing the alpha4 subunit by GABA and pentobarbital. J Physiol (2004) 1.18
Rare missense variants in CHRNB4 are associated with reduced risk of nicotine dependence. Hum Mol Genet (2011) 1.08
Neurosteroid migration to intracellular compartments reduces steroid concentration in the membrane and diminishes GABA-A receptor potentiation. J Physiol (2007) 1.07
Neurosteroid analog photolabeling of a site in the third transmembrane domain of the β3 subunit of the GABA(A) receptor. Mol Pharmacol (2012) 1.05
Steroid interaction with a single potentiating site is sufficient to modulate GABA-A receptor function. Mol Pharmacol (2009) 1.04
Anticonvulsant and anesthetic effects of a fluorescent neurosteroid analog activated by visible light. Nat Neurosci (2007) 1.03
The cholinergic antagonist alpha-bungarotoxin also binds and blocks a subset of GABA receptors. Proc Natl Acad Sci U S A (2006) 1.02
Neuroactive steroids and human recombinant rho1 GABAC receptors. J Pharmacol Exp Ther (2007) 1.00
Activation and block of mouse muscle-type nicotinic receptors by tetraethylammonium. J Physiol (2003) 1.00
Galantamine activates muscle-type nicotinic acetylcholine receptors without binding to the acetylcholine-binding site. J Neurosci (2005) 0.96
Activation and modulation of concatemeric GABA-A receptors expressed in human embryonic kidney cells. Mol Pharmacol (2009) 0.95
Functional characterization of the α5(Asn398) variant associated with risk for nicotine dependence in the α3β4α5 nicotinic receptor. Mol Pharmacol (2011) 0.95
Cytisine binds with similar affinity to nicotinic alpha4beta2 receptors on the cell surface and in homogenates. Brain Res (2003) 0.94
A portable site: a binding element for 17β-estradiol can be placed on any subunit of a nicotinic α4β2 receptor. J Neurosci (2011) 0.94
Multiple modes for conferring surface expression of homomeric beta1 GABAA receptors. J Biol Chem (2008) 0.93
Hydrogen bonding between the 17beta-substituent of a neurosteroid and the GABA(A) receptor is not obligatory for channel potentiation. Br J Pharmacol (2009) 0.93
Role of the agonist binding site in up-regulation of neuronal nicotinic alpha4beta2 receptors. Mol Pharmacol (2006) 0.93
Ethanol modulates the interaction of the endogenous neurosteroid allopregnanolone with the alpha1beta2gamma2L GABAA receptor. Mol Pharmacol (2006) 0.92
Enantiomers of neuroactive steroids support a specific interaction with the GABA-C receptor as the mechanism of steroid action. Mol Pharmacol (2006) 0.92
Characteristics of concatemeric GABA(A) receptors containing α4/δ subunits expressed in Xenopus oocytes. Br J Pharmacol (2012) 0.92
The influence of the membrane on neurosteroid actions at GABA(A) receptors. Psychoneuroendocrinology (2009) 0.91
Kinetic and structural determinants for GABA-A receptor potentiation by neuroactive steroids. Curr Neuropharmacol (2010) 0.90
Low doses of ethanol and a neuroactive steroid positively interact to modulate rat GABA(A) receptor function. J Physiol (2003) 0.89
The nicotinic α5 subunit can replace either an acetylcholine-binding or nonbinding subunit in the α4β2* neuronal nicotinic receptor. Mol Pharmacol (2013) 0.88
Kinetic analysis of voltage-dependent potentiation and block of the glycine alpha 3 receptor by a neuroactive steroid analogue. J Physiol (2009) 0.88
A synthetic 18-norsteroid distinguishes between two neuroactive steroid binding sites on GABAA receptors. J Pharmacol Exp Ther (2010) 0.87
Occupation of either site for the neurosteroid allopregnanolone potentiates the opening of the GABAA receptor induced from either transmitter binding site. Mol Pharmacol (2011) 0.86
Activation and block of the adult muscle-type nicotinic receptor by physostigmine: single-channel studies. Mol Pharmacol (2008) 0.85
Photoaffinity labeling the agonist binding domain of alpha4beta4 and alpha4beta2 neuronal nicotinic acetylcholine receptors with [(125)I]epibatidine and 5[(125)I]A-85380. Biochim Biophys Acta (2009) 0.85
Cis-regulatory variants affect CHRNA5 mRNA expression in populations of African and European ancestry. PLoS One (2013) 0.85
Site-specific fluorescence reveals distinct structural changes induced in the human rho 1 GABA receptor by inhibitory neurosteroids. Mol Pharmacol (2010) 0.84
Common polymorphisms in FMO1 are associated with nicotine dependence. Pharmacogenet Genomics (2011) 0.84
Pharmacology of structural changes at the GABA(A) receptor transmitter binding site. Br J Pharmacol (2011) 0.83
The benzodiazepine diazepam potentiates responses of α1β2γ2L γ-aminobutyric acid type A receptors activated by either γ-aminobutyric acid or allosteric agonists. Anesthesiology (2013) 0.82
A neurosteroid potentiation site can be moved among GABAA receptor subunits. J Physiol (2012) 0.80
Energetic contributions to channel gating of residues in the muscle nicotinic receptor β1 subunit. PLoS One (2013) 0.78
Agonist-specific conformational changes in the α1-γ2 subunit interface of the GABA A receptor. Mol Pharmacol (2012) 0.76
Inhibition of muscle acetylcholine receptors by nondepolarizing drugs: humans are not unique. Anesthesiology (2010) 0.75
Pharmacology: Unready for action. Nature (2008) 0.75
Multiple Non-Equivalent Interfaces Mediate Direct Activation of GABAA Receptors by Propofol. Curr Neuropharmacol (2016) 0.75