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Sulfated and unsulfated steroids modulate γ-aminobutyric acidA receptor function through distinct sites
Sulfated and unsulfated neurosteroids such as pregnenolone sulfate, dehydroepiandrosterone sulfate (DHEAS), pregnanolone, and allopregnanolone, modulate ionotropic amino acid neurotransmitterExpand
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From ion currents to genomic analysis: Recent advances in GABAA receptor research
The γ‐aminobutyric acid type A (GABAA) receptor represents an elementary switching mechanism integral to the functioning of the central nervous system and a locus for the action of many mood‐andExpand
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Pregnenolone sulfate: a positive allosteric modulator at the N-methyl-D-aspartate receptor.
The N-methyl-D-aspartate (NMDA) receptor is believed to play a major role in learning and in excitotoxic neuronal damage associated with stroke and epilepsy. Pregnenolone sulfate, a neurosteroid,Expand
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Distinct sites for inverse modulation of N-methyl-D-aspartate receptors by sulfated steroids.
Steroid sulfation occurs in nervous tissue and endogenous sulfated steroids can act as positive or negative modulators of N-methyl-D-aspartate (NMDA) receptor function. In the current study,Expand
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Inhibition of the NMDA response by pregnenolone sulphate reveals subtype selective modulation of NMDA receptors by sulphated steroids
The neurosteroid pregnenolone sulphate (PS) potentiates N‐methyl‐D‐aspartate (NMDA) receptor mediated responses in various neuronal preparations. The NR1 subunit can combine with NR2A, NR2B, NR2C, orExpand
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Selective anxiolysis produced by ocinaplon, a GABA(A) receptor modulator.
Benzodiazepines remain widely used for the treatment of anxiety disorders despite prominent, often limiting side effects including sedation, muscle relaxation, and ataxia. A compound producing aExpand
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Negative modulation of the gamma-aminobutyric acid response by extracellular zinc.
We have studied the effects of divalent cations on the gamma-aminobutyric acid (GABA) response of voltage-clamped spinal cord neurons, using the whole-cell recording configuration. Zn, Cd, Ni, and MnExpand
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A steroid modulatory domain on NR2B controls N-methyl-D-aspartate receptor proton sensitivity.
N-methyl-D-aspartate (NMDA) receptor function is modulated by several endogenous molecules, including zinc, polyamines, protons, and sulfated neurosteroids. Zinc, polyamines, and phenylethanolaminesExpand
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Benzodiazepine modulation of partial agonist efficacy and spontaneously active GABAA receptors supports an allosteric model of modulation
1 Benzodiazepines (BZDs) have been used extensively for more than 40 years because of their high therapeutic index and low toxicity. Although BZDs are understood to act primarily as allostericExpand
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Molecular Identification of the Human GABABR2: Cell Surface Expression and Coupling to Adenylyl Cyclase in the Absence of GABABR1
We have identified a gene encoding a GABAB receptor, the human GABABR2, located on chromosome 9q22.1, that is distinct from the recently reported rat GABABR1. GABABR2 structurally resembles GABABR1Expand
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