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Zolpidem receptor





Structural determinants for high-affinity zolpidem binding to GABA-A

6/14/2014
01:43 | Author: Kayla Henderson

Zolpidem receptor
Structural determinants for high-affinity zolpidem binding to GABA-A

The imidazopyridine zolpidem (Ambien) is one of the most commonly alpha/gamma subunit interface of the GABA-A receptor (GABAR).

The imidazopyridine zolpidem (Ambien) is one of the most commonly prescribed sleep aids in the United States (Rush, 1998). Similar to classic benzodiazepines (BZDs), zolpidem binds at the extracellular N-terminal alpha/gamma subunit interface of the GABA-A receptor (GABAR). However, zolpidem differs significantly from classic BZDs in chemical structure and neuropharmacological properties. Thus, classic BZDs and zolpidem are likely to have different requirements for high-affinity binding to GABARs.

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Benzodiazepine receptor binding of nonbenzodiazepines in vivo

4/13/2014
01:46 | Author: Emma Coleman

Zolpidem receptor
Benzodiazepine receptor binding of nonbenzodiazepines in vivo

Benzodiazepine receptor binding of nonbenzodiazepines in vivo: alpidem, zolpidem and zopiclone. Byrnes JJ, Greenblatt DJ, Miller LG. Several classes of.

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Several classes of nonbenzodiazepine compounds, including imidazopyridines such as alpidem and zolpidem and cyclopyrrolones, e.g., zopiclone, have effects similar to benzodiazepines and may act at the benzodiazepine receptor in brain. We characterized the binding of these compounds to the benzodiazepine site in three brain regions using specific uptake of the high-affinity ligand Ro15-1788 (flumazenil). For alpidem, benzodiazepine binding was decreased in cortex and hippocampus with increasing drug dose. For zolpidem, receptor binding was reduced in cortex without a dose-response effect and no effect was observed on cerebellar binding. Zopiclone did not alter binding except for a decrease in binding at the lowest dose evaluated and an increase in binding above control at the highest dose. These data corroborate prior studies indicating that the imidazopyridines appear to act at the benzodiazepine receptor, but do not support receptor subtype selectivity of zolpidem. The limited effect of zopiclone except for increased binding at high doses is also consistent with prior studies suggesting that zopiclone acts at a site distinct from the benzodiazepine receptor.

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SLEEP - Association between GABAA Receptor Subunit Gene

12/22/2014
07:31 | Author: Brandon Powell

Zolpidem receptor
SLEEP - Association between GABAA Receptor Subunit Gene

Association between GABAA Receptor Subunit Gene Cluster and Zolpidem-Induced Complex Sleep Behaviors in Han Chinese. http://dx.doi.org/10.5665/sleep.

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The finding reveals that the A15G variant at the GABA A α1 receptor subunit gene confers a high risk of zolpidem-induced CSBs and may be considered in clinical services.

Tsai JH; Yang P; Lin HH; Cheng Kh; Yang YH; Wu MT; Chen CC. Association between GABA A receptor subunit gene cluster and zolpidem-induced complex sleep behaviors in Han Chinese. SLEEP 2013;36(2):197–202.

30 zolpidem-induced CSB subjects and 37 controls. N/A.

You may access and print any article from SLEEP for your personal scholarly, research, and educational use.

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Loss of zolpidem efficacy in the hippocampus of mice with the

10/21/2014
05:12 | Author: Emma Coleman

Zolpidem receptor
Loss of zolpidem efficacy in the hippocampus of mice with the

Zolpidem is a hypnotic benzodiazepine site agonist with some gamma-aminobutyric acid (GABA)(A) receptor subtype selectivity. Here, we have tested the.

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Effect of Zolpidem on Miniature IPSCs and Occupancy of

8/20/2014
03:25 | Author: Kayla Henderson

Zolpidem receptor
Effect of Zolpidem on Miniature IPSCs and Occupancy of

The increase of mIPSC amplitude by zolpidem provides evidence that the GABAA receptors are not saturated during miniature synaptic transmission in the.

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2014 by the Society for Neuroscience. The Journal of Neuroscience is distributed with the assistance of Stanford University's HighWire Press.

GABA A -mediated miniature IPSCs (mIPSCs) were recorded from layer V pyramidal neurons of the visual cortex using whole-cell patch-clamp recording in rat brain slices. At room temperature, the benzodiazepine site agonist zolpidem enhanced both the amplitude (to 138 ± 26% of control value at 10 μ m ) and the duration (163 ± 14%) of mIPSCs. The enhancement of mIPSC amplitude was not caused by an increase of the single-channel conductance of the postsynaptic receptors, as determined by peak-scaled non-stationary fluctuation analysis of mIPSCs. The effect of zolpidem on fast, synaptic-like (1 msec duration) applications of GABA to outside-out patches was also investigated. The EC 50 for fast GABA applications was 310 μ m. In patches, zolpidem enhanced the amplitude of currents elicited by subsaturating GABA applications (100–300 μ m ) but not by saturating applications (10 m m ). The increase of mIPSC amplitude by zolpidem provides evidence that the GABA A receptors are not saturated during miniature synaptic transmission in the recorded cells. By comparing the facilitation induced by 1 μ m zolpidem on outside-out patches and mIPSCs, we estimated the concentration of GABA seen by the postsynaptic GABA A receptors to be ∼300 μ m after single vesicle release. We have estimated a similar degree of receptor occupancy at room and physiological temperature. However, at 35°C, zolpidem did not enhance the amplitude of mIPSCs or of subsaturating GABA applications on patches, implying that, in these neurons, zolpidem cannot be used to probe the degree of receptor occupancy at physiological temperature. What's this? What's this?

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