introduction: estradiol is a neuroactive steroid, which is found in several brain areas such as locus coeruleus (lc). estradiol modulates nociception by binding to its receptors and also by allosteric interaction with other membranebound receptors like glutamate and gabaa receptors. lc is involved in noradrenergic descending pain modulation. methods: in order to study the effect of 17β-estradio...

introduction: 17&beta-estradiol; modulates nociception by binding to the estrogenic receptors and also by allosteric interaction with other membrane-bound receptors like glutamate and gabaa receptors. in addition to its autonomic functions, paragigantocellularis lateralis (lpgi) is involved in the pain modulation, too. the aim of the current study was to investigate the involvement of the membr...

BACKGROUND This study tests the hypothesis that loss of spinal activity of gamma-aminobutyric acid (GABA) contributes to the allodynia and hyperalgesia observed after peripheral nerve injury. METHODS Intrathecal catheters were implanted in male Sprague-Dawley rats. Antinociception was assessed by measuring withdrawal latency to immersion of the tail in a 52 degrees C water bath. Nerve injury ...

Background: Estradiol and progesterone as well as hippocampal GABAA receptors are believed to play a role in the modulation of pain. The aim of present study was to investigate the effect of intrahippocampal injections of GABAA receptor agonist (muscimol) and GABAA receptor antagonist (picrotoxin) on pain sensitivity during estrous cycle. Methods: Pain sensitivity was evaluated in rats ...

In the present study the effects of both CCK receptor agonists and antagonists on antinociception induced by morphine in the tail-flick test have been evaluated. M orphine induced dose-dependent antinociception in mice. The response of morphine was potentiated by sulfated cholecystokinin-8 (CCK-8S) but not by unsulfated cholecystokinin-8 (CCK-8U). The CCK receptor antagonists MK-329 and L-...

A mechanism-based pharmacokinetic-pharmacodynamic (PK/PD) model for neuroactive steroids, comprising a separate characterization of 1) the receptor activation process and 2) the stimulus-response relationship, was applied to various nonsteroidal GABAA receptor modulators. The EEG effects of nine prototypical GABAA receptor modulators (six benzodiazepines, one imidazopyridine, one cyclopyrrolone...

background: estradiol and progesterone as well as hippocampal gabaa receptors are believed to play a role in the modulation of pain. the aim of present study was to investigate the effect of intrahippocampal injections of gabaa receptor agonist (muscimol) and gabaa receptor antagonist (picrotoxin) on pain sensitivity during estrous cycle. methods: pain sensitivity was evaluated in rats by forma...

Benzodiazepine site agonists modulate the firing pattern of neurons via GABAA receptors and by that influence the activity of the network in which they participate and cause appropriate changes in behaviour. Since the amygdala is involved in regulating anxiety, it can be expected that GABAA receptors located in this brain region contribute to the anxiolytic effects of benzodiazepine site agonis...

The behavioural effects of several BZ (omega) receptor ligands were compared in mice using the light/dark choice task, an animal model of "state" anxiety, and the free-exploration test, which has been proposed as an experimental model of "trait" anxiety. The drugs used included non-selective full (alprazolam, clorazepate, chlordiazepoxide and diazepam), partial agonists (bretazenil, imidazenil ...

Benzodiazepines (BZDs) exert their effects in the CNS by binding to a modulatory site on GABAA receptors. Individual amino acids have been implicated in BZD recognition and modulation of the GABAA receptor, but the secondary structure of the amino acids contributing to the BZD binding site has not been elucidated. In this report we used the substituted cysteine accessibility method to understan...