The Antinociceptive Effect of SNAP5114, a Gamma-Aminobutyric Acid Transporter-3 Inhibitor, in Rat Experimental Pain Models

2013 ◽  
Vol 116 (5) ◽  
pp. 1162-1169 ◽  
Author(s):  
Kazunori Kataoka ◽  
Koji Hara ◽  
Yasunori Haranishi ◽  
Tadanori Terada ◽  
Takeyoshi Sata
Keyword(s):  
Antinociceptive Effect ◽  
Experimental Pain ◽  
Aminobutyric Acid ◽  
Gamma Aminobutyric Acid ◽  
Pain Models ◽  
Acid Transporter

scholarly journals Comparison of antinociceptive effect of the antiepileptic drug gabapentin to that of various dosage combinations of gabapentin with lamotrigine and topiramate in mice and rats

2011 ◽  
Vol 02 (02) ◽  
pp. 130-136 ◽  
Author(s):  
Keshab Raj Paudel ◽  
SK Bhattacharya ◽  
GP Rauniar ◽  
BP Das
Keyword(s):  
Pain Perception ◽  
Late Phase ◽  
Antinociceptive Effect ◽  
Experimental Pain ◽  
Mechanical Hyperalgesia ◽  
Tail Flick ◽  
Hot Plate ◽  
Analgesic Effects ◽  
Pain Models ◽  
Antinociceptive Effects

ABSTRACT Introduction: Newer anticonvulsants have a neuromodulatory effect on pain perception mechanisms in a hyperexcitable and damaged nervous system. Aim: This study was designed to study the analgesic effects of gabapentin alone and in combination with lamotrigine and topiramate in experimental pain models. Materials and Methods: Adult albino mice (n = 490) weighing 20–30 g and rats (n = 130) weighing 100–200 g were injected intraperitoneally with gabapentin, lamotrigine, and topiramate alone and in different dose combinations. The hot-plate method, tail-flick method, capsaicin-induced mechanical hyperalgesia, and formalin assay were used to assess the antinociceptive effects. Results: Of the three antiepileptic drugs, when given separately, gabapentin was more efficacious than either topiramate or lamotrigine in all the pain models. Combination of 25 mg/kg gabapentin with 25 mg/kg topiramate was more efficacious (P <.05) than 50 mg/kg gabapentin alone in the capsaicin-induced mechanical hyperalgesia test. Similarly, 50 mg/kg gabapentin with 50 mg/kg topiramate or 5 mg/kg lamotrigine was more efficacious (P <.05) than 50 or 100 mg/kg gabapentin alone in late-phase formalin-induced behaviors. Conclusions: Combination of gabapentin with either lamotrigine or topiramate produced better results than gabapentin alone in capsaicin-induced mechanical hyperalgesia test and in late-phase formalin-induced behaviors.

scholarly journals A gamma-aminobutyric acid transporter driven by a proton pump is present in synaptic-like microvesicles of pancreatic beta cells.

1993 ◽  
Vol 90 (11) ◽  
pp. 5317-5321 ◽  
Author(s):  
A. Thomas-Reetz ◽  
J. W. Hell ◽  
M. J. During ◽  
C. Walch-Solimena ◽  
R. Jahn ◽  
...  
Keyword(s):  
Beta Cells ◽  
Proton Pump ◽  
Pancreatic Beta Cells ◽  
Aminobutyric Acid ◽  
Gamma Aminobutyric Acid ◽  
Acid Transporter

Brain Stem Opioidergic and GABAergic Neurons Mediate the Antinociceptive Effect of Nitrous Oxide in Fischer Rats

2003 ◽  
Vol 99 (4) ◽  
pp. 947-954 ◽  
Author(s):  
Yoko Ohashi ◽  
Tianzhi Guo ◽  
Ryo Orii ◽  
Mervyn Maze ◽  
Masahiko Fujinaga
Keyword(s):  
Spinal Cord ◽  
Brain Stem ◽  
Antinociceptive Effect ◽  
Opioid Peptide ◽  
Periaqueductal Gray ◽  
Gabaergic Neurons ◽  
Aminobutyric Acid ◽  
Gamma Aminobutyric Acid ◽  
Gray Area ◽  
Fos Expression

Background Recent studies have revealed that N2O exerts its antinociceptive effect by inducing opioid peptide release in the brain stem, thereby activating the descending noradrenergic inhibitory neurons, which modulate pain processing in the spinal cord. However, the precise neuronal pathways that mediate these events remain to be determined. Methods Using immunohistochemical and behavioral techniques in adult male Fischer rats, the authors studied the involvement of brain stem opioidergic and gamma-aminobutyric acid-mediated (GABAergic) neurons in the N2O-induced antinociceptive effect using discrete microinjections of an opioid receptor antagonist or GABAergic activator into the periaqueductal gray area and pontine noradrenergic nuclei. They used c-Fos expression as an immunohistochemical mark of neuronal activation induced by N2O and the plantar test as the behavioral paradigm for nociception. Results Microinjection of either naloxone (an opioid receptor antagonist) or muscimol (a gamma-aminobutyric acid receptor type A agonist) into the ventrolateral periaqueductal gray area inhibited N2O-induced c-Fos expression in the spinal cord and pontine noradrenergic nuclei, particularly in the A7. Microinjection of either naloxone or muscimol into the A7 nuclei also inhibited N2O-induced c-Fos expression in the spinal cord and the N2O-induced antinociceptive effect by the plantar test. Conclusions These results support the hypothesis that both opioidergic and GABAergic neurons mediate the antinociceptive effect of N2O at the periaqueductal gray area and A7 in the brain stem. The authors postulate that N2O-induced opioid peptide release leads to inhibition of GABAergic neurons via opioid receptors. The descending noradrenergic inhibitory pathways, which are tonically inhibited by these gamma-aminobutyric acid neurons, are thereby activated (disinhibited) and modulate pain processing in the spinal cord.

A functional reconstitution of the .gamma.-aminobutyric acid transporter from synaptic vesicles using artificial ion gradients

Biochemistry ◽  
1991 ◽  
Vol 30 (51) ◽  
pp. 11795-11800 ◽  
Author(s):  
Johannes W. Hell ◽  
Lambert Edelmann ◽  
Joachim Hartinger ◽  
Reinhard Jahn
Keyword(s):  
Synaptic Vesicles ◽  
Aminobutyric Acid ◽  
Gamma Aminobutyric Acid ◽  
Ion Gradients ◽  
Acid Transporter

scholarly journals Insights into binding events of GABA- and Tiagabine- analogues in the Gamma-Aminobutyric Acid Transporter 1 by means of Molecular Modelling

2012 ◽  
Vol 4 (S1) ◽  
Author(s):  
Barbara Zdrazil ◽  
Andreas Jurik ◽  
Regina Reicherstorfer ◽  
Thomas Stockner ◽  
Harald H Sitte ◽  
...  
Keyword(s):  
Molecular Modelling ◽  
Aminobutyric Acid ◽  
Gamma Aminobutyric Acid ◽  
Acid Transporter
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