The antiepileptic agent gabapentin (Neurontin) possesses anxiolytic-like and antinociceptive actions that are reversed byd -serine Export

@article{citeulike:4758299, abstract = {Abstract\ \ This report describes the activity of the antiepileptic agent gabapentin (Neurontin) in animal models predictive of anxiolysis and analgesia. Gabapentin displayed anxiolytic-like action in the rat conflict test, the mouse light/dark box and the rat elevated X-maze with respective minimum effective doses (MEDs) of 3, 10 and 30 mg/kg. Furthermore, gabapentin also induced behavioural changes suggestive of anxiolysis in the marmoset human threat test with a MED of 30 mg/kg. In the rat formalin test of tonic nociception, gabapentin dose-dependently (30–300 mg/kg) and selectively blocked the late phase with a MED of 100 mg/kg. However, it failed to block carrageenan-induced paw oedema. The intracerebroventricular (ICV) administration of the glycine/NMDA receptor agonistd-Serine, dose-dependently (10–100 μg/animal) reversed the antinociceptive action of gabapentin (200 mg/kg, SC).d-Serine (30 μg/animal, ICV) also reversed the anxiolytic-like effects (in the light/dark box and the rat elevated X-maze) of gabapentin (30 mg/kg). In contrast,l-Serine (100 μg, ICV) failed to block the antinociceptive action of gabapentin. The antinociceptive action of (+)-HA-966 (25 mg/kg, SC), a partial agonist at the glycine/NMDA receptor, was reversed byd-Serine (100 μg/animal, ICV). However,d-Serine (100 μg/animal, ICV) failed to affect the antinociceptive action of a competitive NMDA receptor antagonist CGS 19755 (3 mg/kg, SC). Gabapentin has negligible affinity for the strychnine insensitive [3H]glycine binding site. This indicates that the interaction between gabapentin andd-Serine may not involve the NMDA receptor complex. Gabapentin may represent a novel type of anxiolytic and analgesic agent.}, author = {Singh, L. and Field, M. and Ferris, P. and Hunter, J. and Oles, R. and Williams, R. and Woodruff, G.}, citeulike-article-id = {4758299}, citeulike-linkout-0 = {http://dx.doi.org/10.1007/BF02805968}, citeulike-linkout-1 = {http://www.springerlink.com/content/u2158t8825m70025}, day = {1}, doi = {10.1007/BF02805968}, journal = {Psychopharmacology}, keywords = {gabapentin}, month = {June}, number = {1}, pages = {1--9}, posted-at = {2009-06-06 03:30:57}, priority = {2}, title = {The antiepileptic agent gabapentin (Neurontin) possesses anxiolytic-like and antinociceptive actions that are reversed byd -serine}, url = {http://dx.doi.org/10.1007/BF02805968}, volume = {127}, year = {1996} }

TY - JOUR ID - citeulike:4758299 L3 - citeulike-article-id:4758299 N2 - Abstract  This report describes the activity of the antiepileptic agent gabapentin (Neurontin) in animal models predictive of anxiolysis and analgesia. Gabapentin displayed anxiolytic-like action in the rat conflict test, the mouse light/dark box and the rat elevated X-maze with respective minimum effective doses (MEDs) of 3, 10 and 30 mg/kg. Furthermore, gabapentin also induced behavioural changes suggestive of anxiolysis in the marmoset human threat test with a MED of 30 mg/kg. In the rat formalin test of tonic nociception, gabapentin dose-dependently (30–300 mg/kg) and selectively blocked the late phase with a MED of 100 mg/kg. However, it failed to block carrageenan-induced paw oedema. The intracerebroventricular (ICV) administration of the glycine/NMDA receptor agonistd-Serine, dose-dependently (10–100 μg/animal) reversed the antinociceptive action of gabapentin (200 mg/kg, SC).d-Serine (30 μg/animal, ICV) also reversed the anxiolytic-like effects (in the light/dark box and the rat elevated X-maze) of gabapentin (30 mg/kg). In contrast,l-Serine (100 μg, ICV) failed to block the antinociceptive action of gabapentin. The antinociceptive action of (+)-HA-966 (25 mg/kg, SC), a partial agonist at the glycine/NMDA receptor, was reversed byd-Serine (100 μg/animal, ICV). However,d-Serine (100 μg/animal, ICV) failed to affect the antinociceptive action of a competitive NMDA receptor antagonist CGS 19755 (3 mg/kg, SC). Gabapentin has negligible affinity for the strychnine insensitive [3H]glycine binding site. This indicates that the interaction between gabapentin andd-Serine may not involve the NMDA receptor complex. Gabapentin may represent a novel type of anxiolytic and analgesic agent. IS - 1 JF - Psychopharmacology EP - 9 TI - The antiepileptic agent gabapentin (Neurontin) possesses anxiolytic-like and antinociceptive actions that are reversed byd -serine VL - 127 SP - 1 KW - gabapentin AU - Singh, L AU - Field, M AU - Ferris, P AU - Hunter, J AU - Oles, R AU - Williams, R AU - Woodruff, G PY - 1996/06/01/ UR - http://dx.doi.org/10.1007/BF02805968 ER -