@entity1024 ( @entity143 ) is an agonist at the homonymous receptor implicated in the development of neuronal sensitization and its behavioral correlates. An effective modulation of the @entity143 effects, achieved also by uncompetitive antagonists, could contribute to controlling @entity158 symptoms in several @entity1109 . Because nefopam is a known analgesic derivative of @entity18362 and of its congener @entity3933 , both uncompetitive @entity143 receptor antagonists, we tested the effect of nefopam on the developing @entity158 and @entity528 in an animal model of @entity1118 with @entity143 receptor involvement. A single intraperitoneal injection of nefopam was administered twenty minutes prior to the chronic @entity1930 (CCI @entity35 ). In the first 10 days, @entity15845 (30 mg/kg) significantly decreased behavioral signs of @entity9 and the stimulus-evoked electrophysiological anomalies in recordings at 14 days, with only slight manifestation afterwards. The dose of 20 mg/kg was ineffective. @entity15845 injected after constriction was ineffective. In normal non-operated @entity35 , Nefopam had no effect on the electrophysiological and behavioral parameters. Iontophoretic nefopam (1 mM, 50-80 nA, positive current) in normal @entity35 did not change the spontaneous neuronal activity, but reduced the mean response to noxious stimuli and the concurrent iontophoretic @entity143 evoked activity. In CCI @entity35 , iontophoretic nefopam did not significantly modify the spontaneous @entity2915 but reduced significantly both the frequency of the responses to noxious stimuli, and the duration of the afterdischarge. We propose that nefopam exerts a preventive analgesic effect, with a possible role in modulating @entity143 receptor-mediated effects in central sensitization.

Neuronal sensitization and its behavioral correlates in a XXXX model of neuropathy are prevented by a cyclic analog of @entity18362 .

@entity3933 :: ('MESH:D004155', 'Chemical') :: ['diphenhydramine'] @entity1024 :: ('CHEBI:31882', 'Chemical') :: ['N-methyl-D-aspartic acid'] @entity35 :: ('10116', 'Species') :: ['rats'] @entity1109 :: ('MESH:D012678', 'Disease') :: ['neuropathic syndromes'] @entity15845 :: ('MESH:D009340', 'Chemical') :: ['Nefopam', 'nefopam'] @entity2915 :: ('MESH:D006948', 'Disease') :: ['hyperactivity'] @entity143 :: ('CHEBI:6121', 'Chemical') :: ['NMDA'] @entity158 :: ('MESH:D010146', 'Disease') :: ['pain'] @entity9 :: ('MESH:D009437', 'Disease') :: ['neuropathic pain'] @entity1930 :: ('MESH:D020426', 'Disease') :: ['constriction injury of the sciatic nerve'] @entity528 :: ('MESH:D009410', 'Disease') :: ['neuronal anomalies'] @entity1118 :: ('MESH:D059350', 'Disease') :: ['chronic pain'] @entity18362 :: ('MESH:D009966', 'Chemical') :: ['orphenadrine']
@entity35 :: (10116,Species) :: ['rat']
