Abstract:
:The involvement of brain monoamines in the mechanism of action of nefopam, a new analgesic, was investigated in rats. The study was designed to evaluate the effect of various means of impairing monoaminergic transmission on nefopam analgesia as measured with the hot plate method. Pretreatment with reserpine (2 mg/kg) significantly reduced the antinociceptive action of nefopam (40 mg/kg), indicating that the interaction of this drug with the monoaminergic systems is important for its effects. A role for serotonin (5-HT) or norepinephrine (NE) was ruled out by the fact that selective depletion of 5-HT (using 5,7-dihydroxytryptamine) or NE (using DSP-4 or FLA-63) did not affect nefopam analgesia. A significant reduction of the effect of nefopam was found in rats pretreated with 6-hydroxydopamine (6-OHDA). Also 6-OHDA plus desipramine, which selectively depleted brain DA, markedly reduced the antinociceptive effect of nefopam. The data strongly suggest that a critical dopaminergic synapse is involved in the mechanism by which nefopam inhibits nociceptive responses in rats.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Esposito E,Romandini S,Merlo-Pich E,Mennini T,Samanin Rdoi
10.1016/0014-2999(86)90762-4subject
Has Abstractpub_date
1986-09-09 00:00:00pages
157-64issue
3eissn
0014-2999issn
1879-0712pii
0014-2999(86)90762-4journal_volume
128pub_type
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