N. J. Tresnak-Rustad, M. Wood
Oct 15, 1981
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Influential Citations
37
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Quality indicators
Journal
Biochemical pharmacology
Abstract
Abstract Nefopam hydrochloride (Acupan), an analgesic in laboratory animals and man, was a very weak inhibitor of [3H]naloxone binding ( ic 50 25 μM) to brain homogenates, in comparison to other analgesic agents. On the other hand, nefopam was a potent inhibitor of synaptosomal uptake of dopamine, norepinephrine, and serotonin, with ic 50 values of 0.47, 0.89, and 0.34 μM respectively. The mechanism of analgesic action by nefopam probably is not related to direct actions on opiate receptors but may be related to an enhancement of monoaminergic function by uptake inhibition.