Abstract
The effect of loperamide on cholinergic neurotransmission in canine bronchial smooth muscle was studied under isometric conditions in-vitro. Addition of loperamide decreased contractile responses to electrical field stimulation in a dose-dependent fashion, the maximal decrease from the control response and the IC50 value being 65.4 +/- 5.9% and 1.5 microM, respectively. In contrast, loperamide was without effect on the responses to exogenously administered acetylcholine. The inhibitory effect of loperamide was not altered by pre-incubation of tissues with propanol, 6-hydroxydopamine, bicuculline, or naloxone. These results suggest that loperamide attenuates the neurally mediated airway contraction probably by inhibiting acetylcholine release from cholinergic nerve terminals through a non-opioid-dependent mechanism.
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