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Vol. 299, Issue 1, 255-260, October 2001
Department of Anesthesiology, University of Occupational and
Environmental Health, School of Medicine, Kitakyushu, Japan (M.S.,
K.M., A.S.); Department of Second Pharmacology, Nagasaki University,
School of Medicine, Nagasaki, Japan (Y.U.); and Department of
Pharmacology, University of Occupational and Environmental Health,
School of Medicine, Kitakyushu, Japan (N.Y.)
Tramadol is a widely used, centrally acting analgesic, but its
mechanisms of action are not completely understood. Muscarinic receptors are known to be involved in neuronal function in the brain
and autonomic nervous system, and much attention has been paid to these
receptors as targets of analgesic drugs in the central nervous system.
This study investigated the effects of tramadol on muscarinic receptors
by using two different systems, i.e., a Xenopus
laevis oocyte expression system and cultured bovine adrenal medullary cells. Tramadol (10 nM-100 µM) inhibited
acetylcholine-induced currents in oocytes expressing the M1
receptor. Although GF109203X, a protein kinase C inhibitor, increased
the basal current, it had little effect on the inhibition of
acetylcholine-induced currents by tramadol. On the other hand, tramadol
did not inhibit the current induced by AlF4
,
a direct activator of GTP-binding protein. In cultured bovine adrenal
medullary cells, tramadol (100 nM-100 µM) suppressed
muscarine-induced cyclic GMP accumulation. Moreover, tramadol inhibited
the specific binding of [3H]quinuclidinyl benzilate
(QNB). Scatchard analysis showed that tramadol increases the apparent
dissociation constant (Kd) value without
changing the maximal binding (Bmax),
indicating competitive inhibition. These findings suggest that tramadol
at clinically relevant concentrations inhibits muscarinic receptor
function via QNB-binding sites. This may explain the neuronal function and anticholinergic effect of tramadol.
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