The Inhibitory Effects of Tramadol on Muscarinic Receptor-Induced Responses in Xenopus Oocytes Expressing Cloned M3 Receptors

@article{Shiga2002TheIE,
  title={The Inhibitory Effects of Tramadol on Muscarinic Receptor-Induced Responses in Xenopus Oocytes Expressing Cloned M3 Receptors},
  author={Yousuke Shiga and Kouichiro Minami and Munehiro Shiraishi and Yasuhito Uezono and Osamu Murasaki and Muneshige Kaibara and Akio Shigematsu},
  journal={Anesthesia \& Analgesia},
  year={2002},
  volume={95},
  pages={1269-1273}
}
Tramadol is a widely used analgesic, but its mechanism of action is not completely understood. Muscarinic receptors are 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. In this study, we investigated the effects of tramadol on type-3 muscarinic (M3) receptors using the Xenopus oocyte expression system. Tramadol (10 nM–100 &mgr;M) inhibited acetylcholine… 
The Effects of the Tramadol Metabolite O-Desmethyl Tramadol on Muscarinic Receptor-Induced Responses in Xenopus Oocytes Expressing Cloned M1 or M3 Receptors
TLDR
O-desmethyl tramadol inhibits functions of M1 receptors but has little effect on those of M3 receptors, which may help to explain its neural function.
The Inhibitory Effects of Alphaxalone on M1 and M3 Muscarinic Receptors Expressed in Xenopus Oocytes
TLDR
It is suggested that alphaxalone at clinically relevant concentrations inhibits the function of M1 and M3 receptors through a protein kinase C-independent mechanism by interfering with the [3H]quinuclidinyl benzilate binding sites on the receptors.
The Inhibitory Effects of Tramadol on 5-Hydroxytryptamine Type 2C Receptors Expressed in Xenopus Oocytes
TLDR
The results suggest that tramadol inhibits 5-HT2CR function, and the mechanism of this inhibitory effect seems to involve competitive displacement of the5-HT binding to the 5- HT2CR, rather than via activation of the PKC pathway.
µ-Opioid receptor activation by tramadol and O-desmethyltramadol (M1)
TLDR
The effects of tramadol and its main active metabolite O-desmethyltramadol (M1), on the function of µ ORs using Xenopus oocytes expressing cloned human µORs are examined.
Pharmacological aspects of the effects of tramadol on G-protein coupled receptors.
TLDR
The effects of tramadol on monoamine transporters, GPCRs, and ion channels are presented, and recent research on the pharmacology of tramadol is discussed.
Dexmedetomidine inhibits muscarinic type 3 receptors expressed in Xenopus oocytes and muscarine-induced intracellular Ca2+ elevation in cultured rat dorsal root ganglia cells
TLDR
Examination of the effects of dexmedetomidine on M1, M3, 5-HT2C, substance P, and orexin 1 receptors in Xenopus oocytes expressing individual receptors shows that the compound inhibits the function of M3 receptors, in addition to its agonistic effects on α2-adrenoceptors, which provides further insight into the pharmacological properties.
The Tramadol Metabolite, O-Desmethyl Tramadol, Inhibits 5-Hydroxytryptamine Type 2C Receptors Expressed in Xenopus Oocytes
TLDR
O-desmethyl tramadol inhibits 5-HT2CR, a G-protein-coupled receptor that is expressed widely within brain and that mediates several effects of5-HT, including nociception, feeding, and locomotion, which provides further insight into the pharmacological properties of tramadols.
The effects of the neurosteroids: pregnenolone, progesterone and dehydroepiandrosterone on muscarinic receptor-induced responses in Xenopus oocytes expressing M1 and M3 receptors
TLDR
Investigation of the effects of pregnenolone, progesterone, and DHEA on M1 and M3 muscarinic receptors using the Xenopus oocyte expression system found that pregnanolone and progestersone inhibited M1and M3 receptor functions noncompetitively by the mechanism independent of PKC and by interfering with ACh binding to the receptors.
The Inhibitory Effects of Ketamine and Pentobarbital on Substance P Receptors Expressed in Xenopus Oocytes
TLDR
The results suggest that ketamine and pentobarbital inhibit SPR function, and the mechanism of their inhibition on SPR function could not be through activation of the PKC pathway and may be due to noncompetitive displacing the SP binding.
Tramadol and Its Metabolite M1 Selectively Suppress Transient Receptor Potential Ankyrin 1 Activity, but Not Transient Receptor Potential Vanilloid 1 Activity
TLDR
Data indicate that tramadol and M1 selectively inhibit the function of h TRPA1, but not that of hTRPV1, and that hTRPA1 may play a role in the analgesic effects of these compounds.
...
...

References

SHOWING 1-10 OF 26 REFERENCES
Inhibition by tramadol of muscarinic receptor-induced responses in cultured adrenal medullary cells and in Xenopus laevis oocytes expressing cloned M1 receptors.
TLDR
It is suggested that tramadol at clinically relevant concentrations inhibits muscarinic receptor function via QNB-binding sites, which may explain the neuronal function and anticholinergic effect of tramadol.
Halothane Inhibits Signaling through m1 Muscarinic Receptors Expressed in Xenopus Oocytes
Background Interactions between volatile anesthetics and muscarinic acetylcholine receptors have been studied primarily in binding assays or in functional systems derived from tissues or cells, often
Tramadol Inhibits Norepinephrine Transporter Function at Desipramine-Binding Sites in Cultured Bovine Adrenal Medullary Cells
TLDR
Findings indicate that tramadol competitively inhibits norepinephrine transporter (NET) function at desipramine-binding sites through competition for the NET through competitive inhibition.
Inhibitory effects of anesthetics and ethanol on muscarinic receptors expressed in Xenopus oocytes.
The Effects of Isoflurane on Native and Chimeric Muscarinic Acetylcholine Receptors: The Role of Protein Kinase C
TLDR
The results suggest that isoflurane inhibits m3 and chimeric m1/m3 muscarinic signaling by enhancing PKC activity and that the site of action is located outside of the third intracellular loop.
Characterization of Muscarinic Receptor Subtypes That Mediate Antinociception in the Rat Spinal Cord
TLDR
Using selective receptor antagonists, it is shown that the antinociceptive effects of intrathecally administered muscarinic agonists and a cholinesterase inhibitor are likely mediated by spinal M1 and/or M3 receptor subtypes.
Inhibition by Ketamine of Muscarinic Acetylcholine Receptor Function
TLDR
Ketamine profoundly inhibits muscarinic signaling, which might explain some of the anticholinergic clinical effects of ketamine, both central and peripheral (prominent sympathetic tone, bronchodilation, mydriasis).
Inhibition of 5-hydroxytryptamine type 2A receptor-induced currents by n-alcohols and anesthetics.
TLDR
It is reported that ethanol inhibited (IC50 = 41 mM) 5-HT2A receptor-induced Ca2+-dependent Cl- currents in Xenopus laevis oocytes, and the protein kinase C inhibitor GF109203X and the nonspecificprotein kinase inhibitor staurosporine abolished the inhibitory effects of ethanol and octanol on 5- HT2A receptors.
Receptor binding, analgesic and antitussive potency of tramadol and other selected opioids.
The influence of replacing the phenolic hydroxyl by the methoxy group on opioid receptor binding, analgesic and antitussive action was investigated in the corresponding couples morphine-codeine,
...
...