The Inhibitory Effects of Tramadol on 5-Hydroxytryptamine Type 2C Receptors Expressed in Xenopus Oocytes

@article{Ogata2004TheIE,
  title={The Inhibitory Effects of Tramadol on 5-Hydroxytryptamine Type 2C Receptors Expressed in Xenopus Oocytes},
  author={Junichi Ogata and Kouichiro Minami and Yasuhito Uezono and Takashi Okamoto and Munehiro Shiraishi and Akio Shigematsu and Yoichi Ueta},
  journal={Anesthesia \& Analgesia},
  year={2004},
  volume={98},
  pages={1401-1406}
}
Although tramadol is widely available as an analgesic, its mechanism of antinociception remains unresolved. Serotonin (5-hydroxytryptamine, 5-HT) is a monoaminergic neurotransmitter that modulates numerous sensory, motor, and behavioral processes. The 5-HT type 2C receptor (5-HT2CR) is one of the major 5-HT receptor subtypes and is implicated in many important effects of 5-HT, including pain, feeding, and locomotion. In this study, we used a whole-cell voltage clamp to examine the effects of… 

Figures from this paper

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.
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.
The tramadol metabolite O-desmethyl tramadol inhibits substance P-receptor functions expressed in Xenopus oocytes.
TLDR
The results suggest that the tramadol metabolite ODT inhibits the SPR functions, which may be independent of activation of PKC-mediated pathways.
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.
The Analgesic Drug, Tramadol, Acts as an Agonist of the Transient Receptor Potential Vanilloid-1
TLDR
The findings of this study strongly support the intriguing and novel concept that tramadol acts as an agonist of TRPV1.
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.
Inhibition of L-type calcium current by tramadol and enantiomers in cardiac myocytes from rats.
TLDR
The inhibition of ICa-L induced by tramadol and its enantiomers was unrelated to the activation of opioid receptors and could explain, at least in part, their negative cardiac inotropic effect.
Role of atypical opiates in OCD. Experimental approach through the study of 5-HT2A/C receptor-mediated behavior
TLDR
Behavioral evidence is provided to support convergent effects of the 5-HT and opioid systems in discrete brain areas, offering the potential for therapeutic advances in the management of refractory stereotypes and compulsive behaviors.
...
...

References

SHOWING 1-10 OF 31 REFERENCES
The Inhibitory Effects of Tramadol on Muscarinic Receptor-Induced Responses in Xenopus Oocytes Expressing Cloned M3 Receptors
TLDR
It is suggested that tramadol at clinically relevant concentrations inhibits M3 function via quinuclidinyl benzilate-binding sites, which may explain the modulation of neuronal function and the anticholinergic effects of tramadols.
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.
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.
Effect of acute and chronic tramadol on [3H]‐5‐HT uptake in rat cortical synaptosomes
TLDR
The lack of tolerance development of [3H]‐5‐HT uptake, together with the absence of behavioural alterations after chronic tramadol treatment, suggest that tramadols has an advantage over classical opioids in the treatment of pain disorders.
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.
The antinociceptive effect of tramadol in the formalin test is mediated by the serotonergic component.
Pharmacological antagonism of the antinociceptive effects of serotonin in the rat spinal cord.
Inhibitory effects of anesthetics and ethanol on muscarinic receptors expressed in Xenopus oocytes.
...
...