INT65009
From wiki-pain
|
|
|
|
|
Sentences Mentioned In
Key: | Protein | Mutation | Event | Anatomy | Negation | Speculation | Pain term | Disease term |
Effects of tramadol and O-demethyl-tramadol on human 5-HT reuptake carriers and human 5-HT3A receptors: a possible mechanism for tramadol-induced early emesis.
([3H]5-HT)-uptake and patch-clamp techniques were used to study the actions of (+) and (-) tramadol and the active metabolites of tramadol, (+) and (-) O-demethyl-tramadol on the human serotonin (5-HT) transporter and the human 5-HT3A receptor, stably expressed in HEK-293 cells. | |||||||||||||||
| |||||||||||||||
|
Finally, coexpression of wild-type 5-HT3A or 5-HT3B subunits with 5-HT3A variants A33T, S253N, or M257I resulted in mixed or heteromeric receptors, characterized by significantly reduced maximal responses to 5-HT compared with the wild-type receptors. | |||||||||||||||
| |||||||||||||||
|
The 5-hydroxytryptamine 3 (5-HT3) receptor is expressed widely in the central and peripheral nervous systems, where it mediates or modulates a wide range of physiological processes. | |||||||||||||||
| |||||||||||||||
|
Our data show that 5-HT3A receptors are widely expressed in cells of the immune system and that they might play an important role in inflammatory events and in the observed antiphlogistic effects of 5-HT3 receptor antagonists. | |||||||||||||||
| |||||||||||||||
|
Expression of 5-HT3A receptors in cells of the immune system. | |||||||||||||||
| |||||||||||||||
|
We found that 5-HT3A receptors are expressed in monocytes, chondrocytes, T-cells, and synovial tissue but not in dendritic cells. | |||||||||||||||
| |||||||||||||||
|
Therefore, we investigated the expression of the 5-HT3A receptor in primary human monocytes, chondrocytes, T-cells, dendritic cells, and synovial tissue. | |||||||||||||||
| |||||||||||||||
|
Receptor binding (inhibition of [3H]-GR65630 binding) and agonist effects (stimulation of [14C]-guanidinium influx) at 5-HT3 receptors were studied in murine neuroblastoma N1E-115 cells, which express functional 5-HT3 receptors. | |||||||||||||||
| |||||||||||||||
|
Enkephalinergic neurons express 5-HT3 receptors in the spinal cord dorsal horn: single cell RT-PCR analysis. | |||||||||||||||
| |||||||||||||||
|
However, that at least some airway-specific neurons express 5-HT3 receptors is supported by electrophysiologic studies [4] that showed that 10 out of 12 neurons that were retrogradely labeled by fluorescent dye injection into guinea pig airways depolarized an average of over 8 mV in response to 10 ? | |||||||||||||||
| |||||||||||||||
|
This prompted us to examine whether enkephalinergic dorsal horn neurons express 5-HT3 receptors. | |||||||||||||||
| |||||||||||||||
|
Naturally occurring variations in the human 5-HT3A gene profoundly impact 5-HT3 receptor function and expression. | |||||||||||||||
| |||||||||||||||
|
Radioligand-binding studies with the 5-HT3 receptor antagonist [H]GR65630 were carried out to determine expression levels of heteromeric 5-HT3A/B receptors. | |||||||||||||||
| |||||||||||||||
|
These targets were subsequently classified in the 5-HT1, 5-HT2, and 5-HT3 families using specific and distinguishing agonism and especially antagonism by drugs like Bemestron and Tropisetron (for the 5-HT3 family). | |||||||||||||||
| |||||||||||||||
|
The variant p.V183I decreased surface expression, whereas p.Y129S and p.S156R led to pronounced increases of 5-HT maximum responses, despite nearly unaltered surface expression levels of heteromeric 5-HT3A/B receptors. | |||||||||||||||
| |||||||||||||||
|
Do variations in the 5-HT3A and 5-HT3B serotonin receptor genes (HTR3A and HTR3B) influence the occurrence of postoperative vomiting? | |||||||||||||||
| |||||||||||||||
|
Whole-cell patches from HEK-293 cells stably transfected with the human 5-HT3A receptor cDNA were used to determine the effects of morphine on the 5-HT-induced currents using the patch clamp technique. | |||||||||||||||
| |||||||||||||||
|
Quantitative autoradiography with selective radioligands was used to establish the respective distribution of serotonin 5-HT1A, 5-HT1D, 5-HT2A and 5-HT3 receptors at the cervical, thoracic and lumbar levels of the spinal cord from subjects who died at 81-94 years. | |||||||||||||||
| |||||||||||||||
|
To further investigate the mechanisms underlying the noncompetitive inhibition of the serotonin-evoked cation current, we quantified the concentrations of different types of antidepressants and antipsychotics in fractions of sucrose flotation gradients isolated from HEK293 (human embryonic kidney 293) cells stably transfected with the 5-HT3A receptor and of N1E-115 neuroblastoma cells in relation to the localization of the 5-HT3 receptor protein within the cell membrane. | |||||||||||||||
| |||||||||||||||
|
[Prevention of postoperative nausea and vomiting with highly selective 5-HT3 serotonin receptors antagonists during different types of surgery]. | |||||||||||||||
| |||||||||||||||
|
General Comments
This test has worked.