INT16268
From wiki-pain
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Sentences Mentioned In
Key: | Protein | Mutation | Event | Anatomy | Negation | Speculation | Pain term | Disease term |
Ligands of various chemical classes (e.g., indoles, indazoles, benzamides, carbazoles, and quinolines) have demonstrated high affinity for the 5-HT3 receptor in radiolabeled ligand-binding studies, and have shown 5-HT3 receptor antagonistic activity in functional assays which utilize the excitatory effects of 5-HT on enteric neurons and autonomic afferents. | |||||||||||||||
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The most important neurotransmitters in CINV are serotonin, dopamine, and substance P, which bind to 5HT3, dopamine-2, and NK-1 receptors, respectively.19,20 Another way of emesis activation may be the direct stimulation of CTZ by metabolites of chemotherapy or intestinal peptides circulating in the blood. | |||||||||||||||
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These drugs selectively and competitively bind to 5-HT3 receptors, blocking serotonin binding at vagal afferents in the gut and in the regions of the central nervous system involved in emesis, including the chemoreceptor trigger zone and the nucleus tractus solitarii [28,29]. | |||||||||||||||
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Oral tramadol has been shown to have the same analgesic efficacy as oral diclofenac for post-tonsillectomy pain in patients 11 years and older, without the side effects of NSAIDs.29 It is important to note that the use of ondansetron to treat PONV results in the inhibition of tramadol analgesia probably due to a reduction of binding to the 5-HT3 receptors at the spinal level.30 Tramadol is currently available in a tablet form alone or in combination with acetaminophen in the USA. | |||||||||||||||
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In view of the 5-HT releasing effects of selective 5-HT3 receptor agonists to which metformin (N-N-dimethylbiguanide) is structurally related, we investigated whether metformin directly interacts with 5-HT3 receptors. | |||||||||||||||
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The effect of drugs interacting with serotonergic 5HT3 and 5HT4 receptors on morphine place conditioning. | |||||||||||||||
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However, the recent discovery of additional 5-HT3 subunits and the dawning realization that central and peripheral 5-HT3 receptor populations might comprise several subtypes characterized by distinct functional properties has emphasized the complexity of human 5-HT3 receptor signaling. | |||||||||||||||
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Palonosetron has proven to be an excellent addition to the armamentarium against CINV, specifically against delayed and overall CINV, which until now has proved difficult to treat with conventional 5-HT3 RAs. | |||||||||||||||
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Because local anesthetics have different clinical properties, we have tested the hypothesis that differences in interactions at the 5-HT3 receptor may be clinically relevant by investigating the effects of 4 local anesthetics on recombinant wild-type and 4 mutant 5-HT3A receptors. | |||||||||||||||
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Clinical differences between local anesthetics may be at least partially due to differences in interactions at the 5-HT3A receptor.
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Do variations in the 5-HT3A and 5-HT3B serotonin receptor genes (HTR3A and HTR3B) influence the occurrence of postoperative vomiting? | |||||||||||||||
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The 5-HT3 receptor antagonist ondansetron, first heralded by Lancet in 1987, was rapidly recognized as having broad applicability with significant benefits (Anonymous 1987). | |||||||||||||||
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In conclusion, the ArgPro variation of the h5-HT3A receptor does not change ligand binding to the h5-HT3A receptor, nor does it modify current through the receptor channel. | |||||||||||||||
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In conclusion, the ArgPro variation of the h5-HT3A receptor does not change ligand binding to the h5-HT3A receptor, nor does it modify current through the receptor channel. | |||||||||||||||
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Ligands of various chemical classes (e.g., indoles, indazoles, benzamides, carbazoles, and quinolines) have demonstrated high affinity for the 5-HT3 receptor in radiolabeled ligand-binding studies, and have shown 5-HT3 receptor antagonistic activity in functional assays which utilize the excitatory effects of 5-HT on enteric neurons and autonomic afferents. | |||||||||||||||
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It binds equipotently and with the greatest affinity to 5HT2C and 5HT3 receptor subtypes, and to a lesser extent to 5HT1A and 5HT1D receptors (Gross et al 1998; McDougle 1999). | |||||||||||||||
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General Comments
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