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Granisetron is a serotonin 5-HT 3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy and radiotherapy. Its main effect is to reduce the activity of the vagus nerve, which is a nerve that activates the vomiting center in the medulla oblongata. It does not have much effect on vomiting due to motion sickness.
The 5-HT 3 receptor antagonists suppress vomiting and nausea by inhibiting serotonin binding to the 5-HT 3 receptors. The highest concentration of 5-HT 3 receptors in the central nervous system are found in the STN and chemoreceptor trigger zone (CTZ), and 5-HT 3 antagonists may also suppress vomiting and nausea by acting at these sites. [29]
Cyproheptadine blocks 5-HT 2A, H1 and is a mild anticholinergic. Methysergide is a 5-HT 2A antagonist and nonselective 5-HT 1 receptor blocker. It causes retroperitoneal fibrosis and mediastinal fibrosis. [citation needed] Quetiapine blocks 5-HT 2A, 5-HT 1A, dopamine receptors D 1 and D 2, histamine receptor H1, and A1 adrenoreceptors.
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DOI is a serotonin 5-HT 2A, 5-HT 2B and 5-HT 2C receptor agonist. [4] It is said to be approximately 5- to 12-fold selective for the serotonin 5-HT 2A receptor over the serotonin 5-HT 2C receptor. [7] The drug is not a monoamine releasing agent of serotonin or dopamine. [8] DOI is an agonist of the rat trace amine-associated receptor 1 (TAAR1). [9]
This is a list of agonists of the serotonin receptor subtype 5-HT 2A (and other 5-HT 2 subtypes to a varying extent) which fall outside the common structural classes. Most agonists at this receptor are either substituted phenethylamine derivatives from the 2C, DOx and 25-NB groups, or substituted tryptamines and related compounds along with more complex derivatives of these such as ...
The drug is a silent antagonist of the serotonin 5-HT 1B receptor, unlike the related agent GR-127935. [ 1 ] [ 4 ] GR-55562 has around 10-fold selectivity for the serotonin 5-HT 1B receptor over the serotonin 5-HT 1D receptor and has only weak affinity for a number of other serotonin receptors .
The 5-HT 3C, 5-HT 3D and 5-HT 3E genes tend to show peripherally restricted pattern of expression, with high levels in the gut. In human duodenum and stomach, for example, 5-HT 3C and 5-HT 3E mRNA might be greater than for 5-HT 3A and 5-HT 3B. Polymorphism.