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Lysergic Acid Diethylamide, more commonly known as LSD, is a potent hallucinogen and is derived from ergotamine, an ergopeptine whose structural skeleton is contained in a diverse range of alkaloids. LSD acts as a non-selective 5-HT receptor agonist, meaning it can bind with equal affinity to two or more sub-types of receptors. LSD actively binds in the orthosteric binding pocket to both the 5-HT1B and 5HT-2B receptors, suggesting a similar chemical structure and function between the two receptor families <ref name = "one" />. The docking is stabilized by hydrogen bonding between the amino group of the 5-membered ring of LSD and the threonine residue of the 5-HT1B receptor, in a similar fashion that 5-HT would bind to said receptor. | Lysergic Acid Diethylamide, more commonly known as LSD, is a potent hallucinogen and is derived from ergotamine, an ergopeptine whose structural skeleton is contained in a diverse range of alkaloids. LSD acts as a non-selective 5-HT receptor agonist, meaning it can bind with equal affinity to two or more sub-types of receptors. LSD actively binds in the orthosteric binding pocket to both the 5-HT1B and 5HT-2B receptors, suggesting a similar chemical structure and function between the two receptor families <ref name = "one" />. The docking is stabilized by hydrogen bonding between the amino group of the 5-membered ring of LSD and the threonine residue of the 5-HT1B receptor, in a similar fashion that 5-HT would bind to said receptor. | ||
==5-HT3 receptor antagonist | ==5-HT3 receptor antagonists== | ||
5-HT3 antagonists have been predominantly used as an antiemetic drug in relieving treating symptoms such as nausea and vomiting for a cancer patient receiving chemotherapy. Three high affinity antagonist often used are granisetron, tropisteron and ondansetron. Experimental homology modeling suggests that 5-HT3 antagonists have aromatic rings that form π-π interactions with the tyrosine and tryptophan side chains of the 5-HT3 receptor. It is also theorized that the antagonist contain carbonyl groups which accept hydrogen bonds from serine side chains of the 5-HT3 receptor.<ref>Maksay G, Zsolt B, Miklós S. ''Binding Interactions of Antagonists with 5‐Hydroxytryptamine 3A Receptor Models.'' Journal of Receptors and Signal Transduction 23.2-3 (2003): 255-70. [http://www.tandfonline.com/doi/full/10.1081/RRS-120025568 DOI:10.1081/RRS-120025568]</ref> 5-HT3 antagonists have a wide variety of uses such as treating nausea, vomiting, irritable bowel syndrome and mood disorders. Once a 5-HT3 antagonist has bound to a 5-HT3 receptor, serotonin binding is inhibited.<ref>Brunton LL, Lazo JS, Parker KL. (2006). Goddman & Gilman's The Pharmacological Basis of Therapeutics. New York: McGraw-Hill. pp. 1000–3. ISBN 978-0-07-142280-2.</ref> | |||
5-HT3 antagonists have a wide variety of uses such as treating nausea, vomiting, irritable bowel syndrome and mood disorders. Once a 5-HT3 antagonist has bound to a 5-HT3 receptor, serotonin binding is inhibited.<ref>Brunton LL, Lazo JS, Parker KL. (2006). Goddman & Gilman's The Pharmacological Basis of Therapeutics. New York: McGraw-Hill. pp. 1000–3. ISBN 978-0-07-142280-2. | |||
==References== | ==References== | ||
