PHARMACOLOGY Lecture Notes - Lecture 1: G Protein–Coupled Receptor, Tricyclic Antidepressant, 5-Ht3 Receptor

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Serotonin was the name given to the vasoconstrictor substance which appeared in serum when blood clotted, and was shown to be 5- hydroxytryptamine (5-ht). About 90% of body"s content of 5-ht is localized in the intestines; most of the rest is in platelets and brain. 5-ht is synthesized from the amino acid tryptophan and degraded primarily by mao and to a small extent by a dehydrogenase . Like na, 5-ht is actively taken up by an amine pump serotonin transporter (sert) which operates at the membrane of platelets (therefore, 5-ht does not circulate in free form in plasma) and serotonergic nerve endings. Again, like cas, 5-ht is stored within storage vesicles and its uptake at the vesicular membrane is inhibited by reserpine. Four families of 5-ht receptors (5-ht1 , 5-ht2 , 5-ht3 , 5-ht4-7) comprising of 14 receptor subtypes have so far been recognized. However, only some of these have been functionally correlated or their selective agonists/ antagonists defined.

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