Erowid References Database
Shih JC, Chen K, Gallaher TK.
“Structure and Function of Serotonin 5-HT2 Receptors”.
NIDA Research Monograph. 1994 Oct;146:284-296.
One of at least seven known subtypes of serotonin (5-hydroxytryptamine [5-HT2]) receptors is the 5-HT2 receptor. The molecular cloning of these subtypes has unequivocally defined receptor subtypes and confirmed the existence of 5-HT receptor subtypes found by earlier pharmacological, biochemical, and physiological studies. The 5-HT2 receptors are integral membrane proteins that elicit a cellular response to serotonin in conjunction with a guanosine triphosphate binding protein (G-protein) and an effector enzyme (Shih et al. 1991). The 5-HT2 receptors are known to activate the inositol triphosphate (IP3)/diacylglycerol second messenger system via enzymatic cleavage of polyphosphoinositol by phospholipase C, which ultimately results in increased calcium ion levels in the cell (Conn and Sanders-Bush 1986; Pritchett et al. 1988).
The 5-HT2 receptors are found in the brain cortical regions and may be involved in depression and suicide (Meltzer and Lowy 1987; Sternbach 1991). In addition, 5-HT2 receptors are targets for hallucinogenic drugs that also implicate 5-HT2 receptors as being important in mental health (Glennon, this volume; Pierce and Peroutka 1989; Sadzot et al. 1989). Outside the brain, 5-HT2 receptors are found in platelets and smooth muscle tissue and play a role in blood pressure and in hypertension (Vanhoutte 1982). The 5-HT2 receptors are of great interest for their multifaceted actions in the body and the importance of their function for mental and physical health.
This chapter presents the background of the research leading up to the identification and cloning of 5-HT2 receptors and the current molecular knowledge of the 5-HT2 receptor, with an emphasis on the structure and functions of these receptors.
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