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5-HT2c receptor agonist
Serotonin 5-HT2 receptors are stimulated by monoaminergic neurotransmitters including serotonin, dopamine and norepinephrine. 5-HT2 receptor stimulation causes a buildup of intracellular inositol triphosphate and thereby an increase of cytosolic Ca2+. 5-HT2C receptor agonists are attractive drug targets that have potential use in the treatment of a number of conditions including obesity, psychiatric disorders, sexual dysfunction and urinary incontinence.
The 5-HT2C receptors are one of three subtypes that belong to the serotonin 5-HT2 receptor subfamily along with 5-HT2A and 5-HT2B receptors. The development of 5-HT2C agonists has been a major obstacle, because of severe side effects due to a lack of selectivity over 5-HT2A and 5-HT2B receptors. Activation of 5-HT2A receptors can induce hallucinations, and the activation of 5-HT2B receptors has been implicated in cardiac valvular insufficiency and possibly in pulmonary hypertension.
== Discovery ==
In the late 1960s, non-selective serotonin receptor antagonists demonstrated a relationship between serotonin receptors and food intake. Later, animal studies showed that serotonin receptor agonists might act as a mediator of satiety. Serotonin has been implicated as a critical factor in the short-term regulation of food intake and in promoting loss of weight associated with hyperphagia. The 5-HT2C receptor subtype was shown to be one of the principal mediators through which serotonin exert its anorectic effects in rodents by using pharmacological and genetic tools. Subsequently these receptors became a promising pharmacotherapeutic target for further investigation for the treatment of obesity. The development of 5-HT2C receptor knock-out mice in the mid-1990s was a hallmark achievement in the identification and development of serotonergic drugs for weight loss. These knock-out mice were hyperphagic which led to obesity, partial leptin resistance, increased adipose deposition, insulin resistance and impaired glucose tolerance. Therefore, the researchers found a functional role for the receptors in serotonergic regulation of food intake and body weight.〔 Later on research showed that 5-HT2C receptors have been proposed as a therapeutic target for the treatment of multiple central nervous system (CNS) disorders including; psychiatric disorders, obesity, sexual dysfunction and urinary incontinence.〔
抄文引用元・出典: フリー百科事典『 ウィキペディア（Wikipedia）』
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