SB-699,551 is a drug which was the first compound developed to act as a selective antagonist for the serotonin receptor 5-HT5A, with selectivity of around 100x over other serotonin receptor subtypes. The function of the 5-HT5A receptor remains poorly defined, but SB-699,551 was found to modulate serotonin release from neurons, suggesting it acts as a presynaptic inhibitory autoreceptor similar to the 5-HT1B and 5-HT1D receptors. Multiple therapeutic roles have been suggested for 5-HT5A ligands due to the presence of this receptor in several areas of the brain, but research is still at an early stage.
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