SB-699,551
Encyclopedia
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.
Serotonin
Serotonin or 5-hydroxytryptamine is a monoamine neurotransmitter. Biochemically derived from tryptophan, serotonin is primarily found in the gastrointestinal tract, platelets, and in the central nervous system of animals including humans...
receptor 5-HT5A
5-HT5A receptor
5-hydroxytryptamine receptor 5A, also known as HTR5A, is a protein which in humans is encoded by the HTR5A gene.- Function :...
, 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
5-HT1B receptor
5-hydroxytryptamine receptor 1B also known as the 5-HT1B receptor is a protein that in humans is encoded by the HTR1B gene. The 5-HT1B receptor is a 5-HT receptor subtype.-Tissue distribution and function:...
and 5-HT1D
5-HT1D receptor
5-hydroxytryptamine receptor 1D, also known as HTR1D, is a 5-HT receptor, but also denotes the human gene encoding it. 5-HT1D acts on the central nervous system, and affects locomotion and anxiety...
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.