5-HT1 receptor

The 5-HT₁ receptors are a subfamily of the 5-HT serotonin receptors that bind to the endogenous neurotransmitter serotonin (also known as 5-hydroxytryptamine, or 5-HT). 5-HT₁ is not a standalone receptor. The 5-HT₁ subfamily consists of five G protein-coupled receptors (GPCRs) that share 40% to 63% overall sequence homology, including 5-HT_1A, 5-HT_1B, 5-HT_1D, 5-HT_1E, and 5-HT_1F. Receptors of the 5-HT₁ type, specifically, the 5-HT_1A and 5-HT_1D receptor subtypes, are present on the cell bodies. Receptors of the 5-HT1 type, specifically, the 5-HT_1B and 5-HT_1D receptor subtypes, are also present on the nerve terminals. These receptors are broadly distributed throughout the brain and are recognized to play a significant part in regulating synaptic levels of 5-HT.

The receptor subfamily is coupled to G_i/G_o and mediates inhibitory neurotransmission by inhibiting the function of adenylate cyclase and modulating downstream ionic effects. This R-coupling to G_i/G_o proteins leads to a reduction in local concentrations of cAMP, proving that 5-HT₁ receptors are primarily inhibitory. There is no 5-HT_1C receptor, as it was reclassified as the 5-HT_2C receptor.

5-HT₁ is one of seven families that make up the complete subtypes of 5-HT serotonin receptors. It is represented by the number 1, and the five subtypes are represented by letters (e.g., a, b, c, d). Unlike other 5-HT subtype receptors, several 5-HT₁ subtypes play a role in pain relief from migraine headaches. The interaction between Serotonin agonists, like Triptans, and these subtypes helps relieve migraine pain There has been and continues to be extensive research on 5-HT₁ and anti-migraine drugs. ÂÂ

For more information, please see the respective main articles of the individual subtypes:

See also

• 5-HT₂ receptor
• 5-HT₃ receptor
• 5-HT₄ receptor
• 5-HT₅ receptor
• 5-HT₆ receptor
• 5-HT₇ receptor

References