5-HT7

links: GPCR reference: 9-19-2021

5-HT7 #

Gs-coupled.

• Expressed in the brain, the highest densities in the Thalamus and Hypothalamus, and high densities on the hippocampus and cortex.
  • Involved in thermoregulation, circadian rhythm, learning, memory, and sleep.
  • Antagonism boosts reference memory and performance in demanding tasks (boosts cortical glutaminergic transmission)
• Increases Glucocorticoid receptors. Expressed in the GI tract, playing a role in smoth muscle contraction.
• Implication of 5-HT7 receptor in prefrontal circuit assembly and detrimental emotional effects of SSRIs during development
  • 5-HTR7 over-expression in the developing PFC, results in depressive-like symptoms in adulthood
  • long-term depressive-like and anxiogenic effects of SSRIs (postnatal administration of fluoxetine from P2 to P14) were not observed in 5-HTR7-KO mice
• Pharmacological Blockade of 5-HT7 Receptors as a Putative Fast Acting Antidepressant Strategy
  • Negatively regulate the firing of Dorsal Raphe Nucleus serotonin neurons and become desensitized after long-term Fluoxetine>
• Pharmacological Blockade of Serotonin 5-HT7 Receptor Reverses Working Memory Deficits in Rats by Normalizing Cortical Glutamate Neurotransmission
  • Mice lacking 5-HT7: impaired contextual fear conditioning but no significant deficits in motor and spatial learning or cued and operant conditioning
  • might reverse cognitive deficits associated with NMDA receptor hypofunction by selectively normalizing glutamatergic neurotransmission.