5-HT5A receptor
Protein-coding gene in the species Homo sapiens
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Function
The gene described in this record is a member of 5-hydroxytryptamine receptor family and encodes a multi-pass membrane protein that functions as a receptor for 5-hydroxytryptamine and couples to G proteins, negatively influencing cAMP levels via Gi and Go. This protein has been shown to function in part through the regulation of intracellular Ca2+ mobilization. The 5-HT5A receptor has been shown to be functional in a native expression system.
Rodents have been shown to possess two functional 5-HT5 receptor subtypes, 5-HT5A and 5-HT5B, however while humans possess a gene coding for the 5-HT5B subtype, its coding sequence is interrupted by stop codons, making the gene non-functional, and so only the 5-HT5A subtype is expressed in human brain.
It also appears to serve as a presynaptic serotonin autoreceptor.
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Clinical significance
The neurotransmitter serotonin (5-hydroxytryptamine, 5-HT) has been implicated in a wide range of psychiatric conditions and also has vasoconstrictive and vasodilatory effects.
Selective ligands
Few highly selective ligands are commercially available for the 5-HT5A receptor, though the field has expanded considerably in recent years. When selective activation of this receptor is desired in scientific research, the non-selective serotonin receptor agonist 5-Carboxamidotryptamine can be used in conjunction with selective antagonists for its other targets (principally 5-HT1A, 5-HT1B, 5-HT1D, and 5-HT7). Research in this area is ongoing.
Agonists
- LSD:(+)-lysergic acid.
- Lisuride – partial agonist.
- 5-CT – full agonist.
- Methylergometrine – full agonist.
- Valerenic acid – a component of valerian, has been shown to act as a 5HT5A partial agonist.
- Olanzapine – an atypical antipsychotic.
- Psilocin
- Aripiprazole - an atypical antipsychotic
- UCSF648 - selective 5-HT5A partial agonist
- Another ligand that has been recently disclosed is shown below, claimed be a selective 5-HT5A agonist with Ki = 124 nM.
Antagonists
- ASP5736
- AS-2030680
- AS-2674723
- MS112 – selective potent antangonist.
- Latrepirdine (non-selective).
- Risperidone – (non-selective), moderate 206 nM affinity.
- SB-699,551