5-HT5 Receptors

Overview

Two genes have been identified that give rise to 5-ht5a and 5-ht5b proteins with structures consistent with GPCRs although in humans the 5-ht5b gene is a pseudogene since a stop codon has evolved that would, if expressed, result in a truncated protein devoid of key functional moieties of the receptor. The predicted protein sequences display less than 38% amino acid sequence identity to other 5-HT GPCRs, thus clearly distinguishing the 5-ht5a protein from other 5-HT receptors.5-ht5a is yet to receive receptor status since no robust response signal in native tissue has been described. Native 5-ht5a protein would appear G-protein coupled and recombinant expression allows coupling via various transduction systems including the G-protein mediated inhibition of adenylate cyclase. A selective antagonist based on recombinant protein function has been identified (SB699551-A).
Excerpt from IUPHAR/BPS Guide to Pharmacology
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Human
Available
Assay modes:
Agonist
Inverse agonist
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PAM
NAM
Panels:
Human non-orphan GPCRs
Psychiatry
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Reference agonist:
serotonin
EC50:
85 nM
Mouse
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Assay modes:
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Antagonist
PAM
NAM
Panels:
Mouse non-orphan GPCRs
à la carte
Reference agonist:
serotonin
EC50:
160 nM