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Two genes have been identified that give rise to 5-ht 5a and 5-ht 5b proteins with structures consistent with GPCRs although in humans the 5-ht 5b 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.
Native 5-ht 5a 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 SBA.
Various selective 5-HT 6 receptor antagonists have been described e. SB and selective agonists are becoming available e. Clinical significance A number of non-selective drugs used to treat schizophrenia e. These receptors are selectively expressed in the CNS, but mouse brain has a notably different regional pattern of expression in comparison to humans or rats. Relatively selective 5-HT 6 antagonists induce precognitive effects in animal models, but little data has been generated in clinical populations.
Several splice variants have been described. Pharmacology Various selective 5-HT 7 receptor agonists e. LP, AS [partial agonist] and antagonists e. SB , SBA have been described. Clinical significance Similar to the 5-HT 6 receptor, various non-selective psychotropic drugs also display high affinity for the 5-HT 7 receptor e.
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