High impact information on Htr6

• In the rat and human brain, 5-HT6 receptors are widely expressed and highly enriched in the basal ganglia [1].
• Despite significant sequence homology between human, rat, and mouse 5-HT6 receptors, the pharmacological profile of the mouse receptor was significantly different from the rat and human receptors [1].
• Differences in the central nervous system distribution and pharmacology of the mouse 5-hydroxytryptamine-6 receptor compared with rat and human receptors investigated by radioligand binding, site-directed mutagenesis, and molecular modeling [1].
• In the present study, receptor binding revealed that the pharmacological properties of the mouse receptor are different from the rat and human receptor: Ro 04-6790 does not bind to the mouse 5-HT6 receptor, so all in vivo testing included in the present report was conducted in rats [2].
• The pharmacological profile of this receptor, characterized by both radioligand binding and functional coupling to adenylyl cyclase, does not correspond to that of any of the currently classified subtypes of 5-HT receptor, but is similar to the 5-HT receptor cloned recently from rat striatum and referred to as the 5-HT6 receptor [3].

Biological context of Htr6

• Cloning of the mouse 5-HT6 serotonin receptor and mutagenesis studies of the third cytoplasmic loop [4].
• We examined the ability of 5-HT6 wild type and receptor mutants to activate a cAMP responsive reporter gene when transiently expressed in JEG-3 or COS-7 cells [4].
• We have cloned the mouse 5-HT6 serotonin receptor and examined structure-function relationships in the C-terminal end of the third cytoplasmic (CIII) loop, introducing point mutations by site-directed mutagenesis at positions 264 to 268 [4].

Associations of Htr6 with chemical compounds

• An aspartate residue (Asp-72) in the transmembrane helix II of mouse 5-hydroxytryptamine-6 receptor (5-HT6) is conserved among most G protein-coupled receptors [5].

Analytical, diagnostic and therapeutic context of Htr6

• However, in the mouse brain, only very low levels of 5-HT6 receptor mRNA and receptor protein, measured by TaqMan reverse transcriptase-polymerase chain reaction and selective radioligand binding, could be detected, with no evidence of enrichment in the basal ganglia [1].

References