Serotonin 5-HT6 receptor

Masellis M, Basils VS, Meltzer HY, Lieberman JA, Sevy S, Goldman DA et al. Lack of association between the T to C 267 serotonin 5-HT6 receptor gene (HTR6) polymorphism and prediction of response to clozapine in schizophrenia. Schizophr Res 2001 47(1) 49—58. 

Ruat M, Traiffort E, Arrang JM, et al. A novel rat serotonin (5-HT6) receptor molecular cloning, localization and stimulation of cAMP accumulation. Biochem Biophys Res Commun 1993 193 268-276. 

Boess FG, Monsma FJ Jr, Sleight AJ, Launay JM. Identification of residues in transmembrane regions III and VI that contribute to the ligand binding site of the serotonin 5-HT6 receptor. J Neurochem 1998 71 2169-2177. 

Russell MG, Baker RJ, Barden L, et al. Y-Atylsuironylindolc derivatives as serotonin 5-HT6 receptor ligands. J Med Chem 2001 44 3881-3895. 

Russell MG, Dias R. Memories are made of this (perhaps) a review of serotonin 5-HT6 receptor ligands and their biological functions. Curr Topics Med Chem 2002 2 643-654. 

Gerard C, el Mestikawy S, Lebrand C, et al. Quantitative RT-PCR distribution of serotonin 5-HT6 receptor mRNA in the central nervous system of control or 5, 7-dihydroxytryptamine-treatedrats. Synapse 1996 23 164-173. 

Gerard C, Martres MP, Lefevre K, et al. Immuno-localization of serotonin 5-HT6 receptor-like material in the rat central nervous system. Brain Res 1997 746 207-219. 

Purohit A, Herrick-Davis K, Teitler M. Creation, expression, and characterization of a constitutively active mutant of the human serotonin 5-HT6 receptor. Synapse 2003 47 218-224. 

Inhibitors of dopamine D2L receptor, serotonin 5-HT2A receptor, serotonin 5-HT6 receptor, adrenaline alD receptor [85]... 

The serotonin 6 (5-HT6) receptor is one of the most recently studied serotonin receptors, and an important candidate gene for the study of MDD because it is abundant in the limbic system and some antidepressants have a high affinity for it (Monsma, Shen, Ward etal, 1993). 

Fig. 7. Schematic representation of the interaction of simple tiyptamines, such as serotonin, and Nj-substituted tryptamines, such as benzenesulfonyltryptamines where X = S02, with receptor features as identified using automated docking studies and a graphics model of the human 5-HT6 receptors. Although both types of ligand might utilize the aspartate moiety of TM3, they seem to be oriented in different sterically accessible pockets. (Adapted from ref. 96.)...

Lindner MD, Hodges DB Jr, Hogan JB, et al. An assessment of the effects of serotonin 6 (5-HT6) receptor antagonists in rodent models of learning. J Pharmacol Exp Ther 2003 307 682-691. 

Vogt IR, Shimron-Ababanell D, Neidt H, et al. Investigation of the human serotonin 6 (5-HT6) receptor gene in bipolar affective disorder and schizophrenia, Am J Med Genet 2000 96 217-221. 

All three compounds have relatively high affinity to serotonin 5-HT2B receptors, and clozapine and olanzapine also have remarkable affinity to 5-HT6 and 5-HT7 receptors, but almost nothing is known of the role of these interactions either in the antipsychotic action or in the side effects. 

Enterochromaffin cells are interspersed with mucosal cells mainly in the stomach and small intestine. In the blood, serotonin is present at high concentrations in platelets, which take up serotonin from the plasma by an active transport process. Serotonin is released on platelet activation. In the central nervous system, serotonin serves as a transmitter. The main serotonin-containing neurons are those clustered in form of the Raphe nuclei. Serotonin exerts its biological effects through the activation of specific receptors. Most of them are G-protein coupled receptors (GPCRs) and belong to the 5-HTr, 5-HT2-, 5-HT4-, 5-HTs-, 5-HT6-, 5-HT7-receptor subfamilies. The 5-HT3-receptor is a ligand-operated ion channel. 

Kohen, R., Metcalf, M. A., Khan, N. etal. (1996). Cloning, characterization and chromosomal localization of a human 5-HT6 serotonin receptor. /. Neurochem., 66, 47-56. 

Three families of serotonin receptor, the 5-HT family, the 5-HT2 family and the family that includes the 5-HT4, 5-ht6 and 5-HT7 receptors represent the three major classes of 5-HT receptor that are G-protein-coupled receptors (Ch. 19). The 5-HT3 receptor is a ligand-gated ion channel and is a separate family. Although each serotonin receptor can be potently activated by 5-HT, differences insignal transduction mechanisms,neuroanatomical distribution and affinities for synthetic chemicals create opportunities for drug discovery and make each 5-HT receptor subtype a potential therapeutic target. 

Histamine H3 antagonists 5-HT3 receptor agonist 5-HTlA receptor agonist 5-HT6 antagonist Serotonin stimulant FK-960 Fujisawa... 

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