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serotonin [5HT]-6 receptor; 5-hydroxytryptamine receptor 6; 5-HT-6; serotonin receptor 6 (HTR6)

Function: - one of several receptors for 5-hydroxytryptamine (serotonin) - activity is mediated by G proteins that stimulate adenylate cyclase (Gs protein) - high affinity for tricyclic psychotropic drugs - controls pyramidal neurons migration during corticogenesis, through the regulation of CDK5 activity - activator of TOR signaling [3] - interacts with MTOR, RPTOR & NF1 - interacts with CDK5 (putative) Structure: - belongs to the G-protein coupled receptor 1 family Compartment: cell membrane Expression: - expressed in several human brain regions, most prominently in the caudate nucleus Pharmacology: - idalopirdine, a 5HT6 receptor antagonist, failed to slow cognitive decline in patients with Alzheimer's disease [2]

General

phosphoprotein serotonin [5HT] receptor G-protein coupled receptor; serpentine receptor

Properties

SIZE: entity length = 440 aa MW = 47 kD COMPARTMENT: synaptic membrane CELL: neuron MOTIF: exoplasmic domain {1-34} transmembrane domain {35-57} cytoplasmic loop {58-64} transmembrane domain {65-85} exoplasmic loop {86-100} MOTIF: cysteine residue {C99} MODIFICATION: cysteine residue {C180} transmembrane domain {101-122} cytoplasmic loop {123-144} MOTIF: Tyr phosphorylation site {Y125} transmembrane domain {145-166} exoplasmic loop {167-184} MOTIF: cysteine residue {C180} MODIFICATION: cysteine residue {C99} transmembrane domain {185-208} cytoplasmic loop {209-265} transmembrane domain {266-290} exoplasmic loop {291-295} transmembrane domain {296-320} cytoplasmic domain {321-440}

Database Correlations

OMIM 601109 UniProt P50406 Pfam PF00001 Entrez Gene 3362 Kegg hsa:3362

References

  1. UniProt :accession P50406
  2. Fiore K NeuroBreak: Alzheimer's Drug Bombs; Elephant Tranquilizer ODs. MEDPAGE TODAY. Sept 27, 2016 http://www.medpagetoday.com/Neurology/GeneralNeurology/60482
  3. Meffre J, Chaumont-Dubel S, Mannoury la Cour C et al 5-HT(6) receptor recruitment of mTOR as a mechanism for perturbed cognition in schizophrenia. EMBO Mol Med. 2012 Oct;4(10):1043-56 PMID: 23027611 Free PMC Article