Samiksha Jaiswal (Editor)

5 HT1D receptor

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Covid-19
Species  Human
Entrez  3352
Human  Mouse
Ensembl  ENSG00000179546
5-HT1D receptor
Aliases  HTR1D, 5-HT1D, HT1DA, HTR1DA, HTRL, RDC4, 5-HT1D receptor, 5-hydroxytryptamine receptor 1D
External IDs  MGI: 96276 HomoloGene: 20240 GeneCards: HTR1D

5-hydroxytryptamine (serotonin) receptor 1D, also known as HTR1D, is a 5-HT receptor, but also denotes the human gene encoding it. 5-HT1D acts on the central nervous system, and affects locomotion and anxiety. It also induces vascular vasoconstriction in the brain.

Contents

Structure

5HT1D receptor is a G protein linked receptor that activates an intracellular messenger cascade to produce an inhibitory response by decreasing cellular levels of cAMP. The 5HT1D is a 7-TM receptor. A large intercellular loop between TM-5 and TM-6 is believed to be associated with coupling to a second messenger. Agonists might bind in a manner that utilizes an aspartate residue in TM-3 and residues in the TM-4, TM-5 and TM-6. A human clone containing an intronless open reading frame was found to encode 377 amino acids of the 5HT1D receptor. The gene has been localized on chromosome 1, region 1p34.3-36.3

Agonists

Molecular modelling has provided a picture of the agonistic binding site of 5HT1D. The amino acid residues within the receptor binding site region have been identified. This is a valuable guide to design potential 5HT1D receptor agonists. When sumatriptan binds there is major conformational change in both ligand and receptor in the binding pocket.

  • 5-(Nonyloxy)tryptamine
  • sumatriptan (vasoconstrictor in migraine)
  • 5-Carboxamidotryptamine (5-CT)
  • 5-(t-Butyl)-N-methyltryptamine
  • CP-135,807
  • CP-286,601
  • PNU-109,291 ((S)-3,4-Dihydro-1-[2-[4-(4-methoxyphenyl)-1-piperazinyl]ethyl]-N-methyl-1H-2-benzopyran-6-carboxamide)
  • PNU-142,633 ((1S)-1-[2-[4-[4-(Aminocarbonyl)phenyl]-1-piperazinyl]ethyl]-3,4-dihydro-N-methyl-1H-2-benzopyran-6-carboxamide)
  • GR-46611 (3-[3-(2-Dimethylaminoethyl)-1H-indol-5-yl]-N-(4-methoxybenzyl)acrylamide)
  • L-694,247 (2-[5-[3-(4-Methylsulfonylamino)benzyl-1,2,4-oxadiazol-5-yl]-1H-indol-3-yl]ethanamine)
  • L-772,405
  • Antagonists

  • Ziprasidone (atypical antipsychotic) [1]
  • methiothepin (antipsychotic)
  • yohimbine (aphrodisiac)
  • metergoline
  • ergotamine (vasoconstrictor in migraine)
  • BRL-15572
  • Vortioxetine (antidepressant)
  • GR-127,935 (mixed 5-HT1B/1D antagonist)
  • LY-310,762
  • LY-367,642
  • LY-456,219
  • LY-456,220
  • References

    5-HT1D receptor Wikipedia


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