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5-HT1D receptor

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HTR1D
Identifiers
Aliases HTR1D, 5-HT1D, HT1DA, HTR1DA, HTRL, RDC4, 5-HT1D receptor, 5-hydroxytryptamine receptor 1D
External IDs OMIM: 182133 MGI: 96276 HomoloGene: 20240 GeneCards: HTR1D
Orthologs
Species Human Mouse
Entrez
Ensembl
UniProt
RefSeq (mRNA)

NM_000864

NM_001285482
NM_001285483
NM_001285484
NM_008309

RefSeq (protein)

NP_000855

NP_001272411
NP_001272412
NP_001272413
NP_032335

Location (UCSC) Chr 1: 23.19 – 23.22 Mb Chr 4: 136.15 – 136.17 Mb
PubMed search
Wikidata
View/Edit Human View/Edit Mouse

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 vasoconstriction in the brain.

Tissue distribution and function

5HT1D receptors are found at low levels in the basal ganglia (globus pallidus, substantia nigra, caudate putamen), the hippocampus, and in the cortex.

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

Ligands

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)
  • Ergotamine (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

See also

External links

  • "5-HT1D". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.
  • Human HTR1D genome location and HTR1D gene details page in the UCSC Genome Browser.

Further reading

This article incorporates text from the United States National Library of Medicine, which is in the public domain.




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