5-HT1D receptor
Serotonin receptor which affects locomotion and anxiety in humans
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Related on Lably
Through Gene, Anxiety and Vasoconstriction
Tissue distribution
5HT1D receptors are found at low levels in the basal ganglia (globus pallidus, substantia nigra, caudate putamen), the hippocampus, and in the cortex.
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Structure
5HT1D receptor is a G protein-coupled receptor that activates an intracellular messenger cascade to produce an inhibitory response by decreasing cellular levels of cAMP. 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)
- Zolmitriptan
- 5-Carboxamidotryptamine (5-CT)
- 5-(t-Butyl)-N-methyltryptamine
- CP-135807
- CP-286601
- PNU-109291 ((S)-3,4-Dihydro-1-[2-[4-(4-methoxyphenyl)-1-piperazinyl]ethyl]-N-methyl-1H-2-benzopyran-6-carboxamide)
- PNU-142633 ((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-694247 (2-[5-[3-(4-Methylsulfonylamino)benzyl-1,2,4-oxadiazol-5-yl]-1H-indol-3-yl]ethanamine)
- L-760790
- L-772405
- PGI-7043
Antagonists
- Ziprasidone (atypical antipsychotic)
- Methiothepin (antipsychotic)
- Yohimbine (aphrodisiac)
- Metergoline
- BRL-15572
- Vortioxetine (antidepressant)
- F-12682
- F-14258
- GR-127935 (mixed 5-HT1B/1D antagonist)
- SB-714786
- LY-310762
- LY-367642
- LY-456219
- LY-456220
Negative allosteric modulators
- 5-HT-moduline