5-hydroxytryptamine 1D receptor
From DrugPedia: A Wikipedia for Drug discovery
Contents |
[edit] Description
5-hydroxytryptamine (serotonin) receptor 1D, also known as HTR1D, is a 5-HT receptor, but also denotes the human gene encoding it.<ref name="entrez">Template:Cite web</ref> 5-HT1D acts on the central nervous system, and affects locomotion and anxiety. It also induces vascular vasoconstriction in the brain. Ergotamine works primarily through the 5-HT1B receptor, since the effect through the 5-HT1D receptor is contrary to the mode of action of ergotamine, i.e. vasoconstriction.
[edit] Source Organism
Canis familiaris (Dog).
[edit] Taxomomy
Eukaryota; Metazoa; Chordata; Craniata; Vertebrata; Euteleostomi;Mammalia; Eutheria; Laurasiatheria; Carnivora; Caniformia; Canidae;Canis.
[edit] Subcellular Localization
Cell membrane; multi-pass membrane protein.
[edit] Developmental Stage
[edit] Similarity
Belongs to the G-protein coupled receptor 1 family.
[edit] Post translational Modification
[edit] Function
This is one of the several different receptors for 5- hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activity of this receptor is mediated by G proteins that inhibit adenylate cyclase activity.
Categories:Receptors Template:Wrongtitle
[edit] Ligands
[edit] Agonists
- 5-(Nonyloxy)tryptamine,<ref name="Glennon_et_al_94">Glennon RA, Hong SS, Dukat M, Teitler M, Davis K (1994). "5-(Nonyloxy)tryptamine: a novel high-affinity 5-HT1D beta serotonin receptor agonist". J. Med. Chem. 37 (18): 2828–30. doi: . PMID 8071931.</ref>
- sumatriptan (vasoconstrictor in migraine)
- 5-Carboxamidotryptamine (5-CT)
- 5-(t-Butyl)-N-methyltryptamine<ref>Xu YC, Schaus JM, Walker C, Krushinski J, Adham N, Zgombick JM, Liang SX, Kohlman DT, Audia JE. N-Methyl-5-tert-butyltryptamine: A novel, highly potent 5-HT1D receptor agonist. Journal of Medicinal Chemistry. 1999 Feb 11;42(3):526-31. PMID 9986723</ref>
- 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
[edit] Antagonists
- Ziprasidone (atypical antipsychotic) [1]
- methiothepin (antipsychotic)
- yohimbine (aphrodisiac)
- metergoline
- ergotamine (vasoconstrictor in migraine)
- BRL-15572
- GR-127,935 (mixed 5-HT1B/1D antagonist)
- LY-310,762
- LY-367,642
- LY-456,219
- LY-456,220
[edit] External links
[edit] References
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