5-hydroxytryptamine (serotonin) receptor 1D, also known as HTR1D, is a 5-HT receptor, but also denotes the human gene encoding it.[1] 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] Ligands [edit] Agonists - 5-(Nonyloxy)tryptamine,[2]
- sumatriptan (vasoconstrictor in migraine)
- 5-Carboxamidotryptamine (5-CT)
- 5-(t-Butyl)-N-methyltryptamine[3]
- 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 [edit] See also [edit] References - ^ "Entrez Gene: HTR1D 5-hydroxytryptamine (serotonin) receptor 1D". http://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=3352.
- ^ 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:10.1021/jm00044a001. PMID 8071931.
- ^ 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
[edit] External links [edit] Further reading - Hamblin MW, Metcalf MA, McGuffin RW, Karpells S (1992). "Molecular cloning and functional characterization of a human 5-HT1B serotonin receptor: a homologue of the rat 5-HT1B receptor with 5-HT1D-like pharmacological specificity.". Biochem. Biophys. Res. Commun. 184 (2): 752–9. doi:10.1016/0006-291X(92)90654-4. PMID 1315531.
- Weinshank RL, Zgombick JM, Macchi MJ, et al. (1992). "Human serotonin 1D receptor is encoded by a subfamily of two distinct genes: 5-HT1D alpha and 5-HT1D beta.". Proc. Natl. Acad. Sci. U.S.A. 89 (8): 3630–4. doi:10.1073/pnas.89.8.3630. PMID 1565658.
- Hamblin MW, Metcalf MA (1991). "Primary structure and functional characterization of a human 5-HT1D-type serotonin receptor.". Mol. Pharmacol. 40 (2): 143–8. PMID 1652050.
- Libert F, Passage E, Parmentier M, et al. (1992). "Chromosomal mapping of A1 and A2 adenosine receptors, VIP receptor, and a new subtype of serotonin receptor.". Genomics 11 (1): 225–7. doi:10.1016/0888-7543(91)90125-X. PMID 1662665.
- Libert F, Parmentier M, Lefort A, et al. (1989). "Selective amplification and cloning of four new members of the G protein-coupled receptor family.". Science 244 (4904): 569–72. doi:10.1126/science.2541503. PMID 2541503.
- Cargill M, Altshuler D, Ireland J, et al. (1999). "Characterization of single-nucleotide polymorphisms in coding regions of human genes.". Nat. Genet. 22 (3): 231–8. doi:10.1038/10290. PMID 10391209.
- Salim K, Fenton T, Bacha J, et al. (2002). "Oligomerization of G-protein-coupled receptors shown by selective co-immunoprecipitation.". J. Biol. Chem. 277 (18): 15482–5. doi:10.1074/jbc.M201539200. PMID 11854302.
- Strausberg RL, Feingold EA, Grouse LH, et al. (2003). "Generation and initial analysis of more than 15,000 full-length human and mouse cDNA sequences.". Proc. Natl. Acad. Sci. U.S.A. 99 (26): 16899–903. doi:10.1073/pnas.242603899. PMID 12477932.
- Bergen AW, van den Bree MB, Yeager M, et al. (2004). "Candidate genes for anorexia nervosa in the 1p33-36 linkage region: serotonin 1D and delta opioid receptor loci exhibit significant association to anorexia nervosa.". Mol. Psychiatry 8 (4): 397–406. doi:10.1038/sj.mp.4001318. PMID 12740597.
- Gerhard DS, Wagner L, Feingold EA, et al. (2004). "The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC).". Genome Res. 14 (10B): 2121–7. doi:10.1101/gr.2596504. PMID 15489334.
- Rual JF, Venkatesan K, Hao T, et al. (2005). "Towards a proteome-scale map of the human protein-protein interaction network.". Nature 437 (7062): 1173–8. doi:10.1038/nature04209. PMID 16189514.
- Gregory SG, Barlow KF, McLay KE, et al. (2006). "The DNA sequence and biological annotation of human chromosome 1.". Nature 441 (7091): 315–21. doi:10.1038/nature04727. PMID 16710414.
- Li J, Zhang X, Wang Y, et al. (2007). "The serotonin 5-HT1D receptor gene and attention-deficit hyperactivity disorder in Chinese Han subjects.". Am. J. Med. Genet. B Neuropsychiatr. Genet. 141 (8): 874–6. doi:10.1002/ajmg.b.30364. PMID 17099886.
This article incorporates text from the United States National Library of Medicine, which is in the public domain. | Transmembrane receptor: G protein-coupled receptors | | | Class A: Rhodopsin like | | | | | | | | | | | | | | | GPR ( 1, 3, 4, 6, 12, 15, 17, 18, 19, 20, 21, 22, 23, 25, 26, 27, 31, 32, 33, 34, 35, 37, 39, 42, 44, 45, 50, 52, 55, 61, 62, 63, 65, 68, 75, 77, 78, 82, 83, 84, 85, 87, 88, 92, 101, 103, 109A, 109B, 119, 120, 132, 135, 137B, 139, 141, 142, 146, 148, 149, 150, 151, 152, 153, 160, 161, 162, 171, 173, 174, 176, 177, 182) | | | | Adenosine ( A1, A2A, A2B, A3) · P2Y ( 1, 2, 4, 5, 6, 8, 9, 10, 11, 12, 13, 14) | | | | | | | Other | Acetylcholine ( M1, M2, M3, M4, M5) · Adrenomedullin · Anaphylatoxin ( C3a, C5a) · Angiotensin ( 1, 2) · Apelin · Bile acid · Bombesin ( BRS3, GRPR, NMBR) · Bradykinin ( B1, B2) · Cannabinoid ( CB1, CB2) · Chemokine · Cholecystokinin ( A, B) · Dopamine ( D1, D2, D3, D4, D5) · EBI2 · Endothelin ( A, B) · Estrogen · Formyl peptide ( 1, 2, 3) · Free fatty acid ( 1, 2, 3, 4) · FSH · Galanin ( 1, 2, 3) · Gonadotropin-releasing hormone ( 1, 2) · GHB receptor · Ghrelin · Histamine ( H1, H2, H3, H4) · Kisspeptin · Luteinizing hormone/choriogonadotropin · lysophosphatidic acid ( 1, 2, 3) · Lysophospholipid ( 1, 2, 3, 4, 5, 6, 7, 8) · MAS ( 1, 1L, D, E, F, G, X1, X2, X3, X4) · Melanocortin ( 1, 2, 3, 4, 5) · MCHR ( 1, 2) · Melatonin ( 1A, 1B, 1C) · Niacin ( 1, 2) · Motilin · Opioid ( Delta, Kappa, Mu, Nociceptin & Zeta, but not Sigma) · Olfactory · Opsin ( 3, 4, 5, 1LW, 1MW, 1SW, RGR, RRH) · Orexin ( 1, 2) · Oxytocin · Oxoglutarate · PAF · Prokineticin ( 1, 2) · Prolactin-releasing peptide · Protease-activated ( 1, 2, 3, 4) · Relaxin ( 1, 2, 3, 4) · Somatostatin ( 1, 2, 3, 4, 5) · Sphingosine-1-phosphate ( 1, 2, 3, 4, 5) · SREB · Succinate · TAAR ( 1, 2, 3, 5, 6, 8, 9) · Tachykinin ( 1, 2, 3) · Thyrotropin · Thyrotropin-releasing hormone · Urotensin-II · Vasopressin ( 1A, 1B, 2) | | | | Class B: Secretin like | | | GPR ( 56, 64, 97, 98, 110, 111, 112, 113, 114, 115, 116, 123, 124, 125, 126, 128, 133, 143, 144, 157) | | | Other | Brain-specific angiogenesis inhibitor ( 1, 2, 3) · Cadherin ( 1, 2, 3) · Calcitonin · CALCRL · CD97 · Corticotropin-releasing hormone ( 1, 2) · EMR ( 1, 2, 3) · Glucagon ( GR, GIPR, GLP1R, GLP2R) · Growth hormone releasing hormone · PACAPR1 · GPR · Latrophilin ( 1, 2, 3, ELTD1) · Methuselah-like proteins · Parathyroid hormone ( 1, 2) · Secretin · Vasoactive intestinal peptide ( 1, 2) | | | Class C: Metabotropic glutamate / pheromone | | | TAS1R ( 1, 2, 3) · TAS2R ( 1, 3, 4, 5, 8, 9, 10, 12, 13, 14, 16, 38, 39, 40, 41, 43, 44, 45, 46, 47, 48, 49, 50) | | | Other | Calcium-sensing receptor · GABA B ( 1, 2) · Glutamate receptor ( Metabotropic glutamate ( 1, 2, 3, 4, 5, 6, 7, 8)) · GPRC6A · GPR ( 156, 158, 179) · RAIG ( 1, 2, 3, 4) | | | | Frizzled / Smoothened | | | | Serotonergics | | Receptor ligands | | | | | | | | | | | | | Agonists: Lysergamides: Dihydroergotamine • Methysergide; Triptans: Almotriptan • Eletriptan • Frovatriptan • Naratriptan • Rizatriptan • Sumatriptan • Zolmitriptan; Tryptamines: 5-CT • 5-MT; Others: CP-135,807 • CP-286,601 • GR-46611 • L-694,247 • L-772,405 • PNU-109,291 • PNU-142,633 Antagonists: Lysergamides: Metergoline • Methiothepin; Tryptamines: Rauwolscine • Yohimbine; Others: Alniditan BRL-15572 • GR-127,935 • Ketanserin • LY-310,762 • LY-367,642 • LY-456,219 • LY-456,220 • Ritanserin • Ziprasidone | | | | | | | | | | | | | | | | | | | | | | | Agonists: Phenethylamines: 2C-B • 2C-E • 2C-I • 2C-T-2 • 2C-T-7 • 2C-T-21 • DOB • DOC • DOI • DOM • MDA • MDMA • Mescaline • Myristicin; Piperazines: Aripiprazole • mCPP • TFMPP; Tryptamines: 5-CT • 5-MeO-α-ET • 5-MeO-α-MT • 5-MeO-DET • 5-MeO-DiPT • 5-MeO-DMT • 5-MeO-DPT • 5-MT • α-ET • α-Methyl-5-HT • α-MT • Bufotenin • DET • DiPT • DMT • DPT • Psilocin • Psilocybin; Others: A-372,159 • AL-38022A • CP-809,101 • Lorcaserin • MK-212 • Org 37684 • PNU-22394 • Ro60-0175 • Vabicaserin • WAY-629 • WAY-161,503 • YM-348 Antagonists: Atypical Antipsychotics: Clozapine • Iloperidone • Melperone • Olanzapine • Paliperidone • Pimozide • Quetiapine • Risperidone • Sertindole • Ziprasidone • Zotepine; Typical Antipsychotics: Chlorpromazine • Loxapine • Pipamperone; Antidepressants: Agomelatine • Amitriptyline • Amoxapine • Etoperidone • Fluoxetine • Mianserin • Mirtazapine • Nefazodone • Nortriptyline • Trazodone; Others: Cinanserin • Cyproheptadine • Deramciclane • Dimebolin • Dotarizine • Eltoprazine • FR-260,010 • Ketanserin • Ketotifen • Methysergide • Pizotifen • Ritanserin • RS-102,221 • SB-200,646 • SB-206,553 • SB-221,284 • SB-228,357 • SB-242,084 • SB-243,213 • SDZ SER-082 • Xylamidine | | | | | | | | | | | | | | | | | | | Agonists: Lysergamides: Ergotamine • LSD Antagonists: Methiothepin * Note that the 5-HT5B receptor is not functional in humans. | | | | | | | | | | | | Reuptake inhibitors | | | Releasing agents | | | Enzyme inhibitors | | | | Others | | | |