5HT1D receptors are found at low levels in the basal ganglia (globus pallidus, substantia nigra, caudate putamen), the hippocampus, and in the cortex.[6]
5HT1D receptor is aG protein linked receptor that activates anintracellular messenger cascade to produce an inhibitory response by decreasing cellular levels of cAMP.[7][8] The 5HT1D is a7-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 anaspartate residue in TM-3 and residues in the TM-4, TM-5 and TM-6.[9] A human clone containing an intronlessopen 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[10][11]
Molecular modelling has provided a picture of theagonistic binding site of 5HT1D. Theamino acid residues within the receptor binding site region have been identified. This is a valuable guide to design potential 5HT1D receptor agonists.Whensumatriptan binds there is major conformational change in both ligand and receptor in the binding pocket.[12]
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^Millan MJ, Marin P, Bockaert J, Mannoury la Cour C (September 2008). "Signaling at G-protein-coupled serotonin receptors: recent advances and future research directions".Trends in Pharmacological Sciences.29 (9):454–64.doi:10.1016/j.tips.2008.06.007.PMID18676031.
^Goadsby PJ (1998). "Serotonin 5-HT1B/1D Receptor Agonists in Migraine: Comparative Pharmacology and Its Therapeutic Implications".CNS Drugs.10 (4):271–286.doi:10.2165/00023210-199810040-00005.
^Bremner DH, Ringan NS, Wishart G (1997). "Modeling of the agonist binding site of serotonin human 5-HT1A, 5-HT1Dα and 5-HT1Dβ receptors".European Journal of Medicinal Chemistry.32 (1):59–69.doi:10.1016/S0223-5234(97)84362-0.
^Glennon RA, Hong SS, Dukat M, Teitler M, Davis K (September 1994). "5-(Nonyloxy)tryptamine: a novel high-affinity 5-HT1D beta serotonin receptor agonist".Journal of Medicinal Chemistry.37 (18):2828–2830.doi:10.1021/jm00044a001.PMID8071931.
^Xu YC, Schaus JM, Walker C, Krushinski J, Adham N, Zgombick JM, et al. (February 1999). "N-Methyl-5-tert-butyltryptamine: A novel, highly potent 5-HT1D receptor agonist".Journal of Medicinal Chemistry.42 (3):526–531.doi:10.1021/jm9805945.PMID9986723.
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Hamblin MW, Metcalf MA (August 1991). "Primary structure and functional characterization of a human 5-HT1D-type serotonin receptor".Molecular Pharmacology.40 (2):143–148.PMID1652050.
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Libert F, Parmentier M, Lefort A, Dinsart C, Van Sande J, Maenhaut C, et al. (May 1989). "Selective amplification and cloning of four new members of the G protein-coupled receptor family".Science.244 (4904):569–572.Bibcode:1989Sci...244..569L.doi:10.1126/science.2541503.PMID2541503.
Cargill M, Altshuler D, Ireland J, Sklar P, Ardlie K, Patil N, et al. (July 1999). "Characterization of single-nucleotide polymorphisms in coding regions of human genes".Nature Genetics.22 (3):231–238.doi:10.1038/10290.PMID10391209.S2CID195213008.
Bergen AW, van den Bree MB, Yeager M, Welch R, Ganjei JK, Haque K, et al. (April 2003). "Candidate genes for anorexia nervosa in the 1p33-36 linkage region: serotonin 1D and delta opioid receptor loci exhibit significant association to anorexia nervosa".Molecular Psychiatry.8 (4):397–406.doi:10.1038/sj.mp.4001318.PMID12740597.S2CID22413624.
