Receptors for 5-Hydroxytryptamine: Current perspectives on classification and nomenclature

With the increasing number of 5-HT receptors recently identified, using molecular biology techniques, the classification of 5-HT receptors is under review. An integrated approach is proposed to include operational and transductional as well as structural criteria for definitive receptor characterization. On this basis the existence of as many as seven classes of 5-HT receptor are recognized although only the 5-HT1, 5-HT2 and 5-HT3 receptor classes are well defined.

[1]  D. Nelson,et al.  Pharmacological characteristics of the newly cloned rat 5-hydroxytryptamine2F receptor. , 1993, Molecular pharmacology.

[2]  M. Mattei,et al.  Mouse 5-hydroxytryptamine5A and 5-hydroxytryptamine5B receptors define a new family of serotonin receptors: cloning, functional expression, and chromosomal localization. , 1993, Molecular pharmacology.

[3]  H. Lester,et al.  The mouse 5-HT1C receptor contains eight hydrophobic domains and is X-linked. , 1991, Brain research. Molecular brain research.

[4]  M. Erlander,et al.  A novel adenylyl cyclase-activating serotonin receptor (5-HT7) implicated in the regulation of mammalian circadian rhythms , 1993, Neuron.

[5]  S. Peroutka.  5‐Hydroxytryptamine Receptors , 1993, Journal of neurochemistry.

[6]  P. Conn,et al.  Agonist‐Induced Phosphoinositide Hydrolysis in Choroid Plexus , 1986, Journal of neurochemistry.

[7]  A. Ford,et al.  5-Hydroxytryptamine stimulates cyclic AMP formation in the tunica muscularis mucosae of the rat oesophagus via 5-HT4 receptors. , 1992, European journal of pharmacology.

[8]  J. Schwartz,et al.  A novel rat serotonin (5-HT6) receptor: molecular cloning, localization and stimulation of cAMP accumulation. , 1993, Biochemical and biophysical research communications.

[9]  P. Seeburg,et al.  Structure and functional expression of cloned rat serotonin 5HT‐2 receptor. , 1988, The EMBO journal.

[10]  J. Bockaert,et al.  A nonclassical 5-hydroxytryptamine receptor positively coupled with adenylate cyclase in the central nervous system. , 1988, Molecular pharmacology.

[11]  G. Engel,et al.  Identification of serotonin M-receptor subtypes and their specific blockade by a new class of drugs , 1985, Nature.

[12]  D. Nelson,et al.  Molecular cloning, functional expression, and pharmacological characterization of a novel serotonin receptor (5-hydroxytryptamine2F) from rat stomach fundus. , 1992, Molecular pharmacology.

[13]  H. Kao,et al.  Site‐directed mutagenesis of a single residue changes the binding properties of the serotonin 5‐HT2 receptor from a human to a rat pharmacology , 1992, FEBS letters.

[14]  C. Malgouris,et al.  Autoradiographic studies of RP 62203, a potent 5-HT2 receptor antagonist. In vitro and ex vivo selectivity profile. , 1993, European journal of pharmacology.

[15]  S. Chaki,et al.  5-HT2 antagonists and minaprine block the 5-HT-induced inhibition of dopamine release from rat brain striatal slices. , 1988, European journal of pharmacology.

[16]  H. Kao,et al.  Cloning of another human serotonin receptor (5-HT1F): a fifth 5-HT1 receptor subtype coupled to the inhibition of adenylate cyclase. , 1993, Proceedings of the National Academy of Sciences of the United States of America.

[17]  D. Middlemiss,et al.  An investigation of the 5-HT1D receptor binding affinity of 5-hydroxytryptamine, 5-carboxyamidotryptamine and sumatriptan in the central nervous system of seven species. , 1992, European journal of pharmacology.

[18]  B. Costall,et al.  Effects of the 5‐HT3 receptor antagonist, GR38032F, on raised dopaminergic activity in the mesolimbic system of the rat and marmoset brain , 1987, British journal of pharmacology.

[19]  W. Feniuk,et al.  An analysis of the mechanism of 5‐hydroxytrypt‐amine‐induced vasopressor responses in ganglion‐blocked anaesthetized dogs , 1981, The Journal of pharmacy and pharmacology.

[20]  M. Hamon,et al.  Quantitative autoradiography of multiple 5-HT1 receptor subtypes in the brain of control or 5,7-dihydroxytryptamine-treated rats , 1986, The Journal of neuroscience : the official journal of the Society for Neuroscience.

[21]  L. Sanders,et al.  A 5‐hydroxytryptamine receptor in human atrium , 1990, British journal of pharmacology.

[22]  M. Moskowitz,et al.  CP‐93,129, a potent and selective 5‐HT1B receptor agonist blocks neurogenic plasma extravasation within rat but not guinea‐pig dura mater , 1991, British journal of pharmacology.

[23]  P. Gupta,et al.  An endothelial 5‐HT receptor that mediates relaxation in guinea‐pig isolated jugular vein resembles the 5‐HT1D subtype , 1992, British journal of pharmacology.

[24]  J. Bockaert,et al.  Serotonin increases calcium current in human atrial myocytes via the newly described 5-hydroxytryptamine4 receptors. , 1992, Molecular pharmacology.

[25]  G. Blauw,et al.  Serotonin induced vasodilatation in the human forearm is antagonized by the selective 5-HT3 receptor antagonist ICS 205-930. , 1988, Life sciences.

[26]  I. Lucki.  5-HT1 receptors and behavior , 1992, Neuroscience & Biobehavioral Reviews.

[27]  A. Kaumann.  5-HT4-like receptors in mammalian atria. , 1991, Journal of neural transmission. Supplementum.

[28]  G. Martin.  Vascular receptors for 5-hydroxytryptamine: distribution, function and classification. , 1994, Pharmacology & therapeutics.

[29]  A. Frazer,et al.  Subtypes of receptors for serotonin. , 1990, Annual review of pharmacology and toxicology.

[30]  M. Pollard,et al.  Effect of indomethacin on intestinal tumors induced in rats by the acetate derivative of dimethylnitrosamine. , 1981, Science.

[31]  Gavin Kilpatrick,et al.  5‐HT3 receptors , 1990, Annals of the New York Academy of Sciences.

[32]  B. O'dowd,et al.  A single amino-acid difference confers major pharmacological variation between human and rodent 5-HT1B receptors , 1992, Nature.

[33]  M. Raiteri,et al.  Differential pharmacology and function of two 5-HT1 receptors modulating transmitter release in rat cerebellum. , 1986, The Journal of pharmacology and experimental therapeutics.

[34]  M. Moskowitz,et al.  Further characterization of the putative 5‐HT receptor which mediates blockade of neurogenic plasma extravasation in rat dura mater , 1991, British journal of pharmacology.

[35]  D. Hoyer,et al.  5-Hydroxytryptamine (5-HT)-induced endothelium-dependent relaxation of pig coronary arteries is mediated by 5-HT receptors similar to the 5-HT1D receptor subtype. , 1990, The Journal of pharmacology and experimental therapeutics.

[36]  G Maura,et al.  Cholinergic terminals in rat hippocampus possess 5-HT1B receptors mediating inhibition of acetylcholine release. , 1986, European journal of pharmacology.

[37]  W. Feniuk,et al.  Studies on the mechanism of 5‐HT1 receptor‐induced smooth muscle contraction in dog saphenous vein , 1992, British journal of pharmacology.

[38]  G. Wilcox,et al.  Spinal 5-HT3 receptor-mediated antinociception: possible release of GABA , 1991, The Journal of neuroscience : the official journal of the Society for Neuroscience.

[39]  T. Bonner,et al.  Definition of pharmacological receptors. , 1992, Pharmacological reviews.

[40]  E. R. Kloet,et al.  8-Hydroxy-2-(DI-N-propylamino)tetralin increases the activity of adenylate cyclase in the hippocampus of freely-moving rats , 1991, Neuropharmacology.

[41]  H. Kao,et al.  [3H]-DOB(4-bromo-2,5-dimethoxyphenylisopropylamine) and [3H] ketanserin label two affinity states of the cloned human 5-hydroxytryptamine2 receptor. , 1990, Molecular pharmacology.

[42]  J. Green,et al.  Serotonergic modulation of the release of endogenous norepinephrine from rat hypothalamic slices. , 1991, The Journal of pharmacology and experimental therapeutics.

[43]  D. Middlemiss,et al.  L‐694,247: a potent 5‐HT1D receptor agonist , 1993, British journal of pharmacology.

[44]  J. Palacios,et al.  Serotonin receptors in the human brain—IV. Autoradiographic mapping of serotonin-2 receptors , 1987, Neuroscience.

[45]  H. Kao,et al.  The molecular biology of serotonin receptors. An overview. , 1990, Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology.

[46]  A. Allgeier,et al.  The human and dog 5-HT1D receptors can both activate and inhibit adenylate cyclase in transfected cells. , 1993, European journal of pharmacology.

[47]  G. Martin,et al.  5‐HT1B receptors mediate potent contractile responses to 5‐HT in rat caudal artery , 1993, British journal of pharmacology.

[48]  J. Launay,et al.  New mouse 5‐HT2‐like receptor Expression in brain, heart and intestine , 1992, FEBS letters.

[49]  G. Martin,et al.  Differential classification of vascular smooth muscle and endothelial cell 5‐HT receptors by use of tryptamine analogues , 1987, British journal of pharmacology.

[50]  W. Feniuk,et al.  5-hydroxytryptamine-induced relaxation of neonatal porcine vena cava in vitro. , 1984, Life sciences.

[51]  J. Pouysségur,et al.  Chinese hamster serotonin (5-HT) type 2 receptor cDNA sequence. , 1990, Nucleic acids research.

[52]  R. Y. Wang,et al.  Effect of 5-hydroxytryptamine3 receptor agonists on phosphoinositides hydrolysis in the rat fronto-cingulate and entorhinal cortices. , 1991, Journal of Pharmacology and Experimental Therapeutics.

[53]  M. Feuilloley,et al.  Serotonin-induced stimulation of cortisol secretion from human adrenocortical tissue is mediated through activation of a serotonin4 receptor subtype , 1992, Neuroscience.

[54]  T. Jessell,et al.  Molecular characterization of a functional cDNA encoding the serotonin 1c receptor. , 1988, Science.

[55]  D. Sibley,et al.  Molecular cloning and expression of a 5-hydroxytryptamine7 serotonin receptor subtype. , 1993, The Journal of biological chemistry.

[56]  J. Fozard,et al.  The 5-HT4 receptor: naughty, but nice. , 1989, Trends in pharmacological sciences.

[57]  D. Clarke,et al.  Pharmacological characterization of a neuronal receptor for 5-hydroxytryptamine in guinea pig ileum with properties similar to the 5-hydroxytryptamine receptor. , 1990, The Journal of pharmacology and experimental therapeutics.

[58]  J. Fozard,et al.  Serotonin: Molecular Biology, Receptors and Functional Effects , 1991, Birkhäuser Basel.

[59]  R. Nicoll,et al.  A G protein couples serotonin and GABAB receptors to the same channels in hippocampus. , 1986, Science.

[60]  D. Hoyer,et al.  A proposed new nomenclature for 5-HT receptors. , 1993, Trends in pharmacological sciences.

[61]  D. Wallis,et al.  5-hydroxytryptamine depolarizes neonatal rat motorneurones through a receptor unrelated to an identified binding site , 1989, Neuropharmacology.

[62]  P. Bradley,et al.  Proposals for the classification and nomenclature of functional receptors for 5-hydroxytryptamine , 1986, Neuropharmacology.

[63]  M. Perren,et al.  Vascular 5‐HT1‐like receptors that mediate contraction of the dog isolated saphenous vein and carotid arterial vasoconstriction in anaesthetized dogs are not of the 5‐HT1A or 5‐HT1D subtype , 1991, British journal of pharmacology.

[64]  W. Stühmer,et al.  Cloning and functional characterization of the rat stomach fundus serotonin receptor. , 1992, The EMBO journal.

[65]  R. Myers,et al.  Primary structure and functional expression of the 5HT3 receptor, a serotonin-gated ion channel. , 1991, Science.

[66]  T. Branchek,et al.  Expression and pharmacological characterization of a canine 5-hydroxytryptamine1D receptor subtype. , 1991, Molecular pharmacology.

[67]  T. Jessell,et al.  5-HT1c receptor is a prominent serotonin receptor subtype in the central nervous system. , 1989, Proceedings of the National Academy of Sciences of the United States of America.

[68]  D. Sibley,et al.  Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. , 1993, Molecular pharmacology.

[69]  M. Titeler,et al.  Detection of a Novel Serotonin Receptor Subtype (5‐HT1E) in Human Brain: Interaction with a GTP‐Binding Protein , 1989, Journal of neurochemistry.

[70]  J. Plassat,et al.  Molecular cloning of a mammalian serotonin receptor that activates adenylate cyclase. , 1993, Molecular pharmacology.

[71]  J. Schwartz,et al.  Molecular cloning, characterization, and localization of a high-affinity serotonin receptor (5-HT7) activating cAMP formation. , 1993, Proceedings of the National Academy of Sciences of the United States of America.

[72]  P. Seeburg,et al.  Structure functional expression and spatial distribution of a cloned cDNA encoding a rat 5-HT1D-like receptor. , 1993, Journal of receptor research.

[73]  J. Green,et al.  Activation of a 5-HT3 receptor releases dopamine from rat striatal slice. , 1988, European journal of pharmacology.

[74]  J. Fozard.  Agonists and antagonists of 5-HT3 receptors , 1990 .

[75]  J. Bockaert,et al.  The 5‐HT4 receptor subtype inhibits K+ current in colliculi neurones via activation of a cyclic AMP‐dependent protein kinase , 1992, British journal of pharmacology.

[76]  J. Palacios,et al.  Serotonin receptors in the human brain. II. Characterization and autoradiographic localization of 5-HT1C and 5-HT2 recognition sites , 1986, Brain Research.

[77]  R. Andrade,et al.  5-Hydroxytryptamine4-like receptors mediate the slow excitatory response to serotonin in the rat hippocampus. , 1991, The Journal of pharmacology and experimental therapeutics.

[78]  J. Palacios,et al.  5-Hydroxytryptamine3 receptors in the human brain: Autoradiographic visualization using [3H]ICS 205-930 , 1989, Neuroscience.

[79]  R. Glennon,et al.  Serotonin receptors and their ligands: A lack of selective agents , 1991, Pharmacology Biochemistry and Behavior.

[80]  Gavin Kilpatrick,et al.  Development of a radioligand binding assay for 5‐HT4 receptors in guinea‐pig and rat brain , 1993, British journal of pharmacology.

[81]  J. A. Peters,et al.  Characterization of 5HT3 Receptor Mediated Electrical Responses in Nodose Ganglion Neurones and Clonal Neuroblastoma Cells Maintained in Culture , 1991 .

[82]  R. North,et al.  5‐Hydroxytryptamine acts at 5‐HT2 receptors to decrease potassium conductance in rat nucleus accumbens neurones. , 1989, The Journal of physiology.

[83]  G. Kennett,et al.  Anxiogenic-like effects of mCPP and TFMPP in animal models are opposed by 5-HT1C receptor antagonists. , 1989, European journal of pharmacology.

[84]  G. Sanger,et al.  Neuropharmacology of emesis induced by anti-cancer therapy. , 1988, Trends in pharmacological sciences.

[85]  P. Hartig.  Molecular biology of 5-HT receptors. , 1989, Trends in pharmacological sciences.

[86]  W. Meyerhof,et al.  A novel rat serotonin receptor: primary structure, pharmacology, and expression pattern in distinct brain regions. , 1993, DNA and cell biology.

[87]  J. Black,et al.  Pharmacological analysis of muscarinic receptors coupled to oxyntic cell secretion in the mouse stomach , 1985, British journal of pharmacology.

[88]  J. Fozard.  Neuronal 5-HT receptors in the periphery , 1984, Neuropharmacology.

[89]  G. Fillion,et al.  The Inhibitory Effect of Trifluoromethylphenylpiperazine on [3H]Acetylcholine Release in Guinea Pig Hippocampal Synaptosomes Is Mediated by a 5‐Hydroxytryptamine1 Receptor Distinct from 1A, 1B, and 1C Subtypes , 1991, Journal of neurochemistry.

[90]  U. Boschert,et al.  Isolation of a mouse "5HT1E-like" serotonin receptor expressed predominantly in hippocampus. , 1992, The Journal of biological chemistry.

[91]  J. Villemure,et al.  Expression of mRNA for the serotonin 5-hydroxytryptamine1D beta receptor subtype in human and bovine cerebral arteries. , 1993, Molecular pharmacology.

[92]  P. Ham,et al.  N-(1-methyl-5-indolyl)-N'-(3-pyridyl)urea hydrochloride: the first selective 5-HT1C receptor antagonist. , 1993, Journal of medicinal chemistry.

[93]  S. Peroutka,et al.  Characterization of a novel 3H-5-hydroxytryptamine binding site subtype in bovine brain membranes , 1987, The Journal of neuroscience : the official journal of the Society for Neuroscience.

[94]  U. Boschert,et al.  The mouse 5HT5 receptor reveals a remarkable heterogeneity within the 5HT1D receptor family. , 1992, The EMBO journal.

[95]  B. Costall,et al.  5-HT3 receptors mediate inhibition of acetylcholine release in cortical tissue , 1989, Nature.

[96]  P. Saxena,et al.  Cardiovascular Pharmacology of 5-Hydroxytryptamine , 1990 .

[97]  H. Boddeke,et al.  Agonist effects at putative central 5-HT4 receptors in rat hippocampus by R(+)- and S(−)-zacopride; no evidence for stereo-selectivity , 1992, Neuroscience Letters.

[98]  W. Feniuk,et al.  Further characterization of the 5‐HT receptor mediating vascular relaxation and elevation of cyclic AMP in porcine isolated vena cava , 1989, British journal of pharmacology.

[99]  J. Palacios,et al.  Localisation by autoradiography of neuronal 5-HT3 receptors in the mouse CNS. , 1988, European journal of pharmacology.

[100]  J. Palacios,et al.  Localization of 5-HT1B, 5-HT1Dα, 5-HT1E and 5-HT1F receptor messenger RNA in rodent and primate brain , 1994, Neuropharmacology.

[101]  M. Caron,et al.  Effector coupling mechanisms of the cloned 5-HT1A receptor. , 1989, The Journal of biological chemistry.

[102]  H. Aihara,et al.  Serotonin-2 receptor-mediated regulation of release of acetylcholine by minaprine in cholinergic nerve terminal of hippocampus of rat , 1988, Neuropharmacology.

[103]  M. Bodelsson,et al.  Endothelial relaxing 5-hydroxytryptamine receptors in the rat jugular vein: similarity with the 5-hydroxytryptamine1C receptor. , 1993, The Journal of pharmacology and experimental therapeutics.

[104]  J. Bockaert,et al.  Pharmacological Characterization of Brain 5-HT4 Receptors: Relationship between the Effects of Indole, Benzamide and Azabicycloalkybenzimidazolone Derivatives , 1991 .

[105]  P. Albert,et al.  Cell-specific signaling of the 5-HT1A receptor. Modulation by protein kinases C and A. , 1991, Journal of Biological Chemistry.

[106]  E. Mylecharane.  Agonists and antagonists of 5-HT2 receptors , 1990 .

[107]  D. Hoyer.  Molecular pharmacology and biology of 5-HT1C receptors. , 1988, Trends in pharmacological sciences.

[108]  D. Yang,et al.  SC-53116: the first selective agonist at the newly identified serotonin 5-HT4 receptor subtype. , 1992, Journal of medicinal chemistry.

[109]  T. Branchek,et al.  The rat 5-hydroxytryptamine1B receptor is the species homologue of the human 5-hydroxytryptamine1D beta receptor. , 1992, Molecular pharmacology.

[110]  M. Raiteri,et al.  Serotonin-glutamate interaction in rat cerebellum: involvement of 5-HT1 and 5-HT2 receptors. , 1988, European journal of pharmacology.

[111]  H. Ladinsky,et al.  The orphan receptor cDNA RDC4 encodes a 5-HT1D serotonin receptor. , 1991, Biochemical and biophysical research communications.

[112]  S. Cooper,et al.  Behavioural pharmacology of 5-HT3 receptor ligands , 1992, Neuroscience & Biobehavioral Reviews.

[113]  A. Galzin,et al.  Modulation of 5-HT Release by Presynaptic Inhibitory and Facilitatory 5-HT Receptors in Brain Slices , 1991 .

[114]  R. Naylor,et al.  Consensus meeting agrees distribution of 5-HT3 receptors in mammalian hindbrain. , 1990 .

[115]  J. Bockaert,et al.  A 5-HT receptor in the central nervous system, positively coupled with adenylate cyclase, is antagonized by ICS 205 930. , 1988, European journal of pharmacology.

[116]  J. Axelrod,et al.  Serotonin stimulates phospholipase A2 and the release of arachidonic acid in hippocampal neurons by a type 2 serotonin receptor that is independent of inositolphospholipid hydrolysis. , 1990, Proceedings of the National Academy of Sciences of the United States of America.

[117]  T. Branchek,et al.  Enteric receptors for 5-hydroxytryptamine , 1984, Brain Research.

[118]  M. Erlander,et al.  Two members of a distinct subfamily of 5-hydroxytryptamine receptors differentially expressed in rat brain. , 1993, Proceedings of the National Academy of Sciences of the United States of America.

[119]  H. Ladinsky,et al.  Azabicycloalkyl benzimidazolones: Interaction with serotonergic 5-HT3 and 5-HT4 receptors and potential therapeutic implications , 1991 .

[120]  M. Hamon,et al.  Presynaptic 5-HT autoreceptors on serotonergic cell bodies and/or dendrites but not terminals are of the 5-HT1A subtype. , 1985, European journal of pharmacology.

[121]  A. Saltzman,et al.  Cloning of the human serotonin 5-HT2 and 5-HT1C receptor subtypes. , 1991, Biochemical and biophysical research communications.

[122]  K. Bunce,et al.  Identification of putative 5-HT4 receptors in guinea-pig ascending colon. , 1991, European journal of pharmacology.

[123]  J. Macor,et al.  3-(1,2,5,6-Tetrahydropyrid-4-yl)pyrrolo[3,2-b]pyrid-5-one: a potent and selective serotonin (5-HT1B) agonist and rotationally restricted phenolic analogue of 5-methoxy-3-(1,2,5,6-tetrahydropyrid-4-yl)indole. , 1990, Journal of medicinal chemistry.

[124]  A. Tsou,et al.  Cloning and Expression of a 5‐Hydroxytryptamine7 Receptor Positively Coupled to Adenylyl Cyclase , 1994, Journal of neurochemistry.