Bibliography
- Hoyer D, Hannon JP, Martin GR. Molecular, pharmacological and functional diversity of 5-HT receptors. Pharmacol Biochem Behav 2002;71:533-54
- Kia HK, Miquel MC, Brisorgueil MJ, Immunocytochemical localization of serotonin1A receptors in the rat central nervous system. J Comp Neurol 1996;365:289-305
- Chalmers DT, Watson SJ. Comparative anatomical distribution of 5-HT1A receptor mRNA and 5-HT1A binding in rat brain–a combined in situ hybridization/in vitro receptor auto radiographic study. Brain Res 1991;561:51-60
- Riad M, Garcia S, Watkins KC, Somatodendritic localization of 5-HT1A and preterminal axonal localization of 5-HT1B serotonin receptors in adult rat brain. J Comp Neurol 2000;417:181-94
- Freund TF, Gulyas AI, Acsady L, Serotonergic control of the hippocampus via local inhibitory interneurons. Proc Natl Acad Sci USA 1990;87:8501-5
- Halasy K, Miettinen R, Szabat E, Freund TF. GABAergic interneurons are the major postsynaptic targets of median raphe afferents in the rat dentate gyrus. Eur J Neurosci 1992;4:144-53
- Cassel JC, Jeltsch H. Serotonergic modulation of cholinergic function in the central nervous system: cognitive implications. Neuroscience 1995;69:1-41
- Sprouse JS, Aghajanian GK. Electrophysiological responses of serotoninergic dorsal raphe neurons to 5-HT1A and 5-HT1B agonists. Synapse 1987;1:3-9
- Sprouse JS, Aghajanian GK. Responses of hippocampal pyramidal cells to putative serotonin 5-HT1A and 5-HT1B agonists: a comparative study with dorsal raphe neurons. Neuropharmacology 1988;27:707-15
- De Vivo M, Maayani S. Characterization of the 5-hydroxytryptamine1a receptor-mediated inhibition of forskolin-stimulated adenylate cyclase activity in guinea pig and rat hippocampal membranes. J Pharmacol Exp Ther 1986;238:248-53
- Dumuis A, Sebben M, Bockaert J. Pharmacology of 5-hydroxytryptamine-1A receptors which inhibit cAMP production in hippocampal and cortical neurons in primary culture. Mol Pharmacol 1988;33:178-86
- Raymond JR, Olsen CL, Gettys TW. Cell-specific physical and functional coupling of human 5-HT1A receptors to inhibitory G protein alpha-subunits and lack of coupling to Gs alpha. Biochemistry 1993;32:11064-73
- Saenz del Burgo L, Cortes R, Mengod G, Distribution and neurochemical characterization of neurons expressing GIRK channels in the rat brain. J Comp Neurol 2008;510:581-606
- Polter AM, Li X. 5-HT1A receptor-regulated signal transduction pathways in brain. Cell Signal 2010;22:1406-12
- Keshet Y, Seger R. The MAP kinase signaling cascades: a system of hundreds of components regulates a diverse array of physiological functions. Methods Mol Biol 2010;661:3-38
- Lacivita E, Leopoldo M, Berardi F, Perrone R. 5-HT1A receptor, an old target for new therapeutic agents. Curr Top Med Chem 2008;8:1024-34
- Jann MW. Buspirone: an update on a unique anxiolytic agent. Pharmacotherapy 1988;8:100-16
- Fuller RW. Role of serotonin in therapy of depression and related disorders. J Clin Psychiatry 1991;152(Suppl l):52-7
- Meltzer HY, Li Z, Kaneda Y, Ichikawa J. Serotonin receptors: their key role in drugs to treat schizophrenia. Prog Neuropsychopharmacol Biol Psychiatry 2003;27:1159-72
- Van Den Hooff P, Galvan M. Actions of 5-hydroxytryptamine and 5-HT1A receptor ligands on rat dorso-lateral septal neurons in vitro. Br J Pharmacol 1992;106:893-9
- Hirose A, Sasa M, Akaike A, Takaori S. Inhibition of hippocampal CA1 neurons by 5-hydroxytryptamine,derived from the dorsal raphe nucleus and the 5-hydroxytryptamine1A agonist SM-3997. Neuropharmacology 1990;29:93-101
- Ohno Y, Ishida K, Ishibashi T, Effects of tandospirone, a selective 5-HT1A agonist, on activities of the lateral septal nucleus neurons in cats. In: Takada Y, Curzon G, editors. Serotonin in the central nervous system and periphery. Elsevier Science BV; Amsterdam: 1995. p. 159-65
- Raymond JR, Muklin YV, Gettys TW, Garnovskaya MN. The recombinant 5-HT1A receptor: G protein coupling and signalling pathways. Br J Pharmacol 1999;127:1751-64
- Tada K, Kasamo K, Ueda N, Anxiolytic 5-hydroxytryptamine1A agonists suppress firing activity of dorsal hippocampus CA1 pyramidal neurons through a postsynaptic mechanism: Single-unit study in unanesthetized, unrestrained rats. J Pharmacol Exp Ther 1999;288:843-8
- Wieland S, Lucki I. Antidepressant-like activity of 5-HT1A agonists measured with the forced swim test. Psychopharmacology (Berl) 1990;101:497-504
- Blier P, Ward NM. Is there a role for 5-HT1A agonists in the treatment of depression? Biol Psychiatry 2003;53:193-203
- Blier P, de Montigny C. Modification of 5-HT neuron properties by sustained administration of the 5-HT1A agonist gepirone: Electrophysiological studies in the rat brain. Synapse 1987;1:470-80
- Schechter LE, Bolanos FJ, Gozlan H, Alterations of central serotoninergic and dopaminergic neurotransmission in rats chronically treated with ipsapirone: biochemical and electrophysiological studies. J Pharmacol Exp Ther 1990;255:1335-47
- Citrome L. Vilazodone for major depressive disorder: a systematic review of the efficacy and safety profile for this newly approved antidepressant - what is the number needed to treat, number needed to harm and likelihood to be helped or harmed? Int J Clin Pract 2012;66:356-68
- Pierre Fabre Medicament. Novel derivatives of aryl-{4-halogeno-4-[aminomethyl]piperidin-1-yl}-methanone, their method of preparation and use as medicinal products. WO10139758; 2010
- Hibert MH, Gittos MW, Middlemiss DN, Graphics computer-aided receptor mapping as a predictive tool for drug design: development of potent, selective, and stereospecific ligands for the 5-HT1A receptor. J Med Chem 1988;31:1087-93
- Friedrich-Alexander-Universitat Erlangen-Nurnberg. Heteroaryl-substituted 2-pyridinylmethylamine derivatives. WO09060030; 2009
- Lopez-Rodriguez ML, Ayala D, Benhamu D, Arylpiperazine derivatives acting at 5-HT1A receptors. Curr Med Chem 2002;9:443-69
- SK Holding. Phenylpiperazine compounds, pharmaceutical composition including the same and use thereof. US0298831; 2009
- Wyeth. Benzofuranyl- and benzothienyl-piperazinyl quinolines and methods of their use. US0054454; 2009
- Perrone R, Berardi F, Colabufo NA, Trans-4-[4-(Methoxyphenyl)cyclohexyl]-1-arylpiperazines: a new class of potent and selective 5-HT(1A) receptor ligands as conformationally constrained analogues of 4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]-1-arylpiperazines. J Med Chem 2001;44:4431-42
- Wyeth. 3-Amino chromane derivatives. WO08080120; 2008
- Mewshaw RE, Zhou D, Zhou P, Studies toward the discovery of the next generation of antidepressants. Dual 5-HT1A and serotonin transporter affinity within a class of N-aryloxyethylindolylalkylamines. J Med Chem 2004;47:3823-42
- Wyeth. Tetrahydroquinoline, indoline, and related aniline derivatives of hetrocycle-fused benzodioxan methylamines. WO08042735; 2008
- Pfizer, Inc. Phenoxy-pyridyl derivatives. WO09081259; 2009
- The General Hospital Corp. Combination therapy for depression. WO08156749; 2008
- Newman-Tancredi A, Kleven MS. Comparative pharmacology of antipsychotics possessing combined dopamine D2 and serotonin 5-HT1A receptor properties. Psychopharmacology (Berl) 2011;216:451-73
- Shimizu S, Tatara A, Imaki J, Ohno Y. Role of cortical and striatal 5-HT1A receptors in alleviating antipsychotic-induced extrapyramidal disorders. Prog Neuropsychopharmacol Biol Psychiatry 2010;34:877-81
- King MV, Marsden CA, Fone KC. A role for the 5-HT1A, 5-HT4 and 5-HT6 receptors in learning and memory. Trends Pharmacol Sci 2008;29:482-92
- Ogren SO, Eriksson TM, Elvander-Tottie E, The role of 5-HT1A receptors in learning and memory. Behav Brain Res 2008;195:54-77
- Madjid N, Tottie EE, Luttgen M, 5-Hydroxytryptamine1A receptor blockade facilitates aversive learning in mice: interactions with cholinergic and glutamatergic mechanisms. J Pharmacol Exp Ther 2006;316:581-91
- Jeltsch H, Bertand F, Galani R, Intraseptal injection of the 5-HT1A/5-HT7 agonist 8-OH DPAT and working memory in rats. Psychopharmacology 2004;175:37-46
- Available from: http://clinicaltrials.gov/ct2/results?term=bifeprunox [Last accessed 4 May 2012]
- Lundbeck. Pipeline update - following an interim analysis the studies with bifeprunox for the treatment of schizophrenia is discontinued. Available from: http://investor.lundbeck.com/releasedetail.cfm?ReleaseID=608617 [Last accessed 4 May 2012]
- NeuroSearch AS. Novel quinolinylamide derivatives useful as modulators of dopamine and serotonin receptors. WO10040808; 2010
- NeuroSearch AS. Novel arylpiperazine derivatives useful as modulators of dopamine and serotonin receptors. WO09095438; 2009
- NeuroSearch AS. Novel quinolinylamide derivatives useful as modulators of dopamine and serotonin receptors. WO009112568; 2009
- Astra Zeneca AB. Methods of treating anxiety and mood disorders. US0093461; 2009
- Reviva Pharmaceuticals, Inc. Compositions, synthesis, and methods of using quinolinone based atypical antipsychotic agents. US0293736; 2008
- Reviva Pharmaceuticals, Inc. Compositions, synthesis, and methods of using piperazine based antipsychotic agents. US0298819; 2009
- Reviva Pharmaceuticals, Inc. Composition, synthesis, and methods of utilizing arylpiperazine derivatives. US0216783; 2010
- Schwarz Pharma AG. Indolizines and aza-analog derivatives thereof as CNS active compounds. WO08113559; 2008
- Pfizer, Inc. 7-(4-(4-[3-Chloro-2-(trifluoromethyl)phenyl]piperazin-1-yl)butoxy)-[1,8]-naphthyridin-2(1H)-one. US0167319; 2008
- Nicholson SL, Brotchie JM. 5-Hydroxytryptamine (5-HT, serotonin) and Parkinson's disease - opportunities for novel therapeutics to reduce the problems of levodopa therapy. Eur J Neurol 2002;9:1-6
- McIntyre JA, Castaner J, Bayes M. Sarizotan hydrochloride. Antidyskinetic drug 5-HT1A receptor agonist dopamine D2 receptor ligand. Drugs Future 2006;31:314-19
- Bronzova J, Sampaio C, Hauser RA, Double-blind study of pardoprunox, a new partial dopamine agonist, in early Parkinson's disease. Mov Disord 2010;25:730-8
- Goetz CG, Damier P, Hicking C, Sarizotan as a treatment for dyskinesias in Parkinson's disease: A double-blind placebo-controlled trial. Mov Disord 2007;22:179-86
- Asubio Pharma Co. Ltd. Agent for improving motor complications or psychiatric symptoms in Parkinson's disease. WO09069828; 2009
- Sumitomo Pharma. Novel benzoxazolone compounds. JP298402; 2005
- US. Department of veterans affairs. pharmacological treatment of Parkinson's disease. US0249621; 2007
- Atir Holding SA. Piperazine, piperidine and tetrahydropyridine derivatives and their pharmaceutical use. WO10137018; 2010
- Bliss TV, Collingridge GL. A synaptic model of memory: long-term potentiation in the hippocampus. Nature 1993;361:31-9
- Bowen DM, Francis PT, Chessell IP, Webster MT. Neurotransmission-the link integrating Alzheimer research? Trends Neurosci 1994;17:149-50
- Harder JA, Maclean CJ, Alder JT, The 5-HT1A antagonist, WAY-100635, ameliorates the cognitive impairment induced by fornix transection in the marmoset. Psychopharmacology (Berl) 1996;127:245-54
- Harder JA, Ridley RM. The 5-HT1A antagonist, WAY-100635, alleviates cognitive impairments induced by dizocilpine (MK-801) in monkeys. Neuropharmacology 2000;39:547-52
- Available from: http://clinicaltrials.gov/ct2/results?term=lecozotan [Last accessed 4 May 2012]
- Schechter LE, Smith DL, Rosenzweig-Lipson S, Lecozotan (SRA-333): a selective serotonin 1a receptor antagonist that enhances the stimulated release of glutamate and acetylcholine in the hippocampus and possesses cognitive-enhancing properties. J Pharmacol Exp Ther 2005;314:1274-89
- Lundbeck AS. Takeda Pharmaceuticals North America, Inc. Therapeutic uses of compounds having combined SERT, 5-HT3, and 5-HT1A activity. WO09062517; 2009
- Lundbeck AS. Novel therapeutic uses of 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine. WO08113359; 2008
- Lundbeck AS. 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine as a compound with combined serotonin reuptake, 5-HT3 and 5-HT1A activity for the treatment of cognitive impairment. WO07144005; 2007
- Available from: http://clinicaltrials.gov/ct2/results?term=Lu+aa21004 [Last accessed 4 May 2012]
- Bang-Andersen B, Ruhland T, Jørgensen M, Discovery of 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine (Lu AA21004): a novel multimodal compound for the treatment of major depressive disorder. J Med Chem 2011;54:3206-21
- Astra Zeneca AB. 2-carboxamide-7-piperazinyl-benzofuran derivatives. US0331341; 2010
- Wyeth. Method for enhancing cognitive function. WO07146073; 2007
- Colpaert FC. 5-HT1A receptor activation: new molecular and neuroadaptive mechanisms of pain relief. Curr Opin Investing Drugs 2006;7:40-7
- Song J, Christian K, Ming GL, Song H. Modification of hippocampal circuitry by adult neurogenesis. Dev Neurobiol 2012; published online 21 February 2012; doi: 10.1002/dneu.22014
- Klempin F, Babu H, De Pietri Tonelli D, Oppositional effects of serotonin receptors 5-HT1a, 2, and 2c in the regulation of adult hippocampal neurogenesis. Front Mol Neurosci 2010;3:14
- Soumier A, Banasr M, Kerkerian-Le Goff L. Daszuta A Region- and phase-dependent effects of 5-HT1A and 5-HT2C receptor activation on adult neurogenesis. Eur Neuropsychopharmacol 2010;20:336-45
- BrainCells, Inc. 5-HT receptor mediated neurogenesis. US0009983; 2010
- BrainCells, Inc. 5-HT receptor mediated neurogenesis. WO07134077; 2007
- BrainCells, Inc. Modulation of neurogenesis with use of modafinil. WO08086483; 2008
- Hilleman DE, Mohiuddin SM, Del Core MG, Sketch MH Sr. Effect of buspirone on withdrawal symptoms associated with smoking cessation. Arch Intern Med 1992;152:350-2
- Farid P, Abate MA. Buspirone use for smoking cessation. Ann Pharmacother 1998;32:1362-4
- Thassin Thomas. Artificial reproduction of pharmaceutical conditions of dependency to tobacco and other addictive drugs (opiacea, psychostimulants, alcohol) by combination of nicotine and a ligand (agonist or antagonist) of 5-HT1A receptors. WO09090556; 2009
- Rose JS, Branchey M, Wallach L, Buydens-Branchey L. Effects of buspirone in withdrawal from opiates. Am J Addict 2003;12:253-9
- Meanwell NA. Synopsis of some recent tactical application of bioisosteres in drug design. J Med Chem 2011;54:2529-91
- Levine LR, Potter WZ. The 5-HTlA receptor: an unkept promise? In: Briley M, Nutt D, Editors Anxiolytics. Birkhauser Verlag; Basel, Boston, Berlin: 2000
- Assie MB, Bardin L, Auclair AL, F15599, a highly selective post-synaptic 5-HT1A receptor agonist: in-vivo profile in behavioural models of antidepressant and serotonergic activity. Int J Neuropsychopharmacol 2010;13:1285-98
- Available from: https://www.clinicaltrialsregister.eu/ctr-search/search?query=eudract_number:2009-012123-28 [Last accessed 4 May 2012]
- Sampaio C, Bronzova J, Hauser RA, Pardoprunox in early Parkinson's disease: results from 2 large, randomized double-blind trials. Mov Disord 2011;26:1464-76
- Available from: http://clinicaltrials.gov/ct2/results?term=flibanserin [Last accessed 4 May 2012]
- Available from: http://clinicaltrials.gov/ct2/results?term=GSK958108 [Last accessed May 2012]