5-HT₃ antagonists under development

Bibliography

• Bonate PL. Serotonin receptors subtypes – functional, physiological, and clinical coorelates. Clin Neuropharmacol 1991;14:1-16
   PubMed Web of Science ®Google Scholar
• Whitaker-Azmitia PM. The discovery of serotonin and its role in neuroscience. Neuropsychopharmacology 1999;21:S2-8
   PubMed Web of Science ®Google Scholar
• Hoyer D, Hannon JP, Martin GR. Molecular, pharmacological and functional diversity of 5-HT receptors. Pharmcol Biochem Behav 2002;71:533-54
   PubMed Web of Science ®Google Scholar
• Keramidas A, Moorhouse AJ, Schofield PR, Ligand-gated ion channels: mechanisms underlying ion selectivity. Prog Biophys Mol Biol 2004;86:161-204
   PubMed Web of Science ®Google Scholar
• Lummis SCR, The transmembrane domain of the 5-HT3 receptor: its role in selectivity and gating. Biochem Soc Trans 2004;32:535-9
   PubMed Web of Science ®Google Scholar
• Monyer H, Inta D. Serotonin 5-HT3A receptors in treatment of neurological and psychiatric disorders. WO2008/020334; 2008
   Google Scholar
• Tyers MB, Freeman AJ. Mechanism of the anti-emetic activity of 5-HT3 receptor antagonists. Oncology 1992;49:263-8
   PubMed Web of Science ®Google Scholar
• Seynaeve C, Verweij J, Demulder PHM. 5-HT3 receptor antagonists, a new approach in emesis-A review of ondansetron, granisetron and tropisetron. Anti-Cancer Drug 1991;2:343-55
   PubMed Web of Science ®Google Scholar
• Aapro MS. 5-HT3 receptor antagonists – an overview of their present status and future potential in cancer therapy-induced emesis. Drugs 1991;42:551-68
   PubMed Web of Science ®Google Scholar
• Gyermek L. 5-HT3 receptors-Pharmacological and therapeutic aspects. J Clin Pharmacol 1995;35:845-55
   PubMed Web of Science ®Google Scholar
• Perez EA. A risk-benefict assessment of serotonin 5-HT3 receptor antagonists in antineoplastic therapy-induced emesis. Drug Safty 1998;18:43-56
   PubMed Web of Science ®Google Scholar
• Humphrey PP, Bountra C, Clayton N, The therapeutic potential of 5-HT3 receptor antagonists in the treatment of irritable bowel symdrome. Aliment pharmacol Ther 1999;132:31-8
   Google Scholar
• Mayer EA, Bradesi S. Alosetron and irritable bowel syndrome. Expert Opin Pharmaco 2003;4:2089-98
   PubMed Web of Science ®Google Scholar
• Mucke H, Cole P, Rabasseda X. Alosetron. Drug Today 2000;36:595-607
   PubMed Web of Science ®Google Scholar
• Spiller R. Serotonergic modulating drugs for functional gastrointestinal diseases. Br J Clin Pharmacol 2002;54:11-20
   PubMed Web of Science ®Google Scholar
• Thompson AJ, Lummis SCR. 5-HT3 receptors. Curr Pharm Design 2006;12:3615-30
   PubMed Web of Science ®Google Scholar
• Kelley SP, Bratt AM, Hodge CW. Targeted gene deletion of the 5-HT3A receptor subunit produces an anxiolytic phenotype in mice. Eur J Pharmacol 2003;461:19-25
   PubMed Web of Science ®Google Scholar
• Bhatnagar S, Nowak N, Babich L, Deletion of the 5-HT3 receptor differentially affects behavior of males and females in the Porsolt forced swim and defensive withdrawal test. Behav Brain Res 2004;153:527-35
   PubMed Web of Science ®Google Scholar
• Barnes NM, Costall B, Ge J, The interaction of R(+)- and S(–)-zacopride with PCPA to modify rodent aversive behavior. Eur J Pharmacol 1992;218:15-25
   PubMed Web of Science ®Google Scholar
• Rammes G, Eisensamer B, Ferrari U, Antipsychotic drugs antagonize human serotonin type 3 receptor currents in a noncompetitive manner. Mol Psychiat 2004;9:846-58
   PubMed Web of Science ®Google Scholar
• Hodge CW, Samson HH, Lewis RS, Specific decreases in ethanol – but not water-reinforced responding produced by the 5-HT3 antagonist ICS205-930. Alcohol 1993;10:191-6
   PubMed Web of Science ®Google Scholar
• Silvestre JS, Palacios JM, Fernandez AG, Comparison of effects of a range of 5-HT receptor modulators on consumption and preference for a sweetened ethanol solution in rats. J Psychopharmacol 1998;12:168-76
   PubMed Web of Science ®Google Scholar
• Depoortere RY, Li DH, Lane JD, Parameters of self-administraion of cocaine in rats under a progressive ratio schedule. Pharmacol Biochem Behav 1993;45:539-48
   PubMed Web of Science ®Google Scholar
• Peltier R, Schenk S. GR38032F, a serotonin 5-HT3 antagonist fails to alter cocaine self-administration in rats. Pharmacol Biochem Behav 1991;39:133-6
   PubMed Web of Science ®Google Scholar
• Johnson BA, Roache JD, Javors MA, Ondansetron for reduction of drinking among biologically predisposed alcoholic patients: a randomized controlled trial. JAMA 2000;284:963-71
   PubMed Web of Science ®Google Scholar
• Akerele EO, Levin FR. Substance abuse among patients with schizophrenia. J Psychiatr Pract 2002;8:70-80
   PubMedGoogle Scholar
• Phillips P, Johnson S. How does drug and alcohol misuse develop among people with psychotic illness? A literature review. Soc Psych Psych Epid 2001;36:269-76
   PubMed Web of Science ®Google Scholar
• Rabasseda X, Mealy N, Castaner J. N-3389. Drugs Fut 1995;20:780
   Google Scholar
• Graul A, Gastaner J. RS-25259-197 Drugs Fut 1996;21:906
   Google Scholar
• Galvan M, Gittos MW, Fatmi M. Dolasetron Mesylate. Drugs Fut 1993;18:506
   Google Scholar
• Ohta M, Miyata K. YM060. Drugs Fut 1992;17:28
   Google Scholar
• Prous J, Castaner J. Azasetron hydochloride. Drugs Fut 1993;18:206
   Google Scholar
• Milne RJ, Heel RC. Ondansetron-therapeutic use as an antiemetic. Drugs 1991;41:574-95
   PubMed Web of Science ®Google Scholar
• Aapro M. Granisetron: an update on its clinical use in the management of nausea and vomiting. Oncologist 2004;9:673-86
   PubMed Web of Science ®Google Scholar
• Duggan ST, Curran MP. Transdermal granisetron. Drugs 2009;69:2597-605
   PubMed Web of Science ®Google Scholar
• Orjales A, Garcia N, Rubio-Royo V, 2-Piperazinylbenzimidazole derivatives. EP0512939; 1999
   Google Scholar
• Orjales A, Mosquera R, Labeaga L, New 2-piperazinylbenzimidazole derivatives as 5-HT3 antagonists. Synthesis and pharmacological evaluation. J Med Chem 1997;40:586-93
   PubMed Web of Science ®Google Scholar
• Jauregiza N, Calvo R, Suarez E, Pharmacokinetics and pharmacological effect of lerisetron, a new 5-HT3 antagonist, in rats. J Pharm Sci US 2002;91:41-52
   PubMed Web of Science ®Google Scholar
• Airey JE, Studt WL, Powers MR, Process for preparing muticyclic oxy-containing ring components. WO9209592; 1992
   Google Scholar
• Martin GE, Chase BJ, Davis MA, Potent 5-hydroxytryptamine3 receptor antagonist activity of RG-12915. Drug Developt Res 1993;28:38-46
   Web of Science ®Google Scholar
• Cohen ML, Lacefield WB. Improvements in or relating to specific 5-HT3 antagonists. EP0307172; 1988
   Google Scholar
• Robertson DW, Lacefield WB, Bloomquist W, Zatosetron, a potent, selective, and long-acting 5-HT3 receptor antagonist: synthesis and structure-activity relationships. J Med Chem 1992;35:310-19
   PubMed Web of Science ®Google Scholar
• Schwartz SM, Goldberg MJ, Gidda JS, Effect of zatosetron on ipecac-induced emesis in dogs and healthy men. J Clin pharmacol 1994;34:250-4
   PubMed Web of Science ®Google Scholar
• Rabasseda X, Leeson P, Silvestre J, Cilansetron. Drugs Fut 1999;24:475-82
   Google Scholar
• CILANSETRON; Solvay Pharmaceuticals suspends registration activites in the U.S., while discussions in Europe continue Brussels, Belgium: Solvay press, 2005. Available from: http://www.solvaypress.com/pressreleases/0,,36423-2-0,00.htm#contact [Last accessed 5 October 2010]
   Google Scholar
• Turconi M, Donetti A, Montagna E, Benzimidazoline-2-oxo-1-carboxylic acid compounds useful as 5-HT receptor antagonists. US5223511; 1993, EP309423; 1994
   Google Scholar
• Turconi M, Sagrada A. New use of 5-HT3 receptor antagonists. WO1994013284; 1994
   Google Scholar
• Brambilla A, Turconi M, Schiantarelli P, Use of benzimidazoline-2-oxo-1-carboxylic acid derivatives in the treatment of organic mental diseases. EP523013; 1992
   Google Scholar
• Noverola AV, Soto JMP, Noguera FP, Improvements relating to N-substituted benzamides. EP0302699; 1988
   Google Scholar
• Fernandez AG, Puig J, Beleta J, Pancopride, a potent and long-acting 5-HT3 receptor antagonist, is orally effective against anticancer drug-evoked emesis. Eur J Pharmacol 1992;222:257-64
   PubMed Web of Science ®Google Scholar
• Monkovic I, Willner D. Pharmacologically active substituted benzamides. US4808624; 1989
   Google Scholar
• Yamakuni H, Nakayama H, Matsui S, Inhibitory effect of zacopride on cisplatin-induced delayed emesis in Ferrets. J Pharmacol Sci 2006;101:99-102
   PubMed Web of Science ®Google Scholar
• Depoortere H. (R)-zacopride or a salt for pharmaceuticals in treatment of sleep apnea. EP1090638; 2001
   Google Scholar
• Carley DW, Depoortere H, Radulovacki M. R-zacopride, a 5-HT3 antagonist/5-HT4 agonist, reduces sleep apneas in rats. Pharmacol Biochem Behav 2001;69:283-9
   PubMed Web of Science ®Google Scholar
• King F, Joiner K. Indole derivatives having an azabicyclic side chain, process for their preparation, intermediates, and pharmaceutical compositions. EP0247266; 1993
   Google Scholar
• Blackburn TP, Baxter GS, Kennett GA, BRL 46470A: a highly potent, selective and long acting 5-HT3 receptor antagonist with anxiolytic-like properties. Psychopharmaocol 1993;110:257-64
   PubMed Web of Science ®Google Scholar
• Kon T, Kato S, Morie T, Indazole-3-carboxylic acid derivatives. EP358903; 1990
   Google Scholar
• Yoshida N, Omoya H, Ito T. DAT-582, a novel serotonin3 receptor antagonist, is a potent and long-lasting antiemetic agent in the ferret and dog. J Pharmacol Exp Ther 1992;260:1159-65
   PubMed Web of Science ®Google Scholar
• Nagakura Y, Kadowaki M, Tokoro K, Pharmacological characterization of FK1052, a dihydropyridoindole derivative, as a new serotonin 3 and 4 dual receptor antagonist. J Pharmacol Exp Ther 1993;265:752-8
   PubMed Web of Science ®Google Scholar
• Nakayama H, Yanakuni H, Higaki M, Antiemetic activity of FK1052, a 5-HT3- and 5-HT4-receptor antagonist, in Suncus murinus nad ferrets. J Pharmacol Sci 2005;98:396-403
   PubMed Web of Science ®Google Scholar
• Yamano M, Kamato T, Nishida A, Serotonin (5-HT)3-receptor antagonism of 4,5,6,7-tetrahydrobenzimidazole derivatives against 5-HT-induced bradycardia in anesthetized rats. Jpn J Pharmacol 1994;65:241-8
   PubMedGoogle Scholar
• Munson HR Jr, Lo YS. Synthesis of 4-amino-1,2-hydrocarbyl pyrazolidines via 4-nitro analogs. US4358599; 1982
   Google Scholar
• Grant SC, Kris MG, Gralla RJ, Dose-ranging evaluation of the substituted benzamide dazopride when used as an antiemetic in patients receiving anticancer chemotherapy. Cancer Chemother Pharmacol 1993;31:442-4
   PubMed Web of Science ®Google Scholar
• Logue J, Wilkinson P, Haegele KD, A single-dose-finding study of the antiemetic effect and associated plasma-levels of MDL-72222 in patients receiving cisplatin. Cancer Chemother Phamcol 1991;27:472-6
   PubMed Web of Science ®Google Scholar
• Homesley HD, Hahne WF, McLees B, Randomized comparison of the antiemetic efficacy of a serotonin type 3 receptor antagonist (MDL 72,222) with a high-dose metoclopriamide regimen. Am J Clin Oncology 1993;16:175-9
   PubMed Web of Science ®Google Scholar
• Okegawa T, Kawamura M. Isoquinolinone derivative. EP0482939; 1992
   Google Scholar
• Matsui T, Sugiura T, Nakai H, Novel 5-HT3 antagonists. Isoauinolinones and 3-aryl-2-pyridones. J Med Chem 1992;35:3307-19
   PubMed Web of Science ®Google Scholar
• Ward R, White J. Heterocyclic compounds. WO9105783, EP0494978; 1991
   Google Scholar
• Middlefell VC, Bill DJ, Brammer NT, WAY-SEC-597: a novel 5-HT3 receptor antagonist. CNS Drug Reviews 1996;2:269-93
   Google Scholar
• Arnsten AF, Lin CH, Van Dyck CH, The effects of 5-HT3 receptor antagonists on cognitive performance in aged monkeys. Neurobiol Aging 1997;18:21-8
   PubMed Web of Science ®Google Scholar
• Eglen RM, Lee CH, Smith WL, RS 42358-197, a novel and potent 5-HT3 receptor antagonist, in vitro and in vivo. J Pharmacol Exp Ther 1993;266:535-43
   PubMed Web of Science ®Google Scholar
• Clark RD, Miller AB, Berger J, 2-(Quinuclidin-3-yl)pyrido[4,3-b]indol-1-ones and isoquinolin-1-ones. Potent conformationally restricted 5-HT3 receptor antagonists. J Med Chem 1993;26:2645-57
   Web of Science ®Google Scholar
• Bonhaus DW, Wong EHF, Stefanich E, Pharmacological characterization of 5-hydroxytryptamine3 receptors in murine brain and ileum using the novel radioligand [3H]RS-42358-197: evidence for receptor heterogeity. J Neurochem 1993;61:1927-32
   PubMed Web of Science ®Google Scholar
• Ward TJ, White JC. Aroyl-ureas. EP0422846; 1991
   Google Scholar
• Bradley G, Ward TJ, White JC, Novel antagonists of the 5-HT3 receptor. Synthesis and structure-activity relationships of (2-alkoxybenzoyl)ureas. J Med Chem 1992;35:1515-20
   PubMed Web of Science ®Google Scholar
• Rhodes KF, Middlefell VC, Lattimer N, WAY 100289: Pharmacological profile of a novel 5-HT3 receptor antagonist. Drug Develop Res 1993;28:128-40
   Web of Science ®Google Scholar
• Turconi M, Donetti A, Montagna E, Benzimidazoline-2-oxo-1-carboxylic acid compounds useful as 5-HT receptor antagonists. US 5223511; 1993
   Google Scholar
• Turconi M, Nicola M, Quintero MG, Synthesis of a new class of 2,3-dihydro-2-oxo-1H-bnezimidazole-1-carboxylic acid derivatives as highly potent 5-HT3 receptor antagonists. J Med Chem 1990;33:2101-8
   PubMed Web of Science ®Google Scholar
• Rizzi CA, Sagrada A, Schiavone A, Gastroporkinetic properties of the benzimidazolone derivative BIMU 1, an agonist at 5-hydroxytryptamine4 and antagonist at 5-hydroxytryptamine3. N-S Arch Pharmacol 1994;349:338-45
   PubMedGoogle Scholar
• Pijpers F. Pipeline and commercial insight: Supportive care in oncology, Datamonitor Report 2009; DMHC2557; 186-238
   Google Scholar
• Osoba D. Current applications of health-related quality-of-life assessment in oncology. Support Care Cancer 1997;5:307-13
   PubMed Web of Science ®Google Scholar
• Laszlo J. Cotanch PH. Managing chemotherapy-induced nausea and vomiting – a paradigm supportive care. Cancer 1992;70:1007-11
   PubMed Web of Science ®Google Scholar
• Schmitt R. Quality-of-life issues in lung-cancer-New symptom management strategies. Chest 1993;103:S51-5
   PubMed Web of Science ®Google Scholar
• De La Vega L, Munoz E, Calzado MA, The 5-HT3 receptor antagonist tropisetron inhibits T cell activation by targeting the calcineurin pathway. Biochem Pharmcol 2005;70:369-80
   PubMed Web of Science ®Google Scholar
• Fiebich BL, Akundi RS, Lieb K, Anti-inflammatory effects of 5-HT3 receptor antagonists in lipopolysaccharide-stimulated primary human monocytes. Scand J Rheumatol 2004;33:28-32
   Web of Science ®Google Scholar
• Schneider EM, Ma X, Stratz T, Immunomodulatory function of the 5-HT3 receptor antagonist tropisetron. Scand J Rheumatol 2004;s119:34-40
   Web of Science ®Google Scholar
• Seidel MF, Ulrich-Merzenich G, Fiebich BL, Tropisetron inhibits serotonin-induced PGE2 release from macrophage-like synovial cells in serum-free tissue culture. Scand J Rheumatol Suppl 2004;119:33
   PubMedGoogle Scholar
• Oatway MA, Chen Y, Weaver LC. The 5-HT3 receptor facilitates at-level mechanical allodynia following spinal cord injury. Pain 2004;110:259-68
   PubMed Web of Science ®Google Scholar