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Tachykinin receptor antagonists in clinical trials

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Pages 1843-1864 | Published online: 25 Nov 2009

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Guy Boeckxstaens, Pere Clavé, Enrico S Corazziari & Jan Tack. (2014) Irritable bowel syndrome: focus on otilonium bromide. Expert Review of Gastroenterology & Hepatology 8:2, pages 131-137.
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Maria Altamura. (2012) Tachykinin NK2 receptor antagonists. A patent review (2006 – 2010). Expert Opinion on Therapeutic Patents 22:1, pages 57-77.
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Mario Pellegatti & Sabrina Pagliarusco. (2011) Drug and metabolite concentrations in tissues in relationship to tissue adverse findings: a review. Expert Opinion on Drug Metabolism & Toxicology 7:2, pages 137-146.
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Articles from other publishers (56)

Yasir Dilshad Siddiqui, Xuguang Nie, Sheng Wang, Yasaman Abbasi, Lauren Park, Xiaoxuan Fan, Vivek Thumbigere-Math & Man-Kyo Chung. (2023) Substance P aggravates ligature-induced periodontitis in mice. Frontiers in Immunology 14.
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Antonio Florido, Estefanía Moreno, Enric I. Canela & Raül Andero. (2022) Nk3R blockade has sex-divergent effects on memory in mice. Biology of Sex Differences 13:1.
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Abbas AlAlikhan, Atefeh Ghahremanloo, Hossein Javid, Safieh Ebrahimi & Seyed Isaac Hashemy. (2022) The Effect of Blocking Neurokinin-1 Receptor by Aprepitant on the Inflammatory and Apoptosis Pathways in Human Ovarian Cancer Cells. Cell Biochemistry and Biophysics 80:4, pages 819-827.
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Maryam Momen Razmgah, Atefeh Ghahremanloo, Hossein Javid, Abbas AlAlikhan, Amir-R Afshari & Seyed Isaac Hashemy. (2022) The effect of substance P and its specific antagonist (aprepitant) on the expression of MMP-2, MMP-9, VEGF, and VEGFR in ovarian cancer cells. Molecular Biology Reports 49:10, pages 9307-9314.
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Daniel Butler, Ines Ambite, Murphy Lam Yim Wan, Thi Hien Tran, Björn Wullt & Catharina Svanborg. (2022) Immunomodulation therapy offers new molecular strategies to treat UTI. Nature Reviews Urology 19:7, pages 419-437.
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Nan Wang, Jue Wang, Yongjing Zhang, Shiling Hu, Tianxiao Zhang, Yuanyuan Wu, Xiuzhen Sun, Tao Zhang, Shuanying Yang & Langchong He. (2021) Substance P‐induced lung inflammation in mice is mast cell dependent. Clinical & Experimental Allergy 52:1, pages 46-58.
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Atefeh Ghahremanloo, Hossein Javid, Amir R. Afshari & Seyed Isaac Hashemy. (2021) Investigation of the Role of Neurokinin-1 Receptor Inhibition Using Aprepitant in the Apoptotic Cell Death through PI3K/Akt/NF-κB Signal Transduction Pathways in Colon Cancer Cells. BioMed Research International 2021, pages 1-10.
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Amrita Mishra & Girdhari Lal. (2021) Neurokinin receptors and their implications in various autoimmune diseases. Current Research in Immunology 2, pages 66-78.
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Safieh Ebrahimi, Hosein Javid, Amin Alaei & Seyed Isaac Hashemy. (2020) New insight into the role of substance P/neurokinin‐1 receptor system in breast cancer progression and its crosstalk with microRNAs . Clinical Genetics 98:4, pages 322-330.
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Valentin S. Dorokhov, Yulia V. Nelyubina, Sema L. Ioffe & Alexey Yu. Sukhorukov. (2020) Asymmetric Synthesis of Merck’s Potent hNK 1 Antagonist and Its Stereoisomers via Tandem Acylation/[3,3]-Rearrangement of 1,2-Oxazine N -Oxides . The Journal of Organic Chemistry 85:17, pages 11060-11071.
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Paweł K. Halik, Piotr F. J. Lipiński, Joanna Matalińska, Przemysław Koźmiński, Aleksandra Misicka & Ewa Gniazdowska. (2020) Radiochemical Synthesis and Evaluation of Novel Radioconjugates of Neurokinin 1 Receptor Antagonist Aprepitant Dedicated for NK1R-Positive Tumors. Molecules 25:16, pages 3756.
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Paulina D. Ramírez-García, Jeffri S. Retamal, Priyank Shenoy, Wendy Imlach, Matthew Sykes, Nghia Truong, Luis Constandil, Teresa Pelissier, Cameron J. Nowell, Song Y. Khor, Louis M. Layani, Chris Lumb, Daniel P. Poole, TinaMarie Lieu, Gregory D. Stewart, Quynh N. Mai, Dane D. Jensen, Rocco Latorre, Nicole N. Scheff, Brian L. Schmidt, John F. Quinn, Michael R. Whittaker, Nicholas A. Veldhuis, Thomas P. Davis & Nigel W. Bunnett. (2019) A pH-responsive nanoparticle targets the neurokinin 1 receptor in endosomes to prevent chronic pain. Nature Nanotechnology 14:12, pages 1150-1159.
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Michael Stassen, Ann-Kathrin Hartmann, Sharon Jiménez Delgado, Susann Dehmel & Armin Braun. (2019) Mast cells within cellular networks. Journal of Allergy and Clinical Immunology 144:4, pages S46-S54.
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Chentao GeHemiao HuangFeiyan HuangTianxin YangTengfei ZhangHongzhang WuHanwei ZhouQi ChenYue ShiYanfang SunLiangjue LiuXi WangRichard B. PearsonYihai Cao, Jian Kang & Caiyun Fu. (2019) Neurokinin-1 receptor is an effective target for treating leukemia by inducing oxidative stress through mitochondrial calcium overload. Proceedings of the National Academy of Sciences 116:39, pages 19635-19645.
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Agnieszka Majkowska-Pilip, Paweł Krzysztof Halik & Ewa Gniazdowska. (2019) The Significance of NK1 Receptor Ligands and Their Application in Targeted Radionuclide Tumour Therapy. Pharmaceutics 11:9, pages 443.
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Jie YinKaren ChapmanLindsay D. ClarkZhenhua ShaoDominika Borek, Qingping XuJunmei Wang & Daniel M. Rosenbaum. (2018) Crystal structure of the human NK 1 tachykinin receptor . Proceedings of the National Academy of Sciences 115:52, pages 13264-13269.
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Esra Nizam & Nuray Erin. (2018) Differential consequences of neurokinin receptor 1 and 2 antagonists in metastatic breast carcinoma cells; Effects independent of Substance P. Biomedicine & Pharmacotherapy 108, pages 263-270.
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Sergei Spitsin, Vasiliki Pappa & Steven D Douglas. (2018) Truncation of neurokinin-1 receptor—Negative regulation of substance P signaling. Journal of Leukocyte Biology 103:6, pages 1043-1051.
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Adil E. Bharucha & Simon J.H. Brookes. 2018. Physiology of the Gastrointestinal Tract. Physiology of the Gastrointestinal Tract 517 564 .
J Tack, K Schumacher, G Tonini, S Scartoni, A Capriati & C A Maggi. (2017) The neurokinin-2 receptor antagonist ibodutant improves overall symptoms, abdominal pain and stool pattern in female patients in a phase II study of diarrhoea-predominant IBS. Gut 66:8, pages 1403-1413.
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M. Brittany Johnson, Ada D. Young & Ian Marriott. (2017) The Therapeutic Potential of Targeting Substance P/NK-1R Interactions in Inflammatory CNS Disorders. Frontiers in Cellular Neuroscience 10.
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Hydar Ali. 2017. G Protein-Coupled Receptors in Immune Response and Regulation. G Protein-Coupled Receptors in Immune Response and Regulation 123 162 .
Samaneh Bayati, Davood Bashash, Shahin Ahmadian, Ava Safaroghli-Azar, Kamran Alimoghaddam, Ardeshir Ghavamzadeh & Seyed H. Ghaffari. (2016) Inhibition of tachykinin NK1 receptor using aprepitant induces apoptotic cell death and G1 arrest through Akt/p53 axis in pre-B acute lymphoblastic leukemia cells. European Journal of Pharmacology 791, pages 274-283.
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Ehsan Azimi, Vemuri B. Reddy, Kai-Ting C. Shade, Robert M. Anthony, Sebastien Talbot, Paula Juliana Seadi Pereira & Ethan A. Lerner. (2016) Dual action of neurokinin-1 antagonists on Mas-related GPCRs. JCI Insight 1:16.
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Sattar Ostadhadi, Ehsan Azimi, Ethan A. Lerner & Ahmad-Reza Dehpour. (2016) Are itch and scratching the nausea and vomiting of skin?. Experimental Dermatology 25:5, pages 340-343.
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Yu Zhou, Jiang Wang, Zhanni Gu, Shuni Wang, Wei Zhu, José Luis Aceña, Vadim A. Soloshonok, Kunisuke Izawa & Hong Liu. (2016) Next Generation of Fluorine-Containing Pharmaceuticals, Compounds Currently in Phase II–III Clinical Trials of Major Pharmaceutical Companies: New Structural Trends and Therapeutic Areas. Chemical Reviews 116:2, pages 422-518.
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M. Corsetti, F. Akyuz & J. Tack. (2015) Targeting tachykinin receptors for the treatment of functional gastrointestinal disorders with a focus on irritable bowel syndrome. Neurogastroenterology & Motility 27:10, pages 1354-1370.
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Li Li, Lei Zhao, Yang Wang, Ke-tao Ma, Wen-yan Shi, Ying-zi Wang & Jun-qiang Si. (2015) PKCɛ mediates substance P inhibition of GABAA receptors-mediated current in rat dorsal root ganglion. Journal of Huazhong University of Science and Technology [Medical Sciences] 35:1, pages 1-9.
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Pari Malherbe, Frédéric Knoflach, Anne Marcuz, Claudia Bohnert, Michael Weber, Henner Knust, Hasane Ratni, Will Spooren, Theresa M. Ballard & Caterina Bissantz. (2014) Mapping the binding pocket of a novel, high-affinity, slow dissociating tachykinin NK3 receptor antagonist: Biochemical and electrophysiological characterization. Neuropharmacology 86, pages 259-272.
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Jesse R. Schank. (2014) The Neurokinin-1 Receptor in Addictive Processes. Journal of Pharmacology and Experimental Therapeutics 351:1, pages 2-8.
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Mark J. Millan. (2013) On ‘polypharmacy’ and multi-target agents, complementary strategies for improving the treatment of depression: a comparative appraisal. The International Journal of Neuropsychopharmacology 17:07, pages 1009-1037.
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Dong Guo, Julia M. Hillger, Adriaan P. IJzerman & Laura H. Heitman. (2014) Drug-Target Residence Time-A Case for G Protein-Coupled Receptors. Medicinal Research Reviews 34:4, pages 856-892.
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Margit Pissarek. (2014) Neuropeptide Receptors in Pain Circuitries: Useful Targets for CNS Imaging with Non-Peptide Ligands Suitable for PET?. World Journal of Neuroscience 04:04, pages 353-383.
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Stephen Hanessian, Vincent Babonneau, Nicolas Boyer, Clotilde Mannoury la Cour, Mark J. Millan & Guillaume De Nanteuil. (2014) Design and synthesis of potential dual NK1/NK3 receptor antagonists. Bioorganic & Medicinal Chemistry Letters 24:2, pages 510-514.
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D. Ang, A. Pauwels, F. Akyuz, R. Vos & J. Tack. (2013) Influence of a neurokinin-1 receptor antagonist (aprepitant) on gastric sensorimotor function in healthy volunteers. Neurogastroenterology & Motility 25:12, pages e830-e838.
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Miguel Mu�oz. (2013) Antitumor activity of neurokinin-1 receptor antagonists in MG-63 human osteosarcoma xenografts. International Journal of Oncology.
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Erik T. te Beek, Justin L. Hay, Jonathan N. Bullman, Clare Burgess, Kimberly J. Nahon, Erica S. Klaassen, Frank A. Gray & Joop M. A. van Gerven. (2013) Pharmacokinetics and central nervous system effects of the novel dual NK 1 /NK 3 receptor antagonist GSK1144814 in alcohol-intoxicated volunteers . British Journal of Clinical Pharmacology 75:5, pages 1328-1339.
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Paolo Santicioli, Stefania Meini, Sandro Giuliani, Claudio Catalani, Paolo Bechi, Sara Riccadonna, Maria Novella Ringressi & Carlo Alberto Maggi. (2013) Characterization of ibodutant at NK2 receptor in human colon. European Journal of Pharmacology 702:1-3, pages 32-37.
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Jesse R. Schank, Andrey E. Ryabinin, William J. Giardino, Roberto Ciccocioppo & Markus Heilig. (2012) Stress-Related Neuropeptides and Addictive Behaviors: Beyond the Usual Suspects. Neuron 76:1, pages 192-208.
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Anna Rizzi, Barbara Campi, Valeria Camarda, Stefano Molinari, Sergio Cantoreggi, Domenico Regoli, Claudio Pietra & Girolamo Calo’. (2012) In vitro and in vivo pharmacological characterization of the novel NK1 receptor selective antagonist Netupitant. Peptides 37:1, pages 86-97.
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Hidemitsu Kitamura, Minoru Kobayashi, Daiko Wakita & Takashi Nishimura. (2012) Neuropeptide Signaling Activates Dendritic Cell-Mediated Type 1 Immune Responses through Neurokinin-2 Receptor. The Journal of Immunology 188:9, pages 4200-4208.
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J. E. Robinson, E. W. Fish, M. C. Krouse, A. Thorsell, M. Heilig & C. J. Malanga. (2011) Potentiation of brain stimulation reward by morphine: effects of neurokinin-1 receptor antagonism. Psychopharmacology 220:1, pages 215-224.
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L. Dai, D. S. Perera, D. W. King, B. R. Southwell, E. Burcher & L. Liu. (2011) Hemokinin-1 Stimulates Prostaglandin E2 Production in Human Colon through Activation of Cyclooxygenase-2 and Inhibition of 15-Hydroxyprostaglandin Dehydrogenase. Journal of Pharmacology and Experimental Therapeutics 340:1, pages 27-36.
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Marisa Rosso, Miguel Muñoz & Michael Berger. (2012) The Role of Neurokinin-1 Receptor in the Microenvironment of Inflammation and Cancer. The Scientific World Journal 2012, pages 1-21.
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Guy Griebel & Sandra Beeské. (2012) Is there still a future for neurokinin 3 receptor antagonists as potential drugs for the treatment of psychiatric diseases?. Pharmacology & Therapeutics 133:1, pages 116-123.
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Adil E. Bharucha & Simon J.H. Brookes. 2012. Physiology of the Gastrointestinal Tract. Physiology of the Gastrointestinal Tract 977 1022 .
Cecilio Lopez-Munoz & Francisco AlamoTih-Shih Lee & K Krishnan. 2011. Neurobiology of Depression. Neurobiology of Depression 317 324 .
Joop van Gerven & Adam Cohen. (2011) Vanishing clinical psychopharmacology. British Journal of Clinical Pharmacology 72:1, pages 1-5.
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Hui Xiong, James Kang, James M. Woods, John P. McCauleyJr.Jr., Gerard M. Koether, Jeffrey S. Albert, Lindsay Hinkley, Yan Li, Reto A. Gadient & Thomas R. Simpson. (2011) Synthesis and SAR of sulfoxide substituted carboxyquinolines as NK3 receptor antagonists. Bioorganic & Medicinal Chemistry Letters 21:6, pages 1896-1899.
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Sabrina Pagliarusco, Silvia Martinucci, Ellenia Bordini, Lidia Miraglia, Domenico Cufari, Luca Ferrari & Mario Pellegatti. (2011) Tissue Distribution and Characterization of Drug-Related Material in Rats and Dogs after Repeated Oral Administration of Casopitant. Drug Metabolism and Disposition 39:2, pages 283-293.
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P Malherbe, F Knoflach, MC Hernandez, T Hoffmann, P Schnider, RH Porter, JG Wettstein, TM Ballard, W Spooren & L Steward. (2011) Characterization of RO4583298 as a novel potent, dual antagonist with in vivo activity at tachykinin NK1 and NK3 receptors. British Journal of Pharmacology 162:4, pages 929-946.
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G. Cipriani, P. Santicioli, S. Evangelista, C. A. Maggi, S. Riccadonna, M. N. Ringressi, P. Bechi, M. S. Faussone-Pellegrini & M. G. Vannucchi. (2011) Effect of otilonium bromide and ibodutant on the internalization of the NK2 receptor in human colon. Neurogastroenterology & Motility 23:1, pages 96-e10.
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Luca Ferrari, Daniela Reami & Marco Michi. (2010) Determination of casopitant and its three major metabolites in dog and rat plasma by positive ion liquid chromatography/tandem mass spectrometry. Journal of Chromatography B 878:29, pages 2974-2982.
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Linda Monaco-Shawver, Lynnae Schwartz, Florin Tuluc, Chang-Jiang Guo, Jian Ping Lai, Satya M Gunnam, Laurie E Kilpatrick, Pinaki P Banerjee, Steven D Douglas & Jordan S Orange. (2011) Substance P inhibits natural killer cell cytotoxicity through the neurokinin-1 receptor. Journal of Leukocyte Biology 89:1, pages 113-125.
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Mark J. Millan, Anne Dekeyne, Alain Gobert, Clotilde Mannoury la Cour, Mauricette Brocco, Jean-Michel Rivet, Benjamin Di Cara, Françoise Lejeune, Thomas I. Cremers, Gunnar Flik, Trynke R. de Jong, Berend Olivier & Guillaume de Nanteuil. (2010) S41744, a dual neurokinin (NK)1 receptor antagonist and serotonin (5-HT) reuptake inhibitor with potential antidepressant properties: A comparison to aprepitant (MK869) and paroxetine. European Neuropsychopharmacology 20:9, pages 599-621.
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J. Culman, G. Das, C. Ohlendorf, M. Haass, C. Maser‐Gluth, M. Zuhayra, Y. Zhao & K. Itoi. (2010) Blockade of Tachykinin NK 1 /NK 2 Receptors in the Brain Attenuates the Activation of Corticotrophin‐Releasing Hormone Neurones in the Hypothalamic Paraventricular Nucleus and the Sympathoadrenal and Pituitary‐Adrenal Responses to Formalin‐Induced Pain in the Rat . Journal of Neuroendocrinology 22:5, pages 467-476.
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