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Expert Opinion on Therapeutic Patents Volume 20, 2010 - Issue 9
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Reviews

Recent advances in histamine H3 receptor antagonists/inverse agonists

Dorota Łażewska Jagiellonian University Medical College, Department of Technology and Biotechnology of Drugs, ul. Medyczna 9, 30-688 Kraków, Poland
&
Katarzyna Kieć-Kononowicz Jagiellonian University Medical College, Department of Technology and Biotechnology of Drugs, ul. Medyczna 9, 30-688 Kraków, Poland +48 12 620 55 80; + 48 12 620 55 94; [email protected]
Pages 1147-1169 | Published online: 18 Aug 2010

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Dorota Łażewska & Katarzyna Kieć-Kononowicz. (2018) Progress in the development of histamine H3 receptor antagonists/inverse agonists: a patent review (2013-2017). Expert Opinion on Therapeutic Patents 28:3, pages 175-196.
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Dorota Łażewska & Katarzyna Kieć-Kononowicz. (2014) New developments around histamine H3 receptor antagonists/inverse agonists: a patent review (2010 – present). Expert Opinion on Therapeutic Patents 24:1, pages 89-111.
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Sebastiaan Kuhne, Maikel Wijtmans, Herman D Lim, Rob Leurs & Iwan JP de Esch. (2011) Several down, a few to go: histamine H3 receptor ligands making the final push towards the market?. Expert Opinion on Investigational Drugs 20:12, pages 1629-1648.
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Peter Norman. (2011) New H1/H3 antagonists for treating allergic rhinitis: WO2010094643. Expert Opinion on Therapeutic Patents 21:3, pages 425-429.
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Patricia Di Ciano, Christian S. Hendershot & Bernard Le Foll. 2022. The Functional Roles of Histamine Receptors. The Functional Roles of Histamine Receptors 169 191 .
Fernando Valenzuela & Rodrigo Flores. (2021) Antihistamínicos: Usos clásicos, nuevos y anecdóticos en dermatología. Parte 1: Histamina, sus receptores y antagonistas. Piel 36:2, pages 95-103.
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Leonardo David Herrera-Zúñiga, Liliana Marisol Moreno-Vargas, Luck Ballaud, José Correa-Basurto, Diego Prada-Gracia, David Pastré, Patrick A. Curmi, Jean Michel Arrang & Rachid C. Maroun. (2020) Molecular dynamics of the histamine H3 membrane receptor reveals different mechanisms of GPCR signal transduction. Scientific Reports 10:1.
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Rim Malek, Raquel L. Arribas, Alejandra Palomino-Antolin, Perle Totoson, Celine Demougeot, Tereza Kobrlova, Ondrej Soukup, Isabel Iriepa, Ignacio Moraleda, Daniel Diez-Iriepa, Justyna Godyń, Dawid Panek, Barbara Malawska, Monika Głuch-Lutwin, Barbara Mordyl, Agata Siwek, Fakher Chabchoub, José Marco-Contelles, Katarzyna Kiec-Kononowicz, Javier Egea, Cristóbal de los Ríos & Lhassane Ismaili. (2019) New Dual Small Molecules for Alzheimer’s Disease Therapy Combining Histamine H 3 Receptor (H3R) Antagonism and Calcium Channels Blockade with Additional Cholinesterase Inhibition . Journal of Medicinal Chemistry 62:24, pages 11416-11422.
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Nakisa Ghamari, Omid Zarei, José-Antonio Arias-Montaño, David Reiner, Siavoush Dastmalchi, Holger Stark & Maryam Hamzeh-Mivehroud. (2019) Histamine H3 receptor antagonists/inverse agonists: Where do they go?. Pharmacology & Therapeutics 200, pages 69-84.
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Anne C. Baakman, Rob Zuiker, Joop M.A. Gerven, Nicholas Gross, Ronghua Yang, Michael Fetell, Ari Gershon, Yossi Gilgun‐Sherki, Edward Hellriegel & Ofer Spiegelstein. (2019) Central nervous system effects of the histamine‐3 receptor antagonist CEP‐26401, in comparison with modafinil and donepezil, after a single dose in a cross‐over study in healthy volunteers. British Journal of Clinical Pharmacology 85:5, pages 970-985.
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Anirban Ghoshal, Ajeet Kumar, Doddapaneni Yugandhar, Chandan Sona, Sunu Kuriakose, Kommu Nagesh, Mamunur Rashid, Sandeep K. Singh, Muhammad Wahajuddin, Prem N. Yadav & Ajay K. Srivastava. (2018) Identification of novel β-lactams and pyrrolidinone derivatives as selective Histamine-3 receptor (H3R) modulators as possible anti-obesity agents. European Journal of Medicinal Chemistry 152, pages 148-159.
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Dorota Łażewska, Maria Kaleta, Stefanie Hagenow, Szczepan Mogilski, Gniewomir Latacz, Tadeusz Karcz, Annamaria Lubelska, Ewelina Honkisz, Jadwiga Handzlik, David Reiner, Grzegorz Satała, Barbara Filipek, Holger Stark & Katarzyna Kieć-Kononowicz. (2018) Novel naphthyloxy derivatives – Potent histamine H3 receptor ligands. Synthesis and pharmacological evaluation. Bioorganic & Medicinal Chemistry 26:9, pages 2573-2585.
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Yu-Jeong Kim, Yukiori Goto & Young-A Lee. (2018) Histamine H3 receptor antagonists ameliorate attention deficit/hyperactivity disorder-like behavioral changes caused by neonatal habenula lesion. Behavioural Pharmacology 29:1, pages 71-78.
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Dorota Łażewska, Maria Kaleta, J. Stephan Schwed, Tadeusz Karcz, Szczepan Mogilski, Gniewomir Latacz, Agnieszka Olejarz, Agata Siwek, Monika Kubacka, Annamaria Lubelska, Ewelina Honkisz, Jadwiga Handzlik, Barbara Filipek, Holger Stark & Katarzyna Kieć-Kononowicz. (2017) Biphenyloxy-alkyl-piperidine and azepane derivatives as histamine H3 receptor ligands. Bioorganic & Medicinal Chemistry 25:20, pages 5341-5354.
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Aurore Sors, Fany Panayi, Lionel Bert, Dominique Favale, Olivier Nosjean, Valérie Audinot, Jean-Michel Arrang, Bruno Buisson, Esther Steidl, Jean-Marie Delbos, Tuulia Huhtala, Outi Kontkanen, Anne-Marie Chollet, Patrick Casara & Pierre Lestage. (2017) Mechanistic characterization of S 38093, a novel inverse agonist at histamine H3 receptors. European Journal of Pharmacology 803, pages 11-23.
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Magdalena Dudek, Kamil Kuder, Marcin Kołaczkowski, Adrian Olczyk, Elżbieta Żmudzka, Aleksandra Rak, Marek Bednarski, Karolina Pytka, Jacek Sapa & Katarzyna Kieć-Kononowicz. (2016) H3 histamine receptor antagonist pitolisant reverses some subchronic disturbances induced by olanzapine in mice. Metabolic Brain Disease 31:5, pages 1023-1029.
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Bassem Sadek & Holger Stark. (2016) Cherry-picked ligands at histamine receptor subtypes. Neuropharmacology 106, pages 56-73.
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Christel A.S. Bergström, William N. Charman & Christopher J.H. Porter. (2016) Computational prediction of formulation strategies for beyond-rule-of-5 compounds. Advanced Drug Delivery Reviews 101, pages 6-21.
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Rashmi R. Shah, Pierre Maison-Blanche, Philippe Robert, Emmanuel Denis & Thierry Duvauchelle. (2016) Can an early phase clinical pharmacology study replace a thorough QT study? Experience with a novel H3-receptor antagonist/inverse agonist. European Journal of Clinical Pharmacology 72:5, pages 533-543.
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Rong Sheng, Li Tang, Liu Jiang, Lingjuan Hong, Ying Shi, Naiming Zhou & Yongzhou Hu. (2015) Novel 1-Phenyl-3-hydroxy-4-pyridinone Derivatives as Multifunctional Agents for the Therapy of Alzheimer’s Disease. ACS Chemical Neuroscience 7:1, pages 69-81.
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Ruben Vardanyan & Victor Hruby. 2016. Synthesis of Best-Seller Drugs. Synthesis of Best-Seller Drugs 247 263 .
B. Sadek, D. Łażewska, S. Hagenow, K. Kieć-Kononowicz & H. Stark. 2016. Histamine Receptors. Histamine Receptors 109 155 .
T. A. M. Mocking, R. Bosma, S. N. Rahman, E. W. E. Verweij, Daniel A. McNaught-Flores, Henry F. Vischer & Rob Leurs. 2016. Histamine Receptors. Histamine Receptors 1 49 .
Pertti Panula, Paul L. Chazot, Marlon Cowart, Ralf Gutzmer, Rob Leurs, Wai L. S. Liu, Holger Stark, Robin L. Thurmond & Helmut L. Haas. (2015) International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors. Pharmacological Reviews 67:3, pages 601-655.
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Zhongli Gao, William J. Hurst, Daniel Hall, Ryan Hartung, William Reynolds, Jiesheng Kang, Raisa Nagorny, James A. Hendrix & Pascal G. George. (2015) Design and synthesis of a novel series of histamine H3 receptor antagonists through a scaffold hopping strategy. Bioorganic & Medicinal Chemistry 23:3, pages 429-438.
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Vivien C. Abad & Christian Guilleminault. 2015. Sleep, Neuronal Plasticity and Brain Function. Sleep, Neuronal Plasticity and Brain Function 503 553 .
Bassem Sadek, Kamil Kuder, Dhanasekaran Subramanian, Mohamed Shafiullah, Holger Stark, Dorota Łażewska, Abdu Adem & Katarzyna Kieć-Kononowicz. (2014) Anticonvulsive effect of nonimidazole histamine H3 receptor antagonists. Behavioural Pharmacology 25:3, pages 245-252.
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Iwona Masłowska-Lipowicz & Krzysztof Walczyński. (2014) Structure-Activity Relationships of New 1-substitutedmethyl-4-[5-( N -methyl- N -propylamino)pentyloxy]piperidines and Selected 1-[( N -substituted- N- methyl)-3-propyloxy]-5-( N -methy-l- N -propyl)-pentanediamines as H 3 -Antagonists . Chemical Biology & Drug Design 83:1, pages 106-118.
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F. Estelle R. Simons & Cezmi A. Akdis. 2014. Middleton's Allergy. Middleton's Allergy 1503 1533 .
Shinya Harusawa, Koichi Sawada, Takuji Magata, Hiroki Yoneyama, Lisa Araki, Yoshihide Usami, Kouta Hatano, Kouichi Yamamoto, Daisuke Yamamoto & Atsushi Yamatodani. (2013) Synthesis and evaluation of N-alkyl-S-[3-(piperidin-1-yl)propyl]isothioureas: High affinity and human/rat species-selective histamine H3 receptor antagonists. Bioorganic & Medicinal Chemistry Letters 23:23, pages 6415-6420.
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Zhongli Gao, William J. Hurst, Etienne Guillot, Raisa Nagorny, Marie-Pierre Pruniaux, James A. Hendrix & Pascal G. George. (2013) Synthesis, characterization, and biological assessment of the four stereoisomers of the H3 receptor antagonist 5-fluoro-2-methyl-N-[2-methyl-4-(2-methyl[1,3′]bipyrrolidinyl-1′-yl)phenyl]benzamide. Bioorganic & Medicinal Chemistry Letters 23:14, pages 4044-4047.
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M Uguen, D Perrin, S Belliard, X Ligneau, PM Beardsley, JM Lecomte & JC Schwartz. (2013) Preclinical evaluation of the abuse potential of P itolisant, a histamine H 3 receptor inverse agonist/antagonist compared with M odafinil . British Journal of Pharmacology 169:3, pages 632-644.
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Ranju Bansal & Sridhar Thota. (2012) Pyridazin-3(2H)-ones: the versatile pharmacophore of medicinal significance. Medicinal Chemistry Research 22:6, pages 2539-2552.
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Mu‐Hong Chen, Tung‐Ping Su, Ying‐Sheue Chen, Ju‐Wei Hsu, Kai‐Lin Huang, Wen‐Han Chang & Ya‐Mei Bai. (2012) Attention deficit hyperactivity disorder, tic disorder, and allergy: is there a link? A nationwide population‐based study. Journal of Child Psychology and Psychiatry 54:5, pages 545-551.
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Zhiwei Feng, Tingjun Hou & Youyong Li. (2013) Docking and MD study of histamine H4R based on the crystal structure of H1R. Journal of Molecular Graphics and Modelling 39, pages 1-12.
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S Miyamoto, N Miyake, L F Jarskog, W W Fleischhacker & J A Lieberman. (2012) Pharmacological treatment of schizophrenia: a critical review of the pharmacology and clinical effects of current and future therapeutic agents. Molecular Psychiatry 17:12, pages 1206-1227.
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Marek Bajda, Kamil J. Kuder, Dorota Łażewska, Katarzyna Kieć‐Kononowicz, Anna Więckowska, Michalina Ignasik, Natalia Guzior, Jakub Jończyk & Barbara Malawska. (2012) Dual‐Acting Diether Derivatives of Piperidine and Homopiperidine with Histamine H 3 Receptor Antagonistic and Anticholinesterase Activity . Archiv der Pharmazie 345:8, pages 591-597.
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Dong Xiao, Anandan Palani, Michael Sofolarides, Robert Aslanian, Robert E. WestJr.Jr., Shirley M. Williams, Ren-Long Wu, Joyce Hwa, Christopher Sondey, Jean Lachowicz & Walter A. Korfmacher. (2012) Fused bicycles as arylketone bioisosteres leading to potent, orally active thiadiazole H3 antagonists. Bioorganic & Medicinal Chemistry Letters 22:9, pages 3354-3357.
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Ashwin U. Rao, Ning Shao, Robert G. Aslanian, Tin-Yau Chan, Sylvia J. Degrado, Li Wang, Brian McKittrick, Mary Senior, Robert E. WestJr.Jr., Shirley M. Williams, Ren-Long Wu, Joyce Hwa, Bhuneshwari Patel, Shuqin Zheng, Christopher Sondey & Anandan Palani. (2011) Discovery of a Potent Thiadiazole Class of Histamine H 3 Receptor Antagonist for the Treatment of Diabetes . ACS Medicinal Chemistry Letters 3:3, pages 198-202.
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Fabrizio Bordi, Silvia Rivara, Elisa Dallaturca, Caterina Carmi, Daniele Pala, Alessio Lodola, Federica Vacondio, Lisa Flammini, Simona Bertoni, Vigilio Ballabeni, Elisabetta Barocelli & Marco Mor. (2012) Dibasic biphenyl H3 receptor antagonists: Steric tolerance for a lipophilic side chain. European Journal of Medicinal Chemistry 48, pages 214-230.
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Graham Lunn, Charles E. Mowbray, Wai L. S. Liu, Valerie M. Joynson, Tanya Hay & Michael Yeadon. (2012) The discovery and profile of PF-0868087, a CNS-sparing histamine H3 receptor antagonist for the treatment of allergic rhinitis. Med. Chem. Commun. 3:3, pages 339-343.
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Gunnar Flik, Eliyahu Dremencov, Thomas I. H. F. Cremers, Joost H. A. Folgering & Ben H. C. Westerink. (2011) The role of cortical and hypothalamic histamine-3 receptors in the modulation of central histamine neurotransmission: an in vivo electrophysiology and microdialysis study. European Journal of Neuroscience 34:11, pages 1747-1755.
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F. Estelle R. Simons & Keith J. Simons. (2011) Histamine and H1-antihistamines: Celebrating a century of progress. Journal of Allergy and Clinical Immunology 128:6, pages 1139-1150.e4.
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Travis T. Wager, Betty A. Pettersen, Anne W. Schmidt, Douglas K. Spracklin, Scot Mente, Todd W. Butler, Harry HowardJrJr, Daniel J. Lettiere, David M. Rubitski, Diane F. Wong, Frank M. Nedza, Frederick R. Nelson, Hans Rollema, Jeffrey W. Raggon, Jiri Aubrecht, Jody K. Freeman, John M. Marcek, Julie Cianfrogna, Karen W. Cook, Larry C. James, Linda A. Chatman, Philip A. Iredale, Michael J. Banker, Michael L. Homiski, Jennifer B. Munzner & Rama Y. Chandrasekaran. (2011) Discovery of Two Clinical Histamine H 3 Receptor Antagonists: trans - N -Ethyl-3-fluoro-3-[3-fluoro-4-(pyrrolidinylmethyl)phenyl]cyclobutanecarboxamide (PF-03654746) and trans -3-Fluoro-3-[3-fluoro-4-(pyrrolidin-1-ylmethyl)phenyl]- N -(2-methylpropyl)cyclobutanecarboxamide (PF-03654764) . Journal of Medicinal Chemistry 54:21, pages 7602-7620.
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. (2011) Current world literature. Current Opinion in Allergy & Clinical Immunology 11:4, pages 386-389.
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Panayiotis A. Procopiou, Christopher Browning, Jennifer M. Buckley, Kenneth L. Clark, Lise Fechner, Paul M. Gore, Ashley P. Hancock, Simon T. Hodgson, Duncan S. Holmes, Michael Kranz, Brian E. Looker, Karen M. L. Morriss, Daniel L. Parton, Linda J. Russell, Robert J. Slack, Steven L. Sollis, Sadie Vile & Clarissa J. Watts. (2011) The Discovery of Phthalazinone-Based Human H 1 and H 3 Single-Ligand Antagonists Suitable for Intranasal Administration for the Treatment of Allergic Rhinitis . Journal of Medicinal Chemistry 54:7, pages 2183-2195.
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