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Review

Assessment of pharmacology and potential anti-obesity properties of H3 receptor antagonists/inverse agonists

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Pages 223-241 | Published online: 22 Apr 2005

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Read on this site (4)

M. Zendehdel, A. Baghbanzadeh, P. Aghelkohan & S. Hassanpour. (2016) Central histaminergic system interplay with suppressive effects of immune challenge on food intake in chicken. British Poultry Science 57:2, pages 271-279.
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Maikel Wijtmans, Rob Leurs & Iwan de Esch. (2007) Histamine H3 receptor ligands break ground in a remarkable plethora of therapeutic areas. Expert Opinion on Investigational Drugs 16:7, pages 967-985.
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Michael Berlin & Christopher W Boyce. (2007) Recent advances in the development of histamine H3 antagonists. Expert Opinion on Therapeutic Patents 17:6, pages 675-687.
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Dr Peter Norman. (2007) A H3 antagonist for treating allergic rhinitis: a development candidate?. Expert Opinion on Therapeutic Patents 17:4, pages 449-452.
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Articles from other publishers (59)

Axelle Khouma, Moein Minbashi Moeini, Julie Plamondon, Denis Richard, Alexandre Caron & Natalie Jane Michael. (2023) Histaminergic regulation of food intake. Frontiers in Endocrinology 14.
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Kamil Mika, Małgorzata Szafarz, Monika Zadrożna, Barbara Nowak, Marek Bednarski, Katarzyna Szczepańska, Krzysztof Pociecha, Monika Kubacka, Noemi Nicosia, Izabela Juda, Katarzyna Kieć-Kononowicz & Magdalena Kotańska. (2022) KSK-74: Dual Histamine H3 and Sigma-2 Receptor Ligand with Anti-Obesity Potential. International Journal of Molecular Sciences 23:13, pages 7011.
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Kamil Mika, Małgorzata Szafarz, Marek Bednarski, Gniewomir Latacz, Sylwia Sudoł, Jadwiga Handzlik, Krzysztof Pociecha, Joanna Knutelska, Noemi Nicosia, Katarzyna Szczepańska, Kamil J. Kuder, Katarzyna Kieć-Kononowicz & Magdalena Kotańska. (2021) Histamine H3 Receptor Ligands—KSK-59 and KSK-73—Reduce Body Weight Gain in a Rat Model of Excessive Eating. Pharmaceuticals 14:11, pages 1080.
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Katarzyna Szczepańska, Kamil J. Kuder & Katarzyna Kieć-Kononowicz. (2021) Dual-targeting Approach on Histamine H3 and Sigma-1 Receptor Ligands as Promising Pharmacological Tools in the Treatment of CNS-linked Disorders. Current Medicinal Chemistry 28:15, pages 2974-2995.
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Katarzyna Szczepańska, Steffen Pockes, Sabina Podlewska, Carina Höring, Kamil Mika, Gniewomir Latacz, Marek Bednarski, Agata Siwek, Tadeusz Karcz, Martin Nagl, Merlin Bresinsky, Denise Mönnich, Ulla Seibel, Kamil J. Kuder, Magdalena Kotańska, Holger Stark, Sigurd Elz & Katarzyna Kieć-Kononowicz. (2021) Structural modifications in the distal, regulatory region of histamine H3 receptor antagonists leading to the identification of a potent anti-obesity agent. European Journal of Medicinal Chemistry 213, pages 113041.
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Magdalena Kotańska, Kamil Mika, Karolina Reguła, Katarzyna Szczepańska, Małgorzata Szafarz, Marek Bednarski, Agnieszka Olejarz-Maciej, Katarzyna Nowak, Gniewomir Latacz, Szczepan Mogilski, Kamil J. Kuder, Katarzyna Kieć-Kononowicz & Jacek Sapa. (2019) KSK19 – Novel histamine H3 receptor ligand reduces body weight in diet induced obese mice. Biochemical Pharmacology 168, pages 193-203.
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Ajeet Kumar, Venkata Reddy Pasam, Ravi Kumar Thakur, Maninder Singh, Kartikey Singh, Mahendra Shukla, Anubhav Yadav, Shalini Dogra, Chandan Sona, Deepmala Umrao, Swati Jaiswal, Hafsa Ahmad, Mamunur Rashid, Sandeep K. Singh, Muhammad Wahajuddin, Anil Kumar Dwivedi, Mohammad Imran Siddiqi, Jawahar Lal, Rama Pati Tripathi & Prem N. Yadav. (2019) Novel Tetrahydroquinazolinamines as Selective Histamine 3 Receptor Antagonists for the Treatment of Obesity. Journal of Medicinal Chemistry 62:9, pages 4638-4655.
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M Jaefari-Anari, M Zendehdel, H Gilanpour, A Asghari & V Babapour. (2018) Central Opioidergic System Interplay with Histamine on Food Intake in Neonatal Chicks: Role of µ-Opioid and H1/H3 Receptors. Brazilian Journal of Poultry Science 20:3, pages 595-604.
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Magdalena Kotańska, Kamil J. Kuder, Katarzyna Szczepańska, Jacek Sapa & Katarzyna Kieć-Kononowicz. (2018) The histamine H3 receptor inverse agonist pitolisant reduces body weight in obese mice. Naunyn-Schmiedeberg's Archives of Pharmacology 391:8, pages 875-881.
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Hooman Heidarzadeh, Morteza Zendehdel, Vahab Babapour & Hasan Gilanpour. (2017) The effect of Nesfatin-1 on food intake in neonatal chicks: role of CRF1 /CRF2 and H1/ H3 receptors. Veterinary Research Communications 42:1, pages 39-47.
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Jolene Zheng, Joseph R. Vasselli, Jason F. King, Michael L. King, Wenqian We, Zachary Fitzpatrick, William D. Johnson, John W. Finley, Roy J. Martin, Michael J. Keenan, Frederic M. Enright & Frank L. Greenway. (2016) Using Caenorhabditis elegans as a Model for Obesity Pharmacology Development. American Journal of Therapeutics 23:6, pages e1363-e1370.
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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.
Crossref
Alessandro Pini, Ilona Obara, Emma Battell, Paul L. Chazot & Arianna Carolina Rosa. (2016) Histamine in diabetes: Is it time to reconsider?. Pharmacological Research 111, pages 316-324.
Crossref
Gustavo Provensi, Patrizio Blandina & Maria Beatrice Passani. (2016) The histaminergic system as a target for the prevention of obesity and metabolic syndrome. Neuropharmacology 106, pages 3-12.
Crossref
Gustavo Provensi, Patrizio Blandina & Maria Beatrice Passani. 2016. Histamine Receptors. Histamine Receptors 341 360 .
Erich H. Schneider, Detlef Neumann & Roland Seifert. (2014) Modulation of behavior by the histaminergic system: Lessons from HDC-, H3R- and H4R-deficient mice. Neuroscience & Biobehavioral Reviews 47, pages 101-121.
Crossref
Gregory Sliwoski, Sandeepkumar Kothiwale, Jens Meiler & Edward W. LoweJr.Jr.. (2013) Computational Methods in Drug Discovery. Pharmacological Reviews 66:1, pages 334-395.
Crossref
Manuel de Lera Ruiz, Junying Zheng, Michael Y. Berlin, Kevin D. McCormick, Robert G. Aslanian, Robert West, Joyce Hwa, Jean Lachowicz & Margaret van Heek. (2013) Bicyclic and tricyclic heterocycle derivatives as histamine H3 receptor antagonists for the treatment of obesity. Bioorganic & Medicinal Chemistry Letters 23:21, pages 6004-6009.
Crossref
Dimitry N. Krementsov, Emma H. Wall, Rebecca A. Martin, Meenakumari Subramanian, Rajkumar Noubade, Roxana Del Rio, Gary M. Mawe, Jeffrey P. Bond, Matthew E. Poynter, Elizabeth P. Blankenhorn & Cory Teuscher. (2013) Histamine H3 Receptor Integrates Peripheral Inflammatory Signals in the Neurogenic Control of Immune Responses and Autoimmune Disease Susceptibility. PLoS ONE 8:7, pages e62743.
Crossref
Meng He, Chao Deng & Xu-Feng Huang. (2013) The Role of Hypothalamic H1 Receptor Antagonism in Antipsychotic-Induced Weight Gain. CNS Drugs 27:6, pages 423-434.
Crossref
RH Clapp & SM Luckman. (2012) Proxyfan acts as a neutral antagonist of histamine H 3 receptors in the feeding-related hypothalamic ventromedial nucleus . British Journal of Pharmacology 167:5, pages 1099-1110.
Crossref
Javier Ceras, Nuria Cirauqui, Silvia Pérez-Silanes, Ignacio Aldana, Antonio Monge & Silvia Galiano. (2012) Novel sulfonylurea derivatives as H3 receptor antagonists. Preliminary SAR studies. European Journal of Medicinal Chemistry 52, pages 1-13.
Crossref
Atsushi Ichikawa & Satoshi Tanaka. 2005. Encyclopedia of Life Sciences. Encyclopedia of Life Sciences.
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.
Crossref
Marie Humbert-Claude, Elisabeth Davenas, Florence Gbahou, Ludwig Vincent & Jean-Michel Arrang. (2011) Involvement of histamine receptors in the atypical antipsychotic profile of clozapine: a reassessment in vitro and in vivo. Psychopharmacology 220:1, pages 225-241.
Crossref
Rob Leurs, Henry F. Vischer, Maikel Wijtmans & Iwan J.P. de Esch. (2011) En route to new blockbuster anti-histamines: surveying the offspring of the expanding histamine receptor family. Trends in Pharmacological Sciences 32:4, pages 250-257.
Crossref
Michael Berlin, Christopher W. Boyce & Manuel de Lera Ruiz. (2010) Histamine H 3 Receptor as a Drug Discovery Target . Journal of Medicinal Chemistry 54:1, pages 26-53.
Crossref
Maria Beatrice Passani, Patrizio Blandina & Fernando Torrealba. (2011) The Histamine H 3 Receptor and Eating Behavior . Journal of Pharmacology and Experimental Therapeutics 336:1, pages 24-29.
Crossref
Leonardo Munari & Maria Beatrice Passani. 2011. Handbook of Behavior, Food and Nutrition. Handbook of Behavior, Food and Nutrition 319 336 .
Z. Iffiú-Soltész, E. Wanecq, D. Prévot, S. Grès & C. Carpéné. (2009) Histamine oxidation in mouse adipose tissue is controlled by the AOC3 gene-encoded amine oxidase. Inflammation Research 59:S2, pages 227-229.
Crossref
Mohammed Shahid, Trivendra Tripathi, Rahat Ali Khan, Nancy Khardori, Ali Ibrahim Al-Sultan, Hamdan Ibrahim AL-Mohammed, Abdulrahman A. Alsultan, Anwar Huq, Aijaz Ahmed Khan & Mashiatullah Siddiqui. 2011. Biomedical Aspects of Histamine. Biomedical Aspects of Histamine 61 100 .
Takayuki Masaki. 2011. Biomedical Aspects of Histamine. Biomedical Aspects of Histamine 299 314 .
Siyuan Le, James P. Finn, Mary E. Larijani, Michael J. Marino & Hervé Schaffhauser. (2009) Detection of low level histamine H3 receptor occupancy by autoradiography. Journal of Neuroscience Methods 185:1, pages 70-75.
Crossref
Rosa María Rodríguez Sarmiento, Matthias H. Nettekoven, Sven Taylor, Jean-Marc Plancher, Hans Richter & Olivier Roche. (2009) Selective naphthalene H3 receptor inverse agonists with reduced potential to induce phospholipidosis and their quinoline analogs. Bioorganic & Medicinal Chemistry Letters 19:15, pages 4495-4500.
Crossref
Pascale David Pierson, Alec Fettes, Christian Freichel, Silvia Gatti-McArthur, Cornelia Hertel, Jörg Huwyler, Peter Mohr, Toshito Nakagawa, Matthias Nettekoven, Jean-Marc Plancher, Susanne Raab, Hans Richter, Olivier Roche, Rosa María Rodríguez Sarmiento, Monique Schmitt, Franz Schuler, Tadakatsu Takahashi, Sven Taylor, Christoph Ullmer & Ruby Wiegand. (2009) 5-Hydroxyindole-2-carboxylic Acid Amides: Novel Histamine-3 Receptor Inverse Agonists for the Treatment of Obesity. Journal of Medicinal Chemistry 52:13, pages 3855-3868.
Crossref
Mark J. Gemkow, Adam J. Davenport, Silke Harich, Bart A. Ellenbroek, Andrea Cesura & David Hallett. (2009) The histamine H3 receptor as a therapeutic drug target for CNS disorders. Drug Discovery Today 14:9-10, pages 509-515.
Crossref
Christian Brabant, Livia Alleva, Thierry Grisar, Etienne Quertemont, Bernard Lakaye, Hiroshi Ohtsu, Jian-Sheng Lin, Peter Jatlow, Marina R. Picciotto & Ezio Tirelli. (2008) Effects of the H3 receptor inverse agonist thioperamide on cocaine-induced locomotion in mice: role of the histaminergic system and potential pharmacokinetic interactions. Psychopharmacology 202:4, pages 673-687.
Crossref
Mark J. Millan. (2009) Dual- and triple-acting agents for treating core and co-morbid symptoms of major depression: novel concepts, new drugs. Neurotherapeutics 6:1, pages 53-77.
Crossref
Timothy Esbenshade, Michael Brune & Marina Strakhova. 2008. The Third Histamine Receptor. The Third Histamine Receptor 277 304 .
Sylvain Celanire, Florence Lebon & Holger Stark. 2008. The Third Histamine Receptor. The Third Histamine Receptor 103 165 .
Timothy A. Esbenshade, Michael E. Brune & Marina I. Strakhova. 2008. The Third Histamine Receptor. The Third Histamine Receptor 277 304 .
Robert Aslanian, Xiaohong Zhu, Henry A. Vaccaro, Neng-Yang Shih, John J. Piwinski, Shirley M. Williams & Robert E. WestJr.Jr.. (2008) Benzimidazole-substituted (3-phenoxypropyl)amines as histamine H3 receptor ligands. Bioorganic & Medicinal Chemistry Letters 18:18, pages 5032-5036.
Crossref
Vincent J. Santora, Jonathan A. Covel, Rena Hayashi, Brian J. Hofilena, Jason B. Ibarra, Michelle D. Pulley, Michael I. Weinhouse, Graeme Semple, Albert Ren, Guilherme Pereira, Jeffrey E. Edwards, Marissa Suarez, John Frazer, William Thomsen, Erin Hauser, Jodie Lorea & Andrew J. Grottick. (2008) Novel H3 receptor antagonists with improved pharmacokinetic profiles. Bioorganic & Medicinal Chemistry Letters 18:14, pages 4133-4136.
Crossref
Li-Li Liu, Jie Yang, Ge-Fei Lei, Gui-Ju Wang, Yu-Wei Wang & Ruo-Peng Sun. (2008) Atomoxetine Increases Histamine Release and Improves Learning Deficits in an Animal Model of Attention-Deficit Hyperactivity Disorder: The Spontaneously Hypertensive Rat. Basic & Clinical Pharmacology & Toxicology 102:6, pages 527-532.
Crossref
Vincent J. Santora, Jonathan A. Covel, Rena Hayashi, Brian J. Hofilena, Jason B. Ibarra, Michelle D. Pulley, Michael I. Weinhouse, Dipanjan Sengupta, Jonathan J. Duffield, Graeme Semple, Robert R. Webb, Carleton Sage, Albert Ren, Guilherme Pereira, Jens Knudsen, Jeffrey E. Edwards, Marissa Suarez, John Frazer, William Thomsen, Erin Hauser, Kevin Whelan & Andrew J. Grottick. (2008) A new family of H3 receptor antagonists based on the natural product Conessine. Bioorganic & Medicinal Chemistry Letters 18:4, pages 1490-1494.
Crossref
Jean-Michel Arrang, Séverine Morisset & Florence Gbahou. (2007) Constitutive activity of the histamine H3 receptor. Trends in Pharmacological Sciences 28:7, pages 350-357.
Crossref
Olivier Roche & Rosa María Rodríguez Sarmiento. (2007) A new class of histamine H3 receptor antagonists derived from ligand based design. Bioorganic & Medicinal Chemistry Letters 17:13, pages 3670-3675.
Crossref
Cory TeuscherMeena SubramanianRajkumar NoubadeJian Feng GaoHalina OffnerJames F. Zachary & Elizabeth P. Blankenhorn. (2007) Central histamine H 3 receptor signaling negatively regulates susceptibility to autoimmune inflammatory disease of the CNS . Proceedings of the National Academy of Sciences 104:24, pages 10146-10151.
Crossref
Kjell Malmlöf, Sven Hastrup, Birgitte Schellerup Wulff, Barbara C. Hansen, Bernd Peschke, Claus Bekker Jeppesen, Rolf Hohlweg & Karin Rimvall. (2007) Antagonistic targeting of the histamine H3 receptor decreases caloric intake in higher mammalian species. Biochemical Pharmacology 73:8, pages 1237-1242.
Crossref
Gerold Bongers, Remko A. Bakker & Rob Leurs. (2007) Molecular aspects of the histamine H3 receptor. Biochemical Pharmacology 73:8, pages 1195-1204.
Crossref
P. Bonaventure, M. Letavic, C. Dugovic, S. Wilson, L. Aluisio, C. Pudiak, B. Lord, C. Mazur, F. Kamme, S. Nishino, N. Carruthers & T. Lovenberg. (2007) Histamine H3 receptor antagonists: From target identification to drug leads. Biochemical Pharmacology 73:8, pages 1084-1096.
Crossref
Kazuhiko Yanai & Manabu Tashiro. (2007) The physiological and pathophysiological roles of neuronal histamine: An insight from human positron emission tomography studies. Pharmacology & Therapeutics 113:1, pages 1-15.
Crossref
Robert L. Hudkins & Rita Raddatz. 2007. Annual Reports in Medicinal Chemistry Volume 42. Annual Reports in Medicinal Chemistry Volume 42 49 62 .
Kjell Malmlöf, Valeria Golozoubova, Bernd Peschke, Birgitte S. Wulff, Hanne H.F. Refsgaard, Peter B. Johansen, Thomas Cremers & Karin Rimvall. (2012) Increase of Neuronal Histamine in Obese Rats Is Associated with Decreases in Body Weight and Plasma Triglycerides. Obesity 14:12, pages 2154-2162.
Crossref
Ryo Yoshimoto, Yasuhisa Miyamoto, Ken Shimamura, Akane Ishihara, Kazuhiko Takahashi, Hidehito Kotani, Airu S. Chen, Howard Y. Chen, Douglas J. MacNeil, Akio Kanatani & Shigeru Tokita. (2006) Therapeutic potential of histamine H3 receptor agonist for the treatment of obesity and diabetes mellitus. Proceedings of the National Academy of Sciences 103:37, pages 13866-13871.
Crossref
Kjell Malmlöf, Rolf Hohlweg & Karin Rimvall. (2006) Targeting of the central histaminergic system for treatment of obesity and associated metabolic disorders. Drug Development Research 67:8, pages 651-665.
Crossref
A.A. Hancock. (2006) The challenge of drug discovery of a GPCR target: Analysis of preclinical pharmacology of histamine H3 antagonists/inverse agonists. Biochemical Pharmacology 71:8, pages 1103-1113.
Crossref
Sylvain Celanire, Maikel Wijtmans, Patrice Talaga, Rob Leurs & Iwan J.P. de Esch. (2005) Keynote review: Histamine H3 receptor antagonists reach out for the clinic. Drug Discovery Today 10:23-24, pages 1613-1627.
Crossref
Steen K. Johansen. (2005) Carbon-14 labelling of selective H3 receptor antagonists. Journal of Labelled Compounds and Radiopharmaceuticals 48:14, pages 1025-1029.
Crossref

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