Advanced search
Publication Cover
Expert Opinion on Investigational Drugs Volume 20, 2011 - Issue 12
Submit an article Journal homepage
757
Views
47
CrossRef citations to date
0
Altmetric
Reviews

Several down, a few to go: histamine H3 receptor ligands making the final push towards the market?

Sebastiaan Kuhne VU University Amsterdam, Leiden/Amsterdam Center for Drug Research (LACDR), Division of Medicinal Chemistry, Department of Pharmacochemistry, Faculty of Exact Sciences, De Boelelaan 1083, 1081 HV, Amsterdam, The Netherlands
,
Maikel Wijtmans VU University Amsterdam, Leiden/Amsterdam Center for Drug Research (LACDR), Division of Medicinal Chemistry, Department of Pharmacochemistry, Faculty of Exact Sciences, De Boelelaan 1083, 1081 HV Amsterdam, The Netherlands+31 20 5987603; +31 20 5987610; [email protected]
,
Herman D Lim Griffin Discoveries BV, Department of Medicinal Chemistry, Room P-246, De Boelelaan 1083, 1081 HV, Amsterdam, The Netherlands
,
Rob Leurs VU University Amsterdam, Leiden/Amsterdam Center for Drug Research (LACDR), Division of Medicinal Chemistry, Department of Pharmacochemistry, Faculty of Exact Sciences, De Boelelaan 1083, 1081 HV, Amsterdam, The Netherlands; Griffin Discoveries BV, Department of Medicinal Chemistry, Room P-246, De Boelelaan 1083, 1081 HV, Amsterdam, The Netherlands
&
Iwan JP de Esch VU University Amsterdam, Leiden/Amsterdam Center for Drug Research (LACDR), Division of Medicinal Chemistry, Department of Pharmacochemistry, Faculty of Exact Sciences, De Boelelaan 1083, 1081 HV, Amsterdam, The Netherlands; Griffin Discoveries BV, Department of Medicinal Chemistry, Room P-246, De Boelelaan 1083, 1081 HV, Amsterdam, The Netherlands
Pages 1629-1648 | Published online: 13 Oct 2011

Citations (47)

Keep up to date with the latest research on this topic with citation updates for this article.

Subscribe to citation updates

Read on this site (5)

Salim M Bastaki, Yousef M Abdulrazzaq, Mohamed Shafiullah, Małgorzata Więcek, Katarzyna Kieć-Kononowicz & Bassem Sadek. (2018) Anticonvulsant and reproductive toxicological studies of the imidazole-based histamine H3R antagonist 2-18 in mice. Drug Design, Development and Therapy 12, pages 179-194.
Read now
Eleni Pontiki & Dimitra Hadjipavlou-Litina. (2017) QSAR models on H4 receptor antagonists associated with inflammation and anaphylaxis. Journal of Biomolecular Structure and Dynamics 35:5, pages 968-1005.
Read now
Bassem Sadek, Ali Saad, Gniewomir Latacz, Kamil Kuder, Agnieszka Olejarz, Tadeusz Karcz, Holger Stark & Katarzyna Kieć-Kononowicz. (2016) Non-imidazole-based histamine H3 receptor antagonists with anticonvulsant activity in different seizure models in male adult rats. Drug Design, Development and Therapy 10, pages 3879-3898.
Read now
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.
Read now
Petra Dunkel, Christina LL Chai, Beáta Sperlágh, Paul B Huleatt & Péter Mátyus. (2012) Clinical utility of neuroprotective agents in neurodegenerative diseases: current status of drug development for Alzheimer's, Parkinson's and Huntington's diseases, and amyotrophic lateral sclerosis. Expert Opinion on Investigational Drugs 21:9, pages 1267-1308.
Read now

Articles from other publishers (42)

Gábor Wágner, Tamara A. M. Mocking, Xiaoyuan Ma, Inna Slynko, Daniel Da Costa Pereira, Robin Breeuwer, Niek J. N. Rood, Cas van der Horst, Henry F. Vischer, Chris de Graaf, Iwan J. P. de Esch, Maikel Wijtmans & Rob Leurs. (2022) SAR exploration of the non‐imidazole histamine H 3 receptor ligand ZEL‐H16 reveals potent inverse agonism . Archiv der Pharmazie 356:1.
Crossref
Yousef M. Abdulrazzaq, Salim M.A. Bastaki & Ernest Adeghate. (2022) Histamine H3 receptor antagonists – Roles in neurological and endocrine diseases and diabetes mellitus. Biomedicine & Pharmacotherapy 150, pages 112947.
Crossref
Anil Karbhari Shinde, Rajesh Kumar Badange, Veena Reballi, Pramod Kumar Achanta, Kumar Bojja, Sravanthi Manchineella, Nageswara Rao Muddana, Ramkumar Subramanian, Raghava Choudary Palacharla, Vijay Benade, Pradeep Jayarajan, Jagadeesh Babu Thentu, Bujji Babu Lingavarapu, Sivasekhar Yarra, Narendra Kagita, Mallikarjuna Rao Doguparthi, Abdul Rasheed Mohammed & Ramakrishna Nirogi. (2021) 1‐[2‐(1‐Cyclobutylpiperidin‐4‐yloxy)‐6,7‐dihydro‐4 H ‐thiazolo[5,4‐ c ]pyridin‐5‐yl]propan‐1‐one: a Histamine H 3 Receptor Inverse Agonist with Efficacy in Animal Models of Cognition . ChemMedChem 17:3.
Crossref
Ramakrishna Nirogi, Venkata R Grandhi, Rajesh B Medapati, Narender Ganuga, Vijay Benade, Sudhakar Gandipudi, Arunkumar Manoharan, Renny Abraham, Pradeep Jayarajan, Gopinadh Bhyrapuneni, Anil Shinde, Rajesh K Badange, Ramkumar Subramanian, Surendra Petlu & Venkat Jasti. (2021) Histamine 3 receptor inverse agonist Samelisant (SUVN-G3031): Pharmacological characterization of an investigational agent for the treatment of cognitive disorders. Journal of Psychopharmacology 35:6, pages 713-729.
Crossref
Ramakrishna Nirogi, Vijay Benade, Saivishal Daripelli, Ramkumar Subramanian, Venkatesh Kamuju, Gopinadh Bhyrapuneni, Nageswara Rao Muddana, Venkat Reddy Mekala, Surendra Petlu, Pradeep Jayarajan, Rajesh Badange, Anil Shinde & Venkat Jasti. (2021) Samelisant (SUVN-G3031), a potent, selective and orally active histamine H3 receptor inverse agonist for the potential treatment of narcolepsy: pharmacological and neurochemical characterisation. Psychopharmacology 238:6, pages 1495-1511.
Crossref
Miłosz Jastrzębski & Adam Przybyłkowski. (2021) Biogenic amines in the colon. Postępy Higieny i Medycyny Doświadczalnej 75:1, pages 183-190.
Crossref
Markus Falkenstein, Milica Elek & Holger Stark. 2022. The Functional Roles of Histamine Receptors. The Functional Roles of Histamine Receptors 29 76 .
Gábor Wágner, Tamara A. M. Mocking, Marta Arimont, Gustavo Provensi, Barbara Rani, Bruna Silva-Marques, Gniewomir Latacz, Daniel Da Costa Pereira, Christina Karatzidou, Henry F. Vischer, Maikel Wijtmans, Katarzyna Kieć-Kononowicz, Iwan J. P. de Esch & Rob Leurs. (2019) 4-(3-Aminoazetidin-1-yl)pyrimidin-2-amines as High-Affinity Non-imidazole Histamine H 3 Receptor Agonists with in Vivo Central Nervous System Activity . Journal of Medicinal Chemistry 62:23, pages 10848-10866.
Crossref
Gábor Wágner, Tamara A. M. Mocking, Albert J. Kooistra, Inna Slynko, Péter Ábrányi-Balogh, György M. Keserű, Maikel Wijtmans, Henry F. Vischer, Iwan J. P. de Esch & Rob Leurs. (2019) Covalent Inhibition of the Histamine H3 Receptor. Molecules 24:24, pages 4541.
Crossref
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.
Crossref
Younggi Choi & Brian K. Raymer. (2019) Sleep modulating agents. Bioorganic & Medicinal Chemistry Letters 29:16, pages 2025-2033.
Crossref
Tamara A. M. Mocking, Maurice C. M. L. Buzink, Rob Leurs & Henry F. Vischer. (2019) Bioluminescence Resonance Energy Transfer Based G Protein-Activation Assay to Probe Duration of Antagonism at the Histamine H3 Receptor. International Journal of Molecular Sciences 20:15, pages 3724.
Crossref
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.
Crossref
Maria Magdalena Tomasiak-Łozowska, Maciej Klimek, Agnieszka Lis, Marcin Moniuszko & Anna Bodzenta-Łukaszyk. (2018) Markers of anaphylaxis – a systematic review. Advances in Medical Sciences 63:2, pages 265-277.
Crossref
Alaa Alachkar, Gniewomir Latacz, Agata Siwek, Annamaria Lubelska, Ewelina Honkisz, Anna Gryboś, Dorota Łażewska, Jadwiga Handzlik, Holger Stark, Katarzyna Kiec-Kononowicz & Bassem Sadek. (2018) Anticonvulsant evaluation of novel non-imidazole histamine H3R antagonists in different convulsion models in rats. Pharmacology Biochemistry and Behavior 170, pages 14-24.
Crossref
Beata Olszewska, Anna Stasiak, Daniel McNaught Flores, Wiesława Fogel, Rob Leurs & Krzysztof Walczyński. (2018) 4-Hydroxypiperidines and Their Flexible 3-(Amino)propyloxy Analogues as Non-Imidazole Histamine H3 Receptor Antagonist: Further Structure–Activity Relationship Exploration and In Vitro and In Vivo Pharmacological Evaluation. International Journal of Molecular Sciences 19:4, pages 1243.
Crossref
Roman Guryn, Marek Staszewski, Anna Stasiak, Daniel McNaught Flores, Wiesława Fogel, Rob Leurs & Krzysztof Walczyński. (2018) Non-Imidazole Histamine H3 Ligands. Part VII. Synthesis, In Vitro and In Vivo Characterization of 5-Substituted-2-thiazol-4-n-propylpiperazines. Molecules 23:2, pages 326.
Crossref
J. Paul Bolam & Tommas J. Ellender. (2016) Histamine and the striatum. Neuropharmacology 106, pages 74-84.
Crossref
J. Kononoff Vanhanen, S. Nuutinen, M. Tuominen & P. Panula. (2016) Histamine H3 Receptor Regulates Sensorimotor Gating and Dopaminergic Signaling in the Striatum. Journal of Pharmacology and Experimental Therapeutics 357:2, pages 264-272.
Crossref
Kamil Kuder, Dorota Łażewska, Gniewomir Latacz, Johannes Stephan Schwed, Tadeusz Karcz, Holger Stark, Janina Karolak-Wojciechowska & Katarzyna Kieć-Kononowicz. (2016) Chlorophenoxy aminoalkyl derivatives as histamine H3R ligands and antiseizure agents. Bioorganic & Medicinal Chemistry 24:2, pages 53-72.
Crossref
Ruben Vardanyan & Victor Hruby. 2016. Synthesis of Best-Seller Drugs. Synthesis of Best-Seller Drugs 247 263 .
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 .
Anna De Benedetto, Takeshi Yoshida, Sade Fridy, Joo-Eun Park, I.-Hsin Kuo & Lisa Beck. (2015) Histamine and Skin Barrier: Are Histamine Antagonists Useful for the Prevention or Treatment of Atopic Dermatitis?. Journal of Clinical Medicine 4:4, pages 741-755.
Crossref
A Deiteren, J G De Man, P A Pelckmans & B Y De Winter. (2015) Histamine H 4 receptors in the gastrointestinal tract . British Journal of Pharmacology 172:5, pages 1165-1178.
Crossref
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.
Crossref
Robin L. Thurmond, Kayvan Kazerouni, Sandra R. Chaplan & Andrew J. Greenspan. 2015. Pharmacology of Itch. Pharmacology of Itch 257 290 .
Katarina Nikolic, Slavica Filipic, Danica Agbaba & Holger Stark. (2014) Procognitive Properties of Drugs with Single and Multitargeting H 3 Receptor Antagonist Activities . CNS Neuroscience & Therapeutics 20:7, pages 613-623.
Crossref
E Carstens & Tasuku AkiyamaRobin Thurmond, Kayvan Kazerouni, Sandra Chaplan & Andrew Greenspan. 2014. Itch. Itch 143 192 .
Dean G. Brown, Peter R. Bernstein, Andrew Griffin, Steve Wesolowski, Denis Labrecque, Maxime C. Tremblay, Mark Sylvester, Russell Mauger, Phillip D. Edwards, Scott R. Throner, James J. Folmer, Joseph Cacciola, Clay Scott, Lois A. Lazor, Mehrnaz Pourashraf, Vijayaratnam Santhakumar, William M. Potts, Simon Sydserff, Pascall Giguère, Carine Lévesque, Mohammed Dasser & Thierry Groblewski. (2014) Discovery of Spirofused Piperazine and Diazepane Amides as Selective Histamine-3 Antagonists with in Vivo Efficacy in a Mouse Model of Cognition. Journal of Medicinal Chemistry 57:3, pages 733-758.
Crossref
Emma Boström, Yi-Fang Cheng, Niclas Brynne & Märta Segerdahl. (2013) Prediction of H3 Receptor Occupancy Diurnal Fluctuations Using Population Modeling and Simulation with Focus on Guiding Dose Selection in a Phase IIa Study. Pharmaceutical Research 31:2, pages 489-499.
Crossref
William T. Barchuk, Anne Marie Salapatek, Tingting Ge, Pina D'Angelo & Xuejun Liu. (2013) A proof-of-concept study of the effect of a novel H3-receptor antagonist in allergen-induced nasal congestion. Journal of Allergy and Clinical Immunology 132:4, pages 838-846.e6.
Crossref
Li Tang, Liying Zhao, Lingjuan Hong, Fenyan Yang, Rong Sheng, Jianzhong Chen, Ying Shi, Naimin Zhou & Yongzhou Hu. (2013) Design and synthesis of novel 3-substituted-indole derivatives as selective H3 receptor antagonists and potent free radical scavengers. Bioorganic & Medicinal Chemistry 21:19, pages 5936-5944.
Crossref
A J Kooistra, S Kuhne, I J P de Esch, R Leurs & C de Graaf. (2013) A structural chemogenomics analysis of aminergic GPCRs: lessons for histamine receptor ligand design. British Journal of Pharmacology 170:1, pages 101-126.
Crossref
Clifford B. Saper & Thomas E. Scammell. (2013) Emerging therapeutics in sleep. Annals of Neurology 74:3, pages 435-440.
Crossref
Pertti Panula & Saara Nuutinen. (2013) The histaminergic network in the brain: basic organization and role in disease. Nature Reviews Neuroscience 14:7, pages 472-487.
Crossref
Doroth?e Kasteleijn- Nolst Trenit?Dominique Parain, Pierre Genton, Pascal Masnou, Jean-Charles Schwartz & Edouard Hirsch. (2013) Efficacy of the histamine 3 receptor (H3R) antagonist pitolisant (formerly known as tiprolisant; BF2.649) in epilepsy: Dose-dependent effects in the human photosensitivity model. Epilepsy & Behavior 28:1, pages 66-70.
Crossref
Marta González-Sepúlveda, Santi Rosell, Hanne M. Hoffmann, Mª del Mar Castillo-Ruiz, Virginie Mignon, David Moreno-Delgado, Michel Vignes, Jorge Díaz, Josefa Sabriá & Jordi Ortiz. (2013) Cellular distribution of the histamine H3 receptor in the basal ganglia: Functional modulation of dopamine and glutamate neurotransmission. Basal Ganglia 3:2, pages 109-121.
Crossref
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.
Crossref
Olivier Labeeuw, Nicolas Levoin, Olivia Poupardin-Olivier, Thierry Calmels, Xavier Ligneau, Isabelle Berrebi-Bertrand, Philippe Robert, Jeanne-Marie Lecomte, Jean-Charles Schwartz & Marc Capet. (2013) Novel and highly potent histamine H3 receptor ligands. Part 3: An alcohol function to improve the pharmacokinetic profile. Bioorganic & Medicinal Chemistry Letters 23:9, pages 2548-2554.
Crossref
Francesco Sirci, Enade P. Istyastono, Henry F. VischerAlbert J. KooistraSaskia NijmeijerMartien KuijerMaikel WijtmansRaimund Mannhold, Rob LeursIwan J. P. de EschChris de Graaf. (2012) Virtual Fragment Screening: Discovery of Histamine H 3 Receptor Ligands Using Ligand-Based and Protein-Based Molecular Fingerprints . Journal of Chemical Information and Modeling 52:12, pages 3308-3324.
Crossref
M Bhowmik, R Khanam & D Vohora. (2012) Histamine H 3 receptor antagonists in relation to epilepsy and neurodegeneration: a systemic consideration of recent progress and perspectives . British Journal of Pharmacology 167:7, pages 1398-1414.
Crossref
Allison L. Zulli, Lisa D. Aimone, Joanne R. Mathiasen, John A. Gruner, Rita Raddatz, Edward R. Bacon & Robert L. Hudkins. (2012) Substituted phenoxypropyl-(R)-2-methylpyrrolidine aminomethyl ketones as histamine-3 receptor inverse agonists. Bioorganic & Medicinal Chemistry Letters 22:8, pages 2807-2810.
Crossref

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Order Reprints Request Corporate Permissions

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

Request Academic Permissions

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.

Related research

People also read lists articles that other readers of this article have read.

Recommended articles lists articles that we recommend and is powered by our AI driven recommendation engine.

Cited by lists all citing articles based on Crossref citations.
Articles with the Crossref icon will open in a new tab.