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Expert Opinion on Therapeutic Patents Volume 13, 2003 - Issue 6
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Review

Recent advances in histamine H3/H4 receptor ligands

Holger Stark Institut für Pharmazeutische Chemie, Johann Wolfgang Goethe-Universität, Biozentrum, Marie-Curie-Strasse 9, 60439 Frankfurt am Main, Germany. [email protected]
Pages 851-865 | Published online: 02 Mar 2005

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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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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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Mai Zhang, Jennifer D Venable & Robin L Thurmond. (2006) The histamine H4 receptor in autoimmune disease. Expert Opinion on Investigational Drugs 15:11, pages 1443-1452.
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Silvia Fonquerna & Montserrat Miralpeix. (2006) H1 antihistamines: patent highlights 2000 – 2005. Expert Opinion on Therapeutic Patents 16:2, pages 109-117.
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Arthur A Hancock & Michael E Brune. (2005) Assessment of pharmacology and potential anti-obesity properties of H3 receptor antagonists/inverse agonists. Expert Opinion on Investigational Drugs 14:3, pages 223-241.
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Arthur A Hancock & Gerard B Fox. (2004) Perspectives on cognitive domains, H3 receptor ligands and neurological disease. Expert Opinion on Investigational Drugs 13:10, pages 1237-1248.
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Harry R Howard. (2004) Agents for attention-deficit hyperactivity disorder – an update. Expert Opinion on Therapeutic Patents 14:7, pages 983-1008.
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Michelle F. Corrêa, André L. Balico-Silva, Dóra J. Kiss, Gustavo A.B. Fernandes, Jhonatan C. Maraschin, Lucas T. Parreiras-e-Silva, Marina T. Varela, Sarah C. Simões, Michel Bouvier, György M. Keserű, Claudio M. Costa-Neto & João Paulo S. Fernandes. (2021) Novel potent (dihydro)benzofuranyl piperazines as human histamine receptor ligands – Functional characterization and modeling studies on H3 and H4 receptors. Bioorganic & Medicinal Chemistry 30, pages 115924.
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Andressa Soliani, Silvia Megumi Kubota, Michelle Fidelis Corrêa, Suzete Maria Cerutti & João Paulo S. Fernandes. (2020) Differential contribution of H3R antagonism by LINS01 compounds on memory, anxiety-like behaviour and spontaneous locomotor activity in healthy rats. Behavioural Brain Research 377, pages 112230.
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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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Monika Gaba & Chander Mohan. (2015) Development of drugs based on imidazole and benzimidazole bioactive heterocycles: recent advances and future directions. Medicinal Chemistry Research 25:2, pages 173-210.
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Hossein Amini-Khoei, Maryam Rahimi-Balaei, Shayan Amiri, Arya Haj-Mirzaian, Mahsa Hassanipour, Armin Shirzadian, Maziar Gooshe, Sakineh Alijanpour, Shahram Ejtemaie Mehr & Ahmad Reza Dehpour. (2015) Morphine modulates the effects of histamine H1 and H3 receptors on seizure susceptibility in pentylenetetrazole-induced seizure model of mice. European Journal of Pharmacology 769, pages 43-47.
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Brad M. Savall, Frank Chavez, Kevin Tays, Paul J. Dunford, Jeffery M. Cowden, Michael D. Hack, Ronald L. Wolin, Robin L. Thurmond & James P. Edwards. (2014) Discovery and SAR of 6-Alkyl-2,4-diaminopyrimidines as Histamine H 4 Receptor Antagonists . Journal of Medicinal Chemistry 57:6, pages 2429-2439.
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Kerstin Wingen & Holger Stark. (2013) Scaffold variations in amine warhead of histamine H3 receptor antagonists. Drug Discovery Today: Technologies 10:4, pages e483-e489.
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Ming Tao, Lisa D. Aimone, John A. Gruner, Joanne R. Mathiasen, Zeqi Huang, Jacquelyn Lyons, Rita Raddatz & Robert L. Hudkins. (2012) Synthesis and structure–activity relationship of 5-pyridazin-3-one phenoxypiperidines as potent, selective histamine H3 receptor inverse agonists. Bioorganic & Medicinal Chemistry Letters 22:2, pages 1073-1077.
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Dahui Zhou, Jonathan L. Gross, Jean Y. Sze, Adedayo B. Adedoyin, Mark Bowlby, Li Di, Brian J. Platt, Guoming Zhang, Nicholas Brandon, Thomas A. Comery & Albert J. Robichaud. (2011) Pyrrolidin-3-yl-N-methylbenzamides as potent histamine 3 receptor antagonists. Bioorganic & Medicinal Chemistry Letters 21:19, pages 5957-5960.
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Gregory A. Gfesser, Henry Zhang, Jurgen Dinges, Gerard B. Fox, Jia Bao Pan, Timothy A. Esbenshade, Betty B. Yao, David Witte, Thomas R. Miller, Chae-Hee Kang, Kathy M. Krueger, Youssef L. Bennani, Arthur A. Hancock & Ramin Faghih. (2004) Structure–activity relationships of non-imidazole H3 receptor ligands. Part 3: 5-Substituted 3-phenyl-1,2,4-oxadiazoles as potent antagonists. Bioorganic & Medicinal Chemistry Letters 14:3, pages 673-676.
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Marlon Cowart, John K. Pratt, Andrew O. Stewart, Youssef L. Bennani, Timothy A. Esbenshade & Arthur A. Hancock. (2004) A new class of potent non-imidazole H3 antagonists: 2-aminoethylbenzofurans. Bioorganic & Medicinal Chemistry Letters 14:3, pages 689-693.
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Shelly A. Glase & David J. Dooley. 2004. 1 12 .

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