A Review on Current Research on H3 and H4 Receptors
DOI:
https://doi.org/10.22270/ajprd.v11i2.1238Keywords:
H3 Receptor, H3 Antagonist, H4 Receptor, H4 Antagonist, Histamine, Histaminergic Neuron, Anti histaminesAbstract
This review article provides an overview of the structure, location, and functional uses of H3 and H4 histamine receptors. It examines the current research on the topic, including the structure of the receptors, their location in the body, and their role in the body's response to histamine. It also looks at potential, therapeutic applications of these receptors and their potential to be used as drug targets. The article concludes with a discussion of potential future directions for research on these receptors. The identification of Histamine (H3) & (H4) receptors .Some years ago relined interest in histamine research and exposed attracting perspectives for the potential therapeutic exploitation & these new drug targets. While the H3 receptors is mainly localized in the CNS, the of the brain and the morphologic characterization histamine producing neurons proved the existence of histaminergic system in the mammalian brain, It is primarily expressed in hematopoietic cell, indicating their function in neurotransmission and immunomodulation, respectively. Although structural similarities between H3 and H4 & Species difference in their pharmacological profiles are causes of limitation in their evaluation & their biological profile the development of selective ligands for there receptors. The H3 and H4 is recognised drug target for neuronal diseases, such as Cognitive Disorder, Neuropathic pain and Sleep Wake Disorder considering the topicality & this area of research. This review focuses on the pharmacology of selected promising indication and the rationalefor the application of H3and H4 ligands.
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References
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14. Franco HF, Detlef Z and Bernhard FG. The 21st century renaissance of the basophil? Current insights into its role in allergic responses and innate immunity. Experimental Dermatology. (2006); 15(11):855-864.
15. Malinowska R, Godlewski G and Schliker E. Histamine H3 Receptors – General Characterization and their function in the cardiovascular system. Journal of Physiology and Pharmacology.1998; 191-211
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24. A E Alewijnse, H Timmerman, E H Jacobs, M J Smit, E Roovers, S Cotecchia, R Leurs, The effect of mutations in the DRY motif on the constitutive activity and structural instability of the histamine H(2) receptor,J.Mol Pharmacol. (2000);57(5):890-8
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29. Jean-Charles Schwartz,The histamine H3 receptor: from discovery to clinical trials with pitolisant".J.Br J Pharmacol (2011);163(4):713-21.
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31. pillot c, ortiz j, héron a, ridray s, schwartzjc, arrangjm J.neuroscienceciproxifan, a histamine h3-receptor antagonist/inverse agonist, potentiates neurochemical and behavioral effects of haloperidol in the rat (2002)22 (16);7272–80
32. X. Ligneau, j.-s. Lin, g. Vanni-mercier, m. Jouvet, j. L. Muir, c. R. Ganellin, h. Stark, s. Elz, w. Schunack and j.-c. Schwartz neurochemical and behavioral effects of ciproxifan, a potent histamine h3-receptor antagonist journal of pharmacology and experimental therapeutics november(1998); 287(2):658-666;
33. Witkin jm, nelson dlselective histamine h3 receptor antagonists for treatment of cognitive deficiencies and other disorders of the central nervous systemnists for treatment of cognitive deficiencies and other disorders of the central nervous system".J. Pharmacology ther. 103 (1): 1–doi:10.1016/j.pharmthera. (2004).05.001. Pmid 15251226; 1-20.
34. Charles h. Pierce "effects of using betahistine to treat adults withattention deficit hyperactivity disorder" J.clinical trial number nct00829881(2009); 108-259
35. Adrion, c; fischer, c. S.; wagner, j; "efficacy and safety of betahistine treatment in patients with meniere's disease: primary results of a long term, multicentre, double blind, randomised, placebo controlled, dose defining trial. J. clinical trial bmj. (2016); 21:10-1136
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37. "Pitolisant Orphan Drug Designations and Approvals". U.S. Food and Drug Administration.(FDA). 17 May 2010. Retrieved ( 2021); 47(16):111-215
38. Haibindai ,qiuli fu, yaoshen, weiwei hu, zhongmiaozhang, henktimmerman, rob leurs, zhongchen ,the histamine h3 receptor antagonist clobenpropit enhances gaba release to protect against nmda-induced excitotoxicity through the camp/protein kinase a pathway in cultured cortical neurons European.J.pharmacol. (2007); 1:117-23.
39. Sahlholm K, Nilsson J, Marcellino D, Fuxe K, Arhem P.; The human histamine h3 receptor couples to girk channels in xenopus oocytes; . European journal of pharmacology, (2007); 206-210
40. Anirban ghoshal ,ajeetkumar , doddapaneniyugandhar , chandansona , sunukuriakose , identification of novel β-lactams and pyrrolidinone derivatives as selective histamine-3 receptor (h3r) modulators as possible anti-obesity agents, eur.J.med chem. (2018); 25 152:148-159
41. Chungping Yu, Jennie GO, Shawn C, Stefan S, Vladimir M. New Insights into the Mechanism of Actionof Viloxazine: Serotonin and Norepinephrine Modulating Properties. Journal of experimental Pharmacology. (2020); 25:285-300.
42. Findling RL, Candler SA, Nasser AF, Schwabe S, Yu C, Garcia J, O'Neal W, Newcorn JH. Viloxazine A New Non-Stimulant Option in the Treatment of Pediatric Attention-Deficit/Hyperactivity Disorder. Journal of Psychosocial Nursing and Mental Health Services. (2022); (4) 7-9.
43. Elisabetta Baldi,CorradoBucherelli, Walter Schunack, Gabriele Cenni, Patrizio Blandina, M Beatrice Passani,The H3 receptor protean agonist proxyfan enhances the expression of fear memory in the rat,J.Neuropharmacology(2005); (2):246-51.
44. F.P. Jansen, Characterization of the binding of the first selective radiolabelled histamine H3-receptor antagonist, 125I-iodophenpropit, to rat brain T.S. Wu, H.-P. Voss, H.W.M. Steinbusch, R.C. Vollinga, B. Rademaker, A. Bast, H. Timmerman,J. British Journal of Pharmacology.(1994); 113(2):355–62
45. Krueger, KM; Witte, DG; Ireland-Denny, L; Miller, TR; Baranowski, JL; Buckner, S; Milicic, I;Esbenshade, TA; Hancock, AA, "G protein-dependent pharmacology of histamine H3receptor ligands: evidence for heterogeneous active state receptor conformations".Journal of Pharmacology and Experimental Therapeutics.(2005); 314 (1):271–81
46. X Ligneau 1, M Garbarg, M L Vizuete, J Diaz, K Purand, H Stark, W Schunack, J C Schwartz,Iodoproxyfan, a new antagonist to label and visualize histamine H3 receptors. J Pharmacology Experiment Theory ,(1994); 271(1):452-9
47. Pillot C, Heron A, Cochois V, Tardivel-Lacombe J, Ligneau X, Schwartz JC, Arrang JM. A detailed mapping of the histamine H(3) receptor and its gene transcripts in rat brain. Thioperamide". IUPHAR/BPS Guide to Pharmacology .J.Neuroscience, (2002); 114 (1):173-93.
2. Ligneau X, Lin J, Vanni-Mercier G, Jouvet M, Muir JL, Ganellin CR, Stark H, Elz S, Schunack W, Schwartz J. Neurochemical and behavioral effects of ciproxifan, a potent histamine H3-receptor antagonist. J Pharmacol Exp Ther. 1998; 287(2):658-66.
3. Esbenshade TA, Fox GB, Krueger KM, Baranowski JL, Miller TR, Kang CH, Denny LI, Witte DG, Yao BB, Pan JB, Faghih R, Bennani YL, Williams M, Hancock AA "Pharmacological and behavioral properties of A-349821, a selective and potent human histamine H3 receptor antagonist". Biochemical Pharmacology.2004; 68(5):933-945.
4. WybrzeżeWyspiańskiego,"Pharmacology" Online Etymology Dictionary. Archived from the original,J.Wrocław University of Science and Technology.2017; 27:50-370
5. Airaksinen MS, Panula P. The histaminergic system in the guinea pig central nervous system: an immunocytochemical mapping study using an antiserum against histamine. J Comp Neurol.1988; 273(2):163-86.
6. Alves-Rodrigues A, Leurs R, Willems E, Timmerman H. Binding of clozapine metabolites and analogues to the histamine H3 receptor in rat brain cortex. Arch Pharm (Weinheim).1996; 329(8-9):413-6.
7. Anichtchik OV, Huotari M, Peitsaro N, Haycock JW, Männistö PT, Panula P. Modulation of histamine H3 receptors in the brain of 6-hydroxydopamine-lesioned rats. Eur J Neurosci.2000; 12(11):3823-32.
8. Akdis, C. A., Akdis, M., Bieber, T., Bindslev-Jensen, C., Boguniewicz, M., Eigenmann, P., et al. Diagnosis and treatment of atopic dermatitis in children and adults: European academy of allergology and clinical immunology/American academy of allergy, asthma and immunology/PRACTALL consensus report. J. Allergy Clin. Immunol. 2006; 61(8):969-87
9. Altenbach, R. J., Adair, R. M., Bettencourt, B. M., Black, L. A., Fix-Stenzel, S. R., Gopalakrishnan, S. M., et al. Structure-activity studies on a series of a 2aminopyrimidine-containing histamine H4 receptor ligands. J. Med. Chem. 2008 ;51(20):6571-80
10. Arrang JM, Garbarg M, Schwartz JC. Auto-inhibition of brain histamine release mediated by a novel class (H3) of histamine receptor. Nature.1983; 302(5911):832-7.
11. Aldesic M, Verdrengh M, Bokarewa M, Dahlberg L, Foster SJ and Tarkowski A. Histamine in rheumatoid arthritis. Scandinavia Journal of Immunology.2007; 65(6):530-537
12. Cezmi A, Estelle F and Simons R. Histamine receptors are hot in immunopharmacology. European Journal of Pharmacology.2006; 69-76
13. Bassam BD, Cecilia BB, Henry JE, Ying W and Azzam AM. Functional expression of H4 histamine receptor in human natural killer cells, monocytes, and dendritic cells. The Journal of Immunology. (2007); 179(11):7907-7915)
14. Franco HF, Detlef Z and Bernhard FG. The 21st century renaissance of the basophil? Current insights into its role in allergic responses and innate immunity. Experimental Dermatology. (2006); 15(11):855-864.
15. Malinowska R, Godlewski G and Schliker E. Histamine H3 Receptors – General Characterization and their function in the cardiovascular system. Journal of Physiology and Pharmacology.1998; 191-211
16. Randi BS, Christina JM, Neil S, Irina LK, Kara L, Timothy LW, and Roberto L. Coupling of histamine H3 receptors to neuronal Na+/H+ exchange: A novel protective mechanism in myocardial ischemia. Proceedings of the National Academy of Sciences.2001; 98(5):2855-2859.
17. Arrang JM, Garbarg M, Schwartz JC. Auto-inhibition of brain histamine release mediated by a novel class (H3) of histamine receptor. Nature.( 1983); (302: 832-837)
18. Arrang JM, Garbarg M, Lancelo JC, Lecomte JM, Pollard H, RobbaM, Schunack W and Schwartz JC. Highly potent and selective ligands for histamine H3-receptors. Nature.( 1987); (117-123)
19. Mike EP & Robin GC. Histamine and its receptors. Brirtish Journal of Pharmacolgy. (2006); (S127-S135)
20. Arrang JM, Garbarg M, Lancelo JC, Lecomte JM, Pollard H, RobbaM, Schunack W and Schwartz JC. Highly potent and selective ligands for histamine H3-receptors. Nature Journal.(1987); (117-123)
21. R E West Jr , A Zweig, N Y Shih, M I Siegel, R W Egan, M A Clark,Identification of two H3-histamine receptor subtypes,J.Molecular Pharmacology..(1999); 38(5):610-3
22. Gustavo Nieto-Alamilla , Ricardo Márquez-Gómez , Ana-Maricela García-Gálvez, Guadalupe-Elide Morales-Figueroa , José-Antonio Arias-Montaño. The Histamine H3 Receptor: Structure, Pharmacology, and Function ,J. Molecular Pharmacology, (2016); 90(5):649-673
23. M S Airaksinen, P Panula,The histaminergic system in the guinea pig central nervous system: an immunocytochemical mapping study using an antiserum against histamine.J.J Comp Neurol. (1988) ;273(2):163-86
24. A E Alewijnse, H Timmerman, E H Jacobs, M J Smit, E Roovers, S Cotecchia, R Leurs, The effect of mutations in the DRY motif on the constitutive activity and structural instability of the histamine H(2) receptor,J.Mol Pharmacol. (2000);57(5):890-8
25. Florence Gbahou, Ludwig Vincent, Marie Humbert-Claude, Joel Tardivel-Lacombe, Claude Chabret, Jean-Michel Arrang,Compared pharmacology of human histamine H3 and H4 receptors: structure–activity relationships of histamine derivatives,J.Br J Pharmacol. (2006); 147(7):744-54.
26. EkateriniTiligada, 1 Konstantinos Kyriakidis, 1 Paul L. Chazot, 2 and M. Beatrice Passani,Histamine Pharmacology and New CNS Drug TargetsCNS NeurosciTher. (2011); 17(6):620–628.
27. Elden Berla Thangam,1 Ebenezer Angel Jemima, Himadri Singh, Mirza Saqib Baig, Mahejibin Khan, Clinton B. Mathias,5 Martin K. Church,The role of histamine and histamine recepters in mast cell and mediated allergy,J.Front Immunol. (2018); 9:1873
28. Dr. Sruthi M., MBBS,How do histamine antagonist-inverse agonists work? Medical BHMS, PGD Health Operations,J.Front SystNeurosci.( 2012); 6(72):145-256
29. Jean-Charles Schwartz,The histamine H3 receptor: from discovery to clinical trials with pitolisant".J.Br J Pharmacol (2011);163(4):713-21.
30. Michael Berlin, Christopher W. Boyce, and Manuel de Lera Ruiz,Histamine H3 Receptor as a Drug Discovery Target".J. of Medicinal Chemistry.(2011); 54 (1):26–53
31. pillot c, ortiz j, héron a, ridray s, schwartzjc, arrangjm J.neuroscienceciproxifan, a histamine h3-receptor antagonist/inverse agonist, potentiates neurochemical and behavioral effects of haloperidol in the rat (2002)22 (16);7272–80
32. X. Ligneau, j.-s. Lin, g. Vanni-mercier, m. Jouvet, j. L. Muir, c. R. Ganellin, h. Stark, s. Elz, w. Schunack and j.-c. Schwartz neurochemical and behavioral effects of ciproxifan, a potent histamine h3-receptor antagonist journal of pharmacology and experimental therapeutics november(1998); 287(2):658-666;
33. Witkin jm, nelson dlselective histamine h3 receptor antagonists for treatment of cognitive deficiencies and other disorders of the central nervous systemnists for treatment of cognitive deficiencies and other disorders of the central nervous system".J. Pharmacology ther. 103 (1): 1–doi:10.1016/j.pharmthera. (2004).05.001. Pmid 15251226; 1-20.
34. Charles h. Pierce "effects of using betahistine to treat adults withattention deficit hyperactivity disorder" J.clinical trial number nct00829881(2009); 108-259
35. Adrion, c; fischer, c. S.; wagner, j; "efficacy and safety of betahistine treatment in patients with meniere's disease: primary results of a long term, multicentre, double blind, randomised, placebo controlled, dose defining trial. J. clinical trial bmj. (2016); 21:10-1136
36. Yahiya y syed,pitolisant: first global approval drugs. J. 76 (13)doi:10.1007/s40265-016-0620-1. Pmid 27438291. S2cid 4268483 ( 2016); 1313-1318
37. "Pitolisant Orphan Drug Designations and Approvals". U.S. Food and Drug Administration.(FDA). 17 May 2010. Retrieved ( 2021); 47(16):111-215
38. Haibindai ,qiuli fu, yaoshen, weiwei hu, zhongmiaozhang, henktimmerman, rob leurs, zhongchen ,the histamine h3 receptor antagonist clobenpropit enhances gaba release to protect against nmda-induced excitotoxicity through the camp/protein kinase a pathway in cultured cortical neurons European.J.pharmacol. (2007); 1:117-23.
39. Sahlholm K, Nilsson J, Marcellino D, Fuxe K, Arhem P.; The human histamine h3 receptor couples to girk channels in xenopus oocytes; . European journal of pharmacology, (2007); 206-210
40. Anirban ghoshal ,ajeetkumar , doddapaneniyugandhar , chandansona , sunukuriakose , identification of novel β-lactams and pyrrolidinone derivatives as selective histamine-3 receptor (h3r) modulators as possible anti-obesity agents, eur.J.med chem. (2018); 25 152:148-159
41. Chungping Yu, Jennie GO, Shawn C, Stefan S, Vladimir M. New Insights into the Mechanism of Actionof Viloxazine: Serotonin and Norepinephrine Modulating Properties. Journal of experimental Pharmacology. (2020); 25:285-300.
42. Findling RL, Candler SA, Nasser AF, Schwabe S, Yu C, Garcia J, O'Neal W, Newcorn JH. Viloxazine A New Non-Stimulant Option in the Treatment of Pediatric Attention-Deficit/Hyperactivity Disorder. Journal of Psychosocial Nursing and Mental Health Services. (2022); (4) 7-9.
43. Elisabetta Baldi,CorradoBucherelli, Walter Schunack, Gabriele Cenni, Patrizio Blandina, M Beatrice Passani,The H3 receptor protean agonist proxyfan enhances the expression of fear memory in the rat,J.Neuropharmacology(2005); (2):246-51.
44. F.P. Jansen, Characterization of the binding of the first selective radiolabelled histamine H3-receptor antagonist, 125I-iodophenpropit, to rat brain T.S. Wu, H.-P. Voss, H.W.M. Steinbusch, R.C. Vollinga, B. Rademaker, A. Bast, H. Timmerman,J. British Journal of Pharmacology.(1994); 113(2):355–62
45. Krueger, KM; Witte, DG; Ireland-Denny, L; Miller, TR; Baranowski, JL; Buckner, S; Milicic, I;Esbenshade, TA; Hancock, AA, "G protein-dependent pharmacology of histamine H3receptor ligands: evidence for heterogeneous active state receptor conformations".Journal of Pharmacology and Experimental Therapeutics.(2005); 314 (1):271–81
46. X Ligneau 1, M Garbarg, M L Vizuete, J Diaz, K Purand, H Stark, W Schunack, J C Schwartz,Iodoproxyfan, a new antagonist to label and visualize histamine H3 receptors. J Pharmacology Experiment Theory ,(1994); 271(1):452-9
47. Pillot C, Heron A, Cochois V, Tardivel-Lacombe J, Ligneau X, Schwartz JC, Arrang JM. A detailed mapping of the histamine H(3) receptor and its gene transcripts in rat brain. Thioperamide". IUPHAR/BPS Guide to Pharmacology .J.Neuroscience, (2002); 114 (1):173-93.
Published
2023-04-15
How to Cite
Chaurasiya, V., Bhoir, V., Bhundere, S., Chauhan, Y., Chavan, K., Shriram, B., & Smita, T. (2023). A Review on Current Research on H3 and H4 Receptors. Asian Journal of Pharmaceutical Research and Development, 11(2), 52–59. https://doi.org/10.22270/ajprd.v11i2.1238
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