Inverse Agonistic Activity of Antihistamines and Suppression of Histamine H1 Receptor Gene Expression
Histamine H1 receptor (H1R) expression influences the severity of allergy symptoms. We examined the effect of inverse agonists on H1R gene expression. Two inverse agonists (carebastine and mepyramine), but not the neutral antagonist oxatomide, decreased inositol phosphate accumulation. The inverse a...
| Main Authors: | , , , |
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| Format: | Article |
| Language: | English |
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Elsevier
2012-01-01
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| Series: | Journal of Pharmacological Sciences |
| Online Access: | http://www.sciencedirect.com/science/article/pii/S134786131930605X |
| _version_ | 1818035150546534400 |
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| author | Hiroyuki Mizuguchi Shohei Ono Masashi Hattori Hiroyuki Fukui |
| author_facet | Hiroyuki Mizuguchi Shohei Ono Masashi Hattori Hiroyuki Fukui |
| author_sort | Hiroyuki Mizuguchi |
| collection | DOAJ |
| description | Histamine H1 receptor (H1R) expression influences the severity of allergy symptoms. We examined the effect of inverse agonists on H1R gene expression. Two inverse agonists (carebastine and mepyramine), but not the neutral antagonist oxatomide, decreased inositol phosphate accumulation. The inverse agonists also decreased H1R gene expression and down-regulated H1R mRNA below basal expression, while basal H1R mRNA expression was maintained after oxatomide treatment. These results suggest that inverse agonists more potently alleviate allergy symptoms by not only inhibiting stimulus-induced up-regulation of H1R gene expression but also by suppressing basal histamine signaling through their inverse agonistic activity. Keywords:: constitutive activity, histamine H1 receptor gene transcription, inverse agonist |
| first_indexed | 2024-12-10T06:50:29Z |
| format | Article |
| id | doaj.art-c52eab385f0144a89f2801ed053d6fe9 |
| institution | Directory Open Access Journal |
| issn | 1347-8613 |
| language | English |
| last_indexed | 2024-12-10T06:50:29Z |
| publishDate | 2012-01-01 |
| publisher | Elsevier |
| record_format | Article |
| series | Journal of Pharmacological Sciences |
| spelling | doaj.art-c52eab385f0144a89f2801ed053d6fe92022-12-22T01:58:34ZengElsevierJournal of Pharmacological Sciences1347-86132012-01-011181117121Inverse Agonistic Activity of Antihistamines and Suppression of Histamine H1 Receptor Gene ExpressionHiroyuki Mizuguchi0Shohei Ono1Masashi Hattori2Hiroyuki Fukui3Department of Molecular Pharmacology, Institute of Health Biosciences, The University of Tokushima Graduate School, Tokushima 770-8505, JapanDepartment of Molecular Pharmacology, Institute of Health Biosciences, The University of Tokushima Graduate School, Tokushima 770-8505, JapanDepartment of Molecular Pharmacology, Institute of Health Biosciences, The University of Tokushima Graduate School, Tokushima 770-8505, JapanDepartment of Molecular Pharmacology, Institute of Health Biosciences, The University of Tokushima Graduate School, Tokushima 770-8505, Japan; Corresponding author. hfukui@ph.tokushima-u.ac.jpHistamine H1 receptor (H1R) expression influences the severity of allergy symptoms. We examined the effect of inverse agonists on H1R gene expression. Two inverse agonists (carebastine and mepyramine), but not the neutral antagonist oxatomide, decreased inositol phosphate accumulation. The inverse agonists also decreased H1R gene expression and down-regulated H1R mRNA below basal expression, while basal H1R mRNA expression was maintained after oxatomide treatment. These results suggest that inverse agonists more potently alleviate allergy symptoms by not only inhibiting stimulus-induced up-regulation of H1R gene expression but also by suppressing basal histamine signaling through their inverse agonistic activity. Keywords:: constitutive activity, histamine H1 receptor gene transcription, inverse agonisthttp://www.sciencedirect.com/science/article/pii/S134786131930605X |
| spellingShingle | Hiroyuki Mizuguchi Shohei Ono Masashi Hattori Hiroyuki Fukui Inverse Agonistic Activity of Antihistamines and Suppression of Histamine H1 Receptor Gene Expression Journal of Pharmacological Sciences |
| title | Inverse Agonistic Activity of Antihistamines and Suppression of Histamine H1 Receptor Gene Expression |
| title_full | Inverse Agonistic Activity of Antihistamines and Suppression of Histamine H1 Receptor Gene Expression |
| title_fullStr | Inverse Agonistic Activity of Antihistamines and Suppression of Histamine H1 Receptor Gene Expression |
| title_full_unstemmed | Inverse Agonistic Activity of Antihistamines and Suppression of Histamine H1 Receptor Gene Expression |
| title_short | Inverse Agonistic Activity of Antihistamines and Suppression of Histamine H1 Receptor Gene Expression |
| title_sort | inverse agonistic activity of antihistamines and suppression of histamine h1 receptor gene expression |
| url | http://www.sciencedirect.com/science/article/pii/S134786131930605X |
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