Desloratadine citrate disodium injection, a potent histamine H1 receptor antagonist, inhibits chemokine production in ovalbumin-induced allergic rhinitis guinea pig model and histamine-induced human nasal epithelial cells via inhibiting the ERK1/2 and NF-kappa B signal cascades

2015 ◽  
Vol 767 ◽  
pp. 98-107 ◽  
Author(s):  
Meiling Chen ◽  
Shuhong Xu ◽  
Peipei Zhou ◽  
Guangwei He ◽  
Qiong Jie ◽  
...  
Keyword(s):  
Allergic Rhinitis ◽  
Guinea Pig ◽  
Receptor Antagonist ◽  
H1 Receptor ◽  
Nf Kappa B ◽  
Chemokine Production ◽  
Human Nasal Epithelial Cells ◽  
Guinea Pig Model ◽  
H1 Receptor Antagonist ◽  
Signal Cascades

scholarly journals Concentrations of H1-Receptor Antagonist in the Human Nasal Mucosa

2009 ◽  
Vol 2009 ◽  
pp. 1-4 ◽  
Author(s):  
Kenji Takasaki ◽  
Kaori Enatsu ◽  
Hidetaka Kumagami ◽  
Haruo Takahashi
Keyword(s):  
Allergic Rhinitis ◽  
Receptor Antagonist ◽  
Nasal Mucosa ◽  
High Performance ◽  
University Hospital ◽  
Sinus Surgery ◽  
H1 Receptor ◽  
Group I ◽  
Significant Difference ◽  
H1 Receptor Antagonist

Aims. To measure blood and tissue concentrations of the H1-receptor antagonist, bepotastine besilate (BB).Methods. Participants included 14 men and six women, whose age ranged from 13 to 76 years, with chronic rhinosinusitis, who underwent endoscopic sinus surgery at our university hospital. Among them, 10 participants had allergic rhinitis (AR) (Group I), and others did not have AR (Group II). Nasal mucosa and blood were collected 55 to 130 minutes after oral administration of BB 10 mg. Concentrations of the agent in the serum and nasal mucosa were measured by high-performance liquid chromatography.Results. Concentrations of BB of the serum in Group I and II were  ng/mL and  ng/mL. Those of the nasal mucosa tissue in Groups I and II were  ng/g and  ng/g. There was no significant difference in the values of concentration of BB between the serum and the nasal mucosa in either Group I or II ( and , resp., Pairedt-test).Conclusion. This preliminary study is considered the first report on the concentration of H1-receptor antagonists in nasal mucosa. The prompt absorption and transition to the nasal mucosa of BB seems to have an effect on allergic rhinitis.

Dose-Related Control of Allergic Rhinitis Symptoms by a H1-Receptor Antagonist

1994 ◽  
Vol 103 (3) ◽  
pp. 298-302 ◽  
Author(s):  
F.F. Horak ◽  
S. Jäger ◽  
G. Nirnberger ◽  
U. Berger ◽  
I. Andresen ◽  
...  
Keyword(s):  
Allergic Rhinitis ◽  
Receptor Antagonist ◽  
H1 Receptor ◽  
H1 Receptor Antagonist

Anti-anaphylactic activity of the non sedative histamime H1 receptor antagonist SL 85.0324 in the rat and guinea pig

1990 ◽  
Vol 183 (2) ◽  
pp. 218 ◽  
Author(s):  
K.G. Lloyd ◽  
J. Lévrier ◽  
D. Duval ◽  
M. Prouteau ◽  
C. Berry ◽  
...  
Keyword(s):  
Guinea Pig ◽  
Receptor Antagonist ◽  
H1 Receptor ◽  
H1 Receptor Antagonist

In sillico analysis, synthesis, and biological evaluation of triazole derivatives as a H1 receptor antagonist

2020 ◽  
Vol 17 ◽  
Author(s):  
Sandip N Badeliya ◽  
Ishan I Panchal ◽  
Bibhranjan Panigrahi ◽  
C. N. Patel
Keyword(s):  
Guinea Pig ◽  
Receptor Antagonist ◽  
Pharmacophore Model ◽  
In Silico Analysis ◽  
Biological Evaluation ◽  
Guinea Pig Ileum ◽  
H1 Receptor ◽  
Chlorpheniramine Maleate ◽  
H1 Receptor Antagonist ◽  
The Impact

Background: Histamine, a biological amine, is considered as a principal mediator of many pathological processes regulating several essential events in allergies and autoimmune diseases. Numerous derivatives have been developed that strive with histamine at H1 receptor and prevent binding of histamine at H1 receptor thus prevent allergic reactions. Molecules containing triazole ring fused with six-membered ring systems are found to possess broad applications in the field of medicine and industry. The present study is an attempt to characterize the impact of the nature of the substituent introduced at the 5 positions of the-4H-1,2,4-triazole-3-thiol on their capacities to bind with H1 receptor. Methods: Molecular docking (PDB ID: 3RZE) revealed that synthesized derivatives and target proteins were actively involved in binding with Tyr-108, Thr-112, Ala-216, and Phe432 subunits. The pharmacophore model new 5-(4-substituted phenyl)-4-(phenylamino)- 4-H-1,2,4-triazole-3-thiols (5a-5h) were designed and evaluated for H1-blocking activity using isolated segments from the guinea pig ileum. Results: According to in silico analysis, all the compounds have a topological polar surface area (TPSA) less than 140 Å squared, so they tend to a good penetration in cell membranes. The results show that most of the compounds are non-inhibitors of CYP450 substrates that play a fundamental role in drug metabolism. Compounds 5d (50.53±12.03), 5h (50.62±12.33) and 7a (55.07±12.41) are more active than others. Conclusion: Finally, these derivatives were screened for H1 receptor antagonist activity using guinea pig ileum taking chlorpheniramine maleate as a standard. Most of the compounds possesses better antihistamine activity.

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