scholarly journals Antihistamine Activity of 1,2,4-Triazolo[1,5-a]quinazolines

2014 ◽  
Vol 26 (24) ◽  
pp. 8617-8619 ◽  
Author(s):  
R.A. Al-Salahi ◽  
I.A. Alswaidan ◽  
M.S. Marzouk ◽  
W. El-Eraky ◽  
D. Saleh
1988 ◽  
Vol 53 (8) ◽  
pp. 1806-1811 ◽  
Author(s):  
Zdeněk Polívka ◽  
Jan Metyš ◽  
Miroslav Protiva

Reactions of 11-chloro-6,11-dihydrodibenzo[b,e]thiepin and its 2-methyl derivative, and further of the methanesulfonates of 2-chloro- and 2-bromo-6,11-dihydrodibenzo[b,e]thiepin-11-ol with 3-quinuclidinol afforded the title ethers I-IV. The 2-methyl compound II (VÚFB-17 088) showed significant antihistamine activity and the 2-chloro compound III (VÚFB-17 089), having antireserpine and anticataleptic activity, proved a potential antidepressant agent.


Molecules ◽  
2021 ◽  
Vol 26 (3) ◽  
pp. 695
Author(s):  
Nur Zahirah Abd Rani ◽  
Kok Wai Lam ◽  
Juriyati Jalil ◽  
Hazni Falina Mohamad ◽  
Mohd Shukri Mat Ali ◽  
...  

Phyllanthus amarus Schum. & Thonn. (Phyllanthaceae) is a medicinal plant that is commonly used to treat diseases such as asthma, diabetes, and anemia. This study aimed to examine the antiallergic activity of P. amarus extract and its compounds. The antiallergic activity was determined by measuring the concentration of allergy markers release from rat basophilic leukemia (RBL-2H3) cells with ketotifen fumarate as the positive control. As a result, P. amarus did not stabilize mast cell degranulation but exhibited antihistamine activity. The antihistamine activity was evaluated by conducting a competition radioligand binding assay on the histamine 1 receptor (H1R). Four compounds were identified from the high performance liquid chromatography (HPLC) analysis which were phyllanthin (1), hypophyllanthin (2), niranthin (3), and corilagin (4). To gain insights into the binding interactions of the most active compound hypophyllanthin (2), molecular docking was conducted and found that hypophyllanthin (2) exhibited favorable binding in the H1R binding site. In conclusion, P. amarus and hypophyllanthin (2) could potentially exhibit antiallergic activity by preventing the activation of the H1 receptor.


ChemInform ◽  
2010 ◽  
Vol 26 (17) ◽  
pp. no-no
Author(s):  
V. KMONICEK ◽  
M. VALCHAR ◽  
Z. POLIVKA

1992 ◽  
Vol 20 (2) ◽  
pp. 106-111 ◽  
Author(s):  
V K Manna ◽  
P Marks ◽  
J R Gibson

In a double-blind, two-period crossover study, 24 healthy volunteers were evaluated to establish the time of onset of action of activity of acrivastine in suppressing the weal and flare response to intradermally injected histamine. Volunteers received single doses of 8 mg acrivastine and placebo according to a fully randomized, balanced treatment plan. Acrivastine significantly ( P < 0.002) reduced the flare response induced by 0.4 μg histamine challenge 15 min after oral acrivastine dosing when compared with placebo. A significant ( P < 0.001) reduction of the weal response was noted at 25 min, although trends in this direction were already present at earlier time points. Dans d'une étude croisée à deux phase, réalisée en double aveugle et ayant porté sur 24 volontaires sains, on a tenté d'établir le moment du début de l'action de l'acrivastine dans la suppression de la réponse inflammatoire consécutive à l'injection intradermique d'histamine. Les volontaires ont reçu des doses uniques de 8 mg d'acrivastine et de placebo, selon un plan de traitement entièrement randomisé et équilibré. L'acrivastine a réduit significativement ( P < 0,002) la réponse de rubéfaction induite par 0,4 μg d'histamine 15 minutes après l'administration orale d'acrivastine, par rapport au placebo. Une réduction significative ( P < 0,001) de la réponse d'enflure a été notée à 25 minutes, bien qu'une tendance en ce sens ait déjà été observée à un stade plus précoce.


2004 ◽  
Vol 2004 (15) ◽  
pp. 3227-3232 ◽  
Author(s):  
Francesca Borrelli ◽  
Claudio Campagnuolo ◽  
Raffaele Capasso ◽  
Ernesto Fattorusso ◽  
Orazio Taglialatela-Scafati

1962 ◽  
Vol 18 (1) ◽  
pp. 101-108 ◽  
Author(s):  
R. K. ARCHER ◽  
W. FELDBERG ◽  
B. A. KOVACS

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