• Archives of Pharmacal Research
• /
• v.28 no.1
• /
• pp.111-114
• /
• 2005

The antihistamine effects of the triprolidine were studied in rats to determine the feasibility of their enhanced transdermal delivery from the poly (4-methyl-1-pentene) (TPX) matrix system containing penetration enhancer and plasticizer. The antihistamine effects were determined by the Evans blue dye procedure by comparing the changes in vascular permeability increase following the transdermal administration. The vascular permeability increase was significantly reduced by transdermal administration of the triprolidine-TPX system containing triethyl citrate (TEC) and polyoxyethylene-2-oleyl ether (POE). Both the plasticizer and penetration enhancer played an important role in the skin permeation of triprolidine and increased the antihistamine effects. These results showed that the triprolidine-TPX matrix system containing plasticizer and penetration enhancer could be a transdermal delivery system providing the increased antihistamine effects.

• Archives of Pharmacal Research
• /
• v.23 no.4
• /
• pp.324-328
• /
• 2000

Three dimensional QSAR studies for antihistamine and antibradykinin effects of new piperazine derivatives were conducted using the comparative molecular field analysis. Electrostatic and steric factors, but not hydrophobic factor, of the synthesized compounds were correlated with the antagonistic effect.

• Parasites, Hosts and Diseases
• /
• v.61 no.2
• /
• pp.172-182
• /
• 2023

At the time of host attachment, ticks are very sensitive to histamine, but during rapid blood sucking they paradoxically require histamine. Using a rabbit model, we studied the effects of histamine and antihistamine during attachment and fast-feeding in different life stages of Haemaphysalis longicorns. We examined how they responded to histamine and antihistamine by analyzing the detachment rate, histology of feeding lesions, and post-feeding behavior. A significant difference (P<0.01) was found in the detachment rate between experimental and control treatments throughout the observation period. Ticks exhibited a higher detachment rate (30.1%) at 12 h after histamine application during attachment time and on antihistamine-treated skin (25.4%) at 96 h during fast-feeding. After feeding on histamine-treated rabbits, the fully engorged body weights of larvae and nymphs were 0.7±0.36 mg and 3.5±0.65 mg, respectively. An average increase in body weight of 0.6±0.05 mg and 3.2±0.30 mg was observed for larvae and nymphs compared to the respective control weights. Nymphs and adults engorged after antihistamine treatment had an average body weight of 1.3±0.54 mg and 54±0.81 mg, respectively. An average decrease in body weight was observed in antihistamine-treated H. longicornis compared with control nymphs (3.3±0.42 mg) and adults (174±1.78 mg). Skin biopsies were collected after treatment, and differential histopathological characteristics were found between the treatment and control groups. Tick-infested skin collected from rabbits in the antihistamine-treated group lacked erythrocytes in the feeding pool, indicating that antihistamine impaired tick fast-feeding stage.

• Biomolecules & Therapeutics
• /
• v.16 no.4
• /
• pp.416-424
• /
• 2008

A series of N,N'-substituted iminodiacetamide derivatives was synthesized and evaluated their inhibitory effects on the histamine-induced smooth muscle contraction in guinea-pig ileum and on the histamine release from IgE-sensitized RBL-2H3 cells (rat basophilic leukemia cell line). Compounds A3, A4 and A5 which have 1-(4-chlorobenzhydryl) piperazine moiety, showed both moderate antihistamine activity and histamine release inhibitory activity.

• The Korean Journal of Physiology and Pharmacology
• /
• v.13 no.3
• /
• pp.215-220
• /
• 2009

Chlorpheniramine is a potent first-generation histamine $H_1$ receptor antagonist that can increase action potential duration and induce QT prolongation in several animal models. Since block of cardiac human ether-a-go-go-related gene (hERG) channels is one of leading causes of acquired long QT syndrome, we investigated the acute effects of chlorpheniramine on hERG channels to determine the electrophysiological basis for its proarrhythmic potential. We examined the effects of chlorpheniramine on the hERG channels expressed in Xenopus oocytes using two-microelectrode voltage-clamp techniques. Chlorpheniramine induced a concentration-dependent decrease of the current amplitude at the end of the voltage steps and hERG tail currents. The $IC_{50}$ of chlorpheniramine-dependent hERG block in Xenopus oocytes decreased progressively relative to the degree of depolarization. Chlorpheniramine affected the channels in the activated and inactivated states but not in the closed states. The S6 domain mutations Y652A and F656A partially attenuated (Y652A) or abolished (F656A) the hERG current block. These results suggest that the $H_1$ antihistamine, chlorpheniramine is a blocker of the hERG channels, providing a molecular mechanism for the drug-induced arrhythmogenic side effects.

• Korean Journal of Pharmacognosy
• /
• v.15 no.4
• /
• pp.188-193
• /
• 1984

It was previously indicated that 'Samulanshintang' had been examined for effects of the anticonvulsive, antipyretic, analgesic, sedative and antispasmodic actions. In order to investigate the effect on the cardiovascular system and anemic rabbits induced by phenlhydrazine HCl, pharmacological studies have been carried out with extract. The results of this investigation were summarized as follows: The relaxation of bronchial smooth muscle and antihistamine action were recognized. Antihypertensive and vasodilating actions due to vascular smooth muscle relaxation were noted in frogs and rabbits. 'Samulanshintang' lowered the rate of anemia induced by phenylhydrazine and rapidly recovered from the anemia state.

• The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
• /
• v.24 no.2
• /
• pp.28-34
• /
• 2011

Background & Objectives : Allergic rhinitis is an inflammation or irritation of the mucous membranes that line the nose. Common symptoms include sneezing, a stuffy or runny nose, itchy eyes, nose and throat, and watery eyes. We aimed to determine therapeutic effects of Tribulus terrestris by observing changes of total IgE level and the scratching or rubbing around the nose behavior. Materials and Methods : Fifteen BALB/c mice were divided into three groups : AR group(allergic rhinitis elicitated), TT group(which ate herbal medicine) and AH group(which ate antihistamine). Allergic rhinitis was induced in the three groups by intraperitoneal and intranasal sensitization with 0.1% ovalbumin solution. Then Tribulus terrestris was orally administered only to the TT group of 28days, while the AH group was given antihistamine. We observed changes of total IgE level and the scratching or rubbing around the nose behavior. We used Kruskal-Wallis test statistically(p<0.05). Results : 1. Tribulus terrestris showed significantly decreased IgE level on the serum of the rat model. 2. Tribulus terrestris showed significantly decreased scratching or rubbing around the nose behaviors of the rat model. Conclusion : According to the above results, it is considered that Tribulus terrestris has an inhibitory effect on the process of allergic rhinitis and it can be used in relieving symptoms of allergic rhinitis.

• Biomedical Science Letters
• /
• v.25 no.1
• /
• pp.83-91
• /
• 2019

This study was undertaken to investigate the therapeutic effect of Angelica acutiloba on allergic dermatitis, which Angelica acutiloba is traditionally known to have antiinflammatory effects. Sprague-Dawley (SD) rats were divided into five groups: normal control group, experimental allergic dermatitis group (vehicle group), low dose of Angelica acutiloba extract (low-dose group), high dose of Angelica acutiloba extract (high-dose group), and antihistamine treated group with experimental dermatitis (antihistamine group). Total leukocyte, neutrophil, lymphocyte, monocyte and eosinophil counts were significantly higher in the vehicle group than in the control group, but these variables were significantly lower in the low- and high-dose groups than in the vehicle group. The platelet/lymphocyte ratio in the red blood cell index was significantly lower in the low- and high-dose groups than in the vehicle group. Low and high doses of the Angelica acutiloba extract did not have toxic effects on liver and kidney. Serum NO, iNOS and levels were highest in the vehicle group but significantly lower in the low- and high-dose groups, especially in the high-dose group. The results of this study suggested that the Angelica acutiloba extract had the effect of alleviating or treating the experimental allergic dermatitis, and it was concluded that the high dose was more effective.

• Korean Journal of Pharmacognosy
• /
• v.13 no.4
• /
• pp.157-162
• /
• 1982

This study was undertaken to investigate effects of 'Oyo-Tang' on the respiratory system. The results of this study were summarized as follows; 1. Antihistamine and relaxed dialating actions were recognized on the extracted ileum and serial broncheal samples in guinea-pigs. 2. Mild hypertensive action was recognized on the carotid artery in rabbits. 3. Antitussive action was noted on mechanically irritated coughs in dogs and cats. In connection with the results of these studies, effects based on the Oriental medical references were consistent with the actual experimental results. It was considered that effective application of 'Oyo-Tang' for the treatment of cough and asthma could be justified.

• Korean Journal of Pharmacognosy
• /
• v.16 no.1
• /
• pp.18-25
• /
• 1985

Experimental studies were conducted to investigate for the effect of Tongkyu-tang on analgesic, antipyretic, sedative, anti-inflammatory, isolated ileum and anti-histamine actions. Tongkyu-Tang was composed of sixteen crude drugs including Astragali Radix, which has been used for the treatment of common cold, headache, rhinitis, nasal obstruction, rhincospasm, etc. The following results have been obtained; analgesic and antipyretic actions were obtained. Prolonged action against the hypnotic duration of pentobarbital were significantly noted in mice. Anti-inflammatory effects in the paw edema induced by 1% carrageenin and 1% dextran were significantly shown in rats. Spontaneous motilities of isolated ileum of mice were strongly suppressed, and contractions of isolated ileum of mice and guinea-pigs induced by acetylcholine chloride, barium chloride and histamine were remarkably inhibited. Antihistamine actions were noted. Considering the above experimental results, it is suggested that effects of Tongkyu-tang based on the Oriental Medical References were similarly consistent with the actual experimental results.