5 research outputs found
Possible role of 18-kDa translocator protein (TSPO) in etifoxine-induced reduction of direct twitch responses in isolated rat nerve-skeletal muscle preparations
Purpose: To determine the effects of etifoxine on directly-elicited twitch tension of isolated rat nerveskeletal muscle preparations and to propose a possible explanation of the mechanism of the observed effect.Methods: Striated muscles contractile activity was elicited by electrical field stimulation. The effects of etifoxine and nifedipine on direct single twitch response were studied.Results: The results demonstrate that the effect of etifoxine on skeletal muscle depends on the concentrations: low concentrations (10-8 Π and 10-7 Π) have little effect on twitch tension, whereas higher concentrations (10-6 Π and 10-5 Π) induced a significant decrease in the direct single twitch response in comparison to controls. The mean IC50 (reduction of directly-elicited twitch tension) of etifoxine was 0.85 x 10-6 M. The selective L-type calcium channel blocker nifedipine (10-5 Π) induced a greater decrease in the muscle force than 10-6 Π etifoxine. The different abilities of etifoxine and nifedipine to reduce direct single twitch response may be related to their distinct mechanisms of action. The observed effect of etifoxine could be more complex. Probably etifoxine acts as a non-selective agent not only on L-type calcium channels Cav1.1 localized in sarcolemma but also on 18-kDa translocator protein (TSPO) in skeletal muscle.Conclusion: Etifoxine-induced reduction of direct twitch responses could be attributed to an effect on TSPO and Cav1.1. Knowledge of the effects of TSPO ligands on the contraction of skeletal muscle might explain the role of TSPO in muscle contractility.Keywords: Etifoxine, TSPO, Calcium channels, Direct single twitch response, Striated muscl
Denatonium benzoate decreases the effect of histamine in vitro and in rats
Purpose: To evaluate the effect of denatonium benzoate (DB) in histamine-induced model of inflammation and the effect of the selective H1 receptor agonist (2-(2-Pyridyl) ethylamine) on rat gastric smooth muscle strips pretreated with DB.Methods: The anti-inflammatory effect of DB was evaluated in vivo on histamine-induced rat paw edema. In vitro studies on spontaneous muscle contraction were performed on smooth muscle strips isolated from rat gastric corpus.Results: The results showed a well-defined anti-inflammatory effect of DB (15 mg/kg) during the early stage of rat paw edema at the 15th (p < 0.001), 30th (p < 0.01) and 60th min (p < 0.001) compared to control. In vitro experiments indicated reduced spontaneous contractile activity of smooth muscle strips to H1 receptor agonist in the presence of DB (0.5 ΞΌM). The vascular effects of histamine are mediated by H1 receptors. Substances, which reduce the effect of histamine on the H1 receptors could influence the early stage of histamine-induced inflammation.Conclusion: The results show that the anti-inflammatory activity of DB probably is related to its antagonistic activity on histamine H1 receptors. The results would contribute to the search for new antiinflammatory drugs.
Keywords: Denatonium benzoate, Inflammation, Histamine, Muscle contractio
Formulation And Performance Evaluation Of Betahistine Dihydrochloride Microspheres As Sustained Release Systems
ΠΠ΅ΡΠ°Π³ΠΈΡΡΠΈΠ½ Π΄ΠΈΠ³ΠΈΠ΄ΡΠΎΡ
Π»ΠΎΡΠΈΠ΄ ΠΏΡΠ΅Π΄ΡΡΠ°Π²Π»ΡΠ΅Ρ ΡΠΎΠ±ΠΎΠΉ Π³ΠΈΡΡΠ°ΠΌΠΈΠ½ΠΎΠ²ΡΠΉ Π°Π½Π°Π»ΠΎΠ³, ΡΠΈΡΠΎΠΊΠΎ ΠΏΡΠΈΠΌΠ΅Π½ΡΠ΅ΠΌΡΠΉ Π΄Π»Ρ ΠΎΠ±Π»Π΅Π³ΡΠ΅Π½ΠΈΡ ΡΠΈΠΌΠΏΡΠΎΠΌΠΎΠ², ΡΠΎΠΏΡΡΡΡΠ²ΡΡΡΠΈΡ
ΡΠΈΠ½Π΄ΡΠΎΠΌ ΠΠ΅Π½ΠΈΠ΅ΡΠ°. ΠΠΎ Π΄Π°Π½Π½ΡΠΌ ΡΠ°ΡΠΌΠ°ΠΊΠΎΠΊΠΈΠ½Π΅ΡΠΈΡΠ΅ΡΠΊΠΈΡ
ΠΈΡΡΠ»Π΅Π΄ΠΎΠ²Π°Π½ΠΈΠΉ Π±Π΅ΡΠ°Π³ΠΈΡΡΠ°ΠΌΠΈΠ½ ΠΈΠΌΠ΅Π΅Ρ ΠΊΡΠ°ΡΠΊΡΡ ΠΏΠ»Π°Π·ΠΌΠ΅Π½Π½ΡΡ ΠΏΠΎΠ»ΡΠΆΠΈΠ·Π½Ρ - 3.4 Ρ. Π ΡΠ°ΠΊΠΈΡ
ΡΠ»ΡΡΠ°ΡΡ
, ΡΡΠΎΠ±Ρ ΠΏΠΎΠ΄Π΄Π΅ΡΠΆΠΈΠ²Π°ΡΡ ΠΊΠΎΠ½ΡΠ΅Π½ΡΡΠ°ΡΠΈΡ ΠΏΠ»Π°Π·ΠΌΡ Π²ΠΎ Π²ΡΠ΅ΠΌΡ ΡΠ΅ΡΠ°ΠΏΠ΅Π²ΡΠΈΡΠ΅ΡΠΊΠΎΠ³ΠΎ βΠΎΠΊΠ½Π°β, ΠΏΡΠΈΡ
ΠΎΠ΄ΠΈΡΡΡ Π²Π²ΠΎΠ΄ΠΈΡΡ Π»Π΅ΠΊΠ°ΡΡΡΠ²Π΅Π½Π½ΠΎΠ΅ Π²Π΅ΡΠ΅ΡΡΠ²ΠΎ ΡΠ°ΡΡΠΎ, ΡΠ΅ΡΠ΅Π· Π½Π΅Π±ΠΎΠ»ΡΡΠΈΠ΅ ΠΈΠ½ΡΠ΅ΡΠ²Π°Π»Ρ. ΠΡΠΎ ΠΌΠΎΠΆΠ΅Ρ ΠΏΡΠΈΠ²Π΅ΡΡΠΈ ΠΊ ΠΎΡΡΡΡΡΡΠ²ΠΈΡ ΡΠΎΠ΄Π΅ΠΉΡΡΠ²ΠΈΡ ΠΏΡΠΈ ΠΏΡΠΎΠ²Π΅Π΄Π΅Π½ΠΈΠΈ Π»Π΅ΡΠ΅Π½ΠΈΡ ΡΠΎ ΡΡΠΎΡΠΎΠ½Ρ ΠΏΠ°ΡΠΈΠ΅Π½ΡΠ°, ΠΊΠ°ΠΊ ΠΈ ΠΊ ΡΡ
ΡΠ΄ΡΠ΅Π½ΠΈΡ Π΅Π³ΠΎ ΠΊΠΎΠΌΡΠΎΡΡΠ°. Π‘ΠΎΠ²ΡΠ΅ΠΌΠ΅Π½Π½ΡΠΉ ΠΏΠΎΠ΄Ρ
ΠΎΠ΄ Π΄ΠΎΡΡΠΈΠΆΠ΅Π½ΠΈΡ ΡΠ΄Π»ΠΈΠ½Π΅Π½Π½ΠΎΠ³ΠΎ ΠΎΡΠ²ΠΎΠ±ΠΎΠΆΠ΄Π΅Π½ΠΈΡ Π»Π΅ΠΊΠ°ΡΡΡΠ²Π° Π·Π°ΠΊΠ»ΡΡΠ°Π΅ΡΡΡ Π² Π΅Π³ΠΎ Π²ΠΊΠ»ΡΡΠ΅Π½ΠΈΠΈ Π² ΡΠ°ΡΡΠΈΡΡ-Π½ΠΎΡΠΈΡΠ΅Π»ΠΈ. Π¦ΠΠΠ¬: Π Π°Π·ΡΠ°Π±ΠΎΡΠ°ΡΡ Π»Π΅ΠΊΠ°ΡΡΡΠ²ΠΎ-Π΄ΠΎΡΡΠ°Π²Π»ΡΡΡΡΡ ΡΠΈΡΡΠ΅ΠΌΡ Ρ ΡΠ΄Π»ΠΈΠ½Π΅Π½Π½ΡΠΌ ΠΎΡΠ²ΠΎΠ±ΠΎΠΆΠ΄Π΅Π½ΠΈΠ΅ΠΌ Π±Π΅ΡΠ°Π³ΠΈΡΡΠΈΠ½Π°, ΡΡΠΎ ΡΠΏΠΎΡΠΎΠ±ΡΡΠ²ΠΎΠ²Π°Π»ΠΎ Π±Ρ ΡΠΌΠ΅Π½ΡΡΠ΅Π½ΠΈΡ ΡΠ°ΡΡΠΎΡΡ ΠΏΡΠΈΠ΅ΠΌΠ° ΠΈ ΡΠ½ΠΈΠΆΠ΅Π½ΠΈΡ ΡΠΈΡΠΊΠ° ΠΏΠΎΡΠ²Π»Π΅Π½ΠΈΡ Π½Π΅ΠΆΠ΅Π»Π°ΡΠ΅Π»ΡΠ½ΡΡ
Π»Π΅ΠΊΠ°ΡΡΡΠ²Π΅Π½Π½ΡΡ
ΡΠ΅Π°ΠΊΡΠΈΠΉ. ΠΠΠ’ΠΠ ΠΠΠΠ« Π ΠΠΠ’ΠΠΠ«: ΠΠΈΠΊΡΠΎΡΡΠ΅ΡΡ ΠΏΠΎΠ»ΡΡΠ΅Π½Ρ ΡΠ΅ΡΠ΅Π· W/Π ΡΠΌΡΠ»ΡΡΠΈΠΎΠ½Π½ΡΡ ΡΠ΅Ρ
Π½ΠΈΠΊΡ Ρ ΠΈΡΠΏΠ°ΡΠ΅Π½ΠΈΠ΅ΠΌ ΡΠ°ΡΡΠ²ΠΎΡΠΈΡΠ΅Π»Ρ ΠΈ ΠΎΡ
Π°ΡΠ°ΠΊΡΠ΅ΡΠΈΠ·ΠΎΠ²Π°Π½Ρ ΠΏΠΎ ΠΎΡΠ½ΠΎΡΠ΅Π½ΠΈΡ ΠΊ ΠΈΡ
ΡΠ°Π·ΠΌΠ΅ΡΡ, ΠΎΠ»ΠΈΡΠ΅ΡΡΠ²Π΅Π½Π½ΠΎΠΌΡ ΡΠΎΠ΄Π΅ΡΠΆΠ°Π½ΠΈΡ Π±Π΅ΡΠ°Π³ΠΈΡΡΠΈΠ½Π° ΠΈ ΡΡΡΠ΅ΠΊΡΠΈΠ²Π½ΠΎΡΡΠΈ Π½Π°Π³ΡΡΠ·ΠΊΠΈ. ΠΡΠ²ΠΎΠ±ΠΎΠΆΠ΄Π΅Π½ΠΈΠ΅ Ρ Π±Π΅ΡΠ°Π³ΠΈΡΡΠΈΠ½ΠΎΠΌ, ΠΏΡΠΈΠ³ΠΎΡΠΎΠ²Π»Π΅Π½Π½ΡΠ΅ ΡΠ΅ΡΠ΅Π· ΡΠΌΡΠ»ΡΡΠΈΠΎΠ½Π½ΡΡ ΡΠ΅Ρ
Π½ΠΈΠΊΡ Ρ ΠΈΡΠΏΠ°ΡΠ΅Π½ΠΈΠ΅ΠΌ ΡΠ°ΡΡΠ²ΠΎΡΠΈΡΠ΅Π»Ρ, ΠΏΠΎΠΊΠ°Π·ΡΠ²Π°ΡΡ ΡΠΊΠ»ΠΎΠ½Π½ΠΎΡΡΡ ΠΊ ΡΠ΄Π»ΠΈΠ½Π΅Π½Π½ΠΎΠΌΡ ΠΎΡΠ²ΠΎΠ±ΠΎΠΆΠ΄Π΅Π½ΠΈΡ ΠΈ ΠΈΠΌΠ΅ΡΡ ΠΏΠΎΡΠ΅Π½ΡΠΈΠ°Π» Π»Π΅ΠΊΠ°ΡΡΡΠ²Π΅Π½ΠΎ-ΠΎΡΠ²ΠΎΠ±ΠΎΠΆΠ΄Π°ΡΡΠΈΡ
ΡΠΈΡΡΠ΅ΠΌ ΠΏΡΠΈ Π»Π΅ΡΠ΅Π½ΠΈΠΈ ΡΠΈΠ½Π΄ΡΠΎΠΌΠ° ΠΠ΅Π½ΠΈΠ΅Ρ
In Vitro Study of Temperature Changes in Pulp Chamber During Root Planing Procedure Using Er:YAG Laser
Aim: To assess temperature changes at specified time intervals during Er:YAG laser scaling and root planing of surfaces with dental calculus
Effects of Low Level Laser Therapy on Erosive-atrophic Oral Lichen Planus
Background: The erosive-atrophic form of oral lichen planus (OLP) is associated with severe pain and burning sensation and is often unresponsive to treatment. Topical corticosteroids are considered as a medication of first choice but they can produce adverse effects. Therefore, new therapeutic approaches are required