Histamin H3 reseptörlerinin rat gastrik fundusundaki kasılma yanıtları üzerine etkisi

Yapılan çalışmada amacımız histamin reseptörlerinin mide düz kas kasılmaları üzerine olan etkilerini incelemek ve bu etkiler üzerinde histamin H3 reseptörlerinin rolünü gözlemlemek. Bu amaçla izole edilen rat mide fundus preparatları izole organ banyosun asılarak ortama histamin agonist ve antagonistleri ilave edildi ve doku örneklerinin elektriksel alan stimülasyonuna verdikleri kasılma yanıtları incelendi. Çalışma gruplarımızda histamin H1, H2, H3 reseptörlerinden birini bloke ettikten sonra elektriksel stimülasyona verilen kasılma yanıtların ne yönde değişeceğini gözlemlemek amacıyla diğer reseptörlerin biri veya her ikisi bloke edilerek kasılma yanıtlarındaki değişiklikler izlendi. Histamin reseptörlerini bloke etmek amacıyla H1 reseptör blokörü olarak pirilamin (10-6 м), H2 reseptör blokörü olarak famotidin (10-6м) ve H3 reseptör blokörü olarak tiyoperamid (10-5м) ve bunların çeşitli kombinasyonları kullanıldı. Tüm gruplara H3 reseptör agonisti (R)-α-metilhistamin10-8, 10-7, 10-6 ve 10-5 molar derişimlerinin etkileri kümülatif olarak incelendi. Bu çalışma sonucunda elde edilen sonuçlar Histamin H3 reseptörünün rat mide fundus düz kasında bulunduğunu ve kas kontraksiyonunun inhibisyonuna aracılık ettiğini göstermiştir. Bu sonuç çeşitli bulgularla desteklenmiştir. 1)Selektif H3 agonisti R-(α)-metilhistamin kontraktil yanıtlarda belirgin bir azalmaya neden olmuştur.2) R-(α)-metilhistamin’in kontraktil yanıtlar üzerindeki azaltıcı yöndeki etkileri yine selektif H3 reseptör antagonisti tiyoperamid tarafından artırılmıştır.

The effects of histamine H3 receptors on contractile responses on rat gastric fundus

The aim of this study is to determine the effects of histamine receptors on the gastrointestinal system smooth muscle contractions and the role of histamine H3 receptors on these effects. İsolated rat gastric fundus preparations were hanged on isolated organ bath and histamine receptor agonist and anthagonists were added to the bath solution and the electrical field stimulation-induced contractile responses were evaluated. In our study groups after blocking one of the histamine receptors H1, H2,H3; contractile responses were observed. Then, other two receptors were blocked one by one or combination of them to observe the changes on the contractile responses given to the electrical stimulation .To blocke histamine receptors pyrilamine (10-6м) as H1 receptor blocker, famotidine (10-6м) as H2 receptor blocker and thioperamide (10-5м) as H3 receptor blocker and various combination of them were used. All groups were treated with H3 receptor anthagonist thioperamide (10-5м) and agonist R)-α-methylhistamine (R)MHA on 10-8, 10-7, 10-6 ve 10-5 molar concentrations cumulatively to observe its mediator effects on contractile responses. We suggested that (R)-α-methylhistamine mediates the inhibition on the contractile effects of rat gastric fundus. This conclusion was supported by these findings: a) the selective agonists (R)MHA caused a dumping of the contractile effect of acetylcholine; b) the effect of (R)MHA was prevented by the selective H3 receptor antagonist thioperamide.

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