H2 antagonisti

Simetidin, H2-reseptör antagonistlerinin prototipi.

H2-reseptör antagonistleri, mide paryetal hücresinde histaminin etkisini bloke ederek bu hücrelerdeki asit salınımını azaltan moleküllerdir. Bu ilaçlar dispepsi tedavisinde kullanılır. Ancak proton pompa inhibitörlerine göre daha az etkili kaldıklarından kullanımları sınırlıdır.

Antihistaminikler'de olduğu gibi H2 antagonistleri de gerçek reseptör antagonisti olarak değil ancak ters agonist olarak etkirler.

Tarihçe ve gelişim

Simetidin bu sınıftaki diğer moleküllerin kendisi üzerinden geliştirildiği prototip moleküldür. Simetidin Smith, Kline & French (SK&F; şimdi GlaxoSmithKline) bir histamin reseptör antagonistinin mide asit sekresyonunu baskılaması için yapılan geliştirme çalışmaları sırasında keşfedilmiştir.

1964'te histaminin mide asidi sekresyonunu stimüle ttiği biliniyordu ancak geleneksel antihistaminiklerin asit üretimi üzerinde etkisi yoktu. Bu gerçeğe bakarak SK&F bilim adamları iki çeşit histamin reseptörü olabileceği fikrini geliştirdi. Anlaşıldı ki geleneksel antihistaminikler H1 etkiliydi ; yeni geliştirilenler ise H2 üzerine etkili olmalıydı.

SK&F takımı rasyonel bir ilaç tasarlama sürecini histaminin yapısını baz alarak başlattı. Bu sırada H2 reseptorü hakkında hiçbir bilgi yoktu. Yüzlerce modifiye bileşik reseptöre model olmak üzere sentezlendi. İlk sonuç kısmi bir H2-reseptör antagonisti olan Nα-guanilhistamin ile alındı. Bundan yola çıkarak ilk H2-reseptör antagonisti olan burimamid ortaya çıkarıldı. Burimamid H2 reseptörüne spesifik bir kompetetif antagonist idi ve Nα-guanilhistamin'e göre 100 kat daha etkiliydi. Bu sırada H2 reseptörünün varlığı da ispatlanmış oldu.

Burimamide yapısı üzerinde yapılan çalışmalar sonucunda metiamid sentezlndi. Metiamid etkili bir ajandı ancak nefrotoksik idi ve agranülositoz yapıyordu.

Kaynakça

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