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Galantamin (Reminyl) - mehanizem delovanja
Pregelj, Peter
Galantamin ima dvojni mehanizem delovanja: zavira katalitično aktivnost encimaacetilholinesteraze (AChE) in alosterično modulira nikotinske receptorjeza acetilholin (nAChR). Galantamin se veže na ...AChE reverzibilno in kompetitivno, torej trajno ne inhibira katalitične funkcije AChE kot nekateri organofosfati, ampak tekmuje z drugimi ligandi za vezavno mesto. Dodatno galantamin z alosterično modulacijo nAChR poveča njihovo občutljivost za acetilholin. Ugotovili so, da galantamin zaščiti celice v celični kulturi predrazličnimi dejavniki, ki so udeleženi pri propadnju živčnih celic pri poteku Alzheimerjeve bolezni (AB). Galantamin s povečanjem števila določenega podtipa nAChR morda poveča sproščanje živčnih prenašalcev, kot je bilo dokazano za glutamat in gama amino masleno kislino (GABA) v hipokampusu in dopamin v striatumu. Apoptoza je najverjetneje glavni mehanizem propadanja nevronov pri bolnikih z AB. Poleg delovanja na spoznavne sposobnosti z ojačanjem holinergičnega živčnega prenosa, galantamin morda deluje tudi nevroprotektivno med napredovanjem AB.
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