Muskarinski acetilholinski receptor M4 (muskarinski holinergijski receptor 4, ), je protein koji je kod ljudi kodiran genom.[1][2]
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Затвори
Muskarinski acetilholinski receptori pripadaju velikoj familiji G protein spregnutih receptora. Funkcionalna raznovrsnost ovih receptora je definisana vezivanjem acetilholina, i obuhvata ćelijske odgovore poput inhibicije adenilat ciklaze, fosfoinozitidne degeneracije i modulacije kalijumovih kanala. Muskarinski receptori posreduju mnoge efekte acetilholina u centralnom i perifernom nervnom sistemu. Klinički značaj ovoj receptora nije poznat; međutim, studije na miševima su ustanovile vezu između njegovog dejstva i inhibicije adenilil ciklaze.[1]
M4 muskarinski receptori deluju kao inhibitorni autoreceptori za acetilholin. Aktivacija M4 receptora inhibira oslobađanje acetilholina u striatumu. M2 podtip acetilholinksog receptora deluje na sličan način, kao inhibitorni autoreceptor acetilholinskog otpuštanja, mada taj receptor deluje prvenstveno u hipokampusu i cerebralnom korteksu.
Muskarinski acetilholinski receptori imaju regulatorno dejstvo na dopaminergijsku neurotransmisiju. Aktivacija M4 receptora u striatumu inhibira D1-indukovanu lokomotornu stimulaciju kod miševa. Miševi koji su deficitarni u M4 receptorima ispoljavaju povećanu lokomotornu stimulaciju u odgovoru na D1 agoniste, amfetamin i kokain.[3][4][5] Neurotransmisija u striatumu utiče na ekstrapiramidalnu motornu kontrolu, tako da alteracije M4 aktivnosti mogu da doprinosu oboljenjima poput Parkinsonove bolesti.[6][7][8]
===Ortosterni agonisti===
Antagonisti
- (mešoviti M2/M4 antagonist, -[2-[2-[(dipropilamino)metil]-1-piperidinil]etil]-5,6-dihidro-6-okso-11-pirido[2,3-b][1,4]benzodiazepin-11-karboksamid
- Dicikloverin[11]
- Himbacin
- Mamba toksin 3[12]
- etil estar (3,6a,11,14-tetrahidro-9-metoksi-2-metil-()-izohino[1,2-b]pirolo[3,2-f][1,3]benzoksazin-1-karboksilne kiseline
- Tropikamid - umereno selektivan u odnosu na druge muskarinske podtipove (oko 2-5 puta)[13]
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