Metabotropni glutamatni receptor 3 je protein koji je kod ljudi kodiran GRM3 genom.[1][2]
Kratke činjenice Dostupne strukture, Identifikatori ...
Zatvori
L-glutamat je jedan od glavnih ekscitatornih neurotransmitera centralnog nervnog sistema. On aktivira jonotropne i metabotropne glutamatne receptore. Glutamatergična neurotransmisija učestvuje u većini aspekata normalne moždane funkcije. Ona može da bude modifikovana mnogim neuropatološkim uslovima. Metabotropini glutamatni receptori su familija G protein spregnutih receptora, koji se dele u tri grupe na bazi homologije sekvenci, mehanizama prenosa signala, i farmakoloških svojstava. Grupa I obuhvata GRM1 i GRM5. Za njih je pokazano da aktiviraju fosfolipazu C. Grupa II obuhvata GRM2 i GRM3, dok su grupi III GRM4, GRM6, GRM7 i GRM8. Grupe II i III receptora su povezane sa inhibicijom kaskade cikličnog AMP-a, ali se razlikuju u selektivnost na agoniste.[2]
Potpuno mGluR3 selektivni agensi nisu dostupni. Poznati su mešoviti mGluR2/3 (grupa II) ligandi sa selektivnošću u odnosu na druge mGluR podtipove. Neki od njih imaju nisku oralnu biodostupnost, ali postoji mogućnost njihove upotrebe u obliku proleka.[3]
Agonisti
- sa biciklo[3.1.0]heksanskom osnovom
- MGS-0028[4]
- LY404040[5]
- LY379268[6]
- LY354740[7]; njegov (+)-C4α-metil analog je GluR2 agonist / GluR3 antagonist[8]
- (R)-2-amino-4-(4-hidroksi[1,2,5]tiadiazol-3-il)buterna kiselina[9]
Alosterni modulatori
- MNI-137[13]: inhibitor
- jedinjenje 7p[14]: nekompetitivni antagonist
Metabotropni glutamatni receptor 3 formira interakcije sa GRIP1,[15] PICK1[15] i PPM1A.[16]
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