Antagonist NMDA receptora

Izvor: Wikipedia
Ketamin, prototipni antagonist NMDA receptora.

Antagonisti NMDA receptora su klasa anestetika koji antagonizuju, ili inhibiraju dejstvo, N-metil-D-aspartatnog receptora (NMDAR). Oni se koriste kao anestetici za životinje i ljude. Stanje anestezije koje oni indukuju se naziva disocijativna anestezija. Postoji evidencija da antagonisti NMDA receptora mogu da uzrokuju određene tipove neurotoksičnosti ili oštećenja mozga koja se nazivaju Olnejeve ozlede kod glodara, mada takva oštećenja nikad nisu bila ubedljivo zapažena kod primata poput čoveka. Nedavna istraživanja na primatima sugerišu da dok veoma konzistentna i dugotrajna upotreba ketamina može da bude neurotoksična, akutna primena nije.[1][2]

Nekoliko sintetičkih opioida dodatno deluju kao NMDAR antagonisti, npr. petidin, metadon, dekstropropoksifen, tramadol i ketobemidon.

Neki antagonisti NMDA receptora, kao što su ketamin, dekstrometorfan (DXM), fenciklidin (PCP), i azot-monoksid (N2O), su popularne rekreacione droge koje se koriste zbog njihovih disocijativnih, halucinogenih, i euforijantnih svojstava.

Primeri[uredi - уреди]

Kompetitivni antagonisti[uredi - уреди]

  • AP5 (APV, R-2-amino-5-fosfonopentanoat)[3]
  • AP7 (2-amino-7-fosfonoheptanska kiselina)[4]
  • Midafotel (3-[(R)-2-karboksipiperazin-4-il]-prop-2-enil-1-fosfonska kiselina)[5]
  • Selfotel: anksiolitik, antikonvulsant sa mogućim neurotoksičnim destvom.

Nekompetitivni blokatori kanala[uredi - уреди]

Nekompetitivni antagonisti[uredi - уреди]

  • Aptiganel (Cerestat, CNS-1102): vezuje se za mestove vezivanja Mg2+ u kanalu NMDA receptora.
  • HU-211: enantiomer potentnog kanabinoida HU-210 koji nema kanabinoidno dejstvo već deluje kao potentan nekompetitivni NMDA antagonist.[19]
  • Remacemid: glavni metabolit nekompetitivnog antagonista sa niskim afinitetom za mestom vezivanja.[20]
  • Rinhofilin, alkaloid.
  • Ketamin: disocijativni psihodelik sa antidepresantskim svojstvima koji se koristi za anasteziju kod ljudi i životinja[21]

Glicinski antagonisti[uredi - уреди]

Ovi lekovi deluju na mestu vezivanja glicina:

Reference[uredi - уреди]

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