Matches in SemOpenAlex for { <https://semopenalex.org/work/W1485553721> ?p ?o ?g. }
Showing items 1 to 57 of
57
with 100 items per page.
- W1485553721 abstract "The G1uN3 subunits of the NMDA receptor are thought to reduce the Ca 2+ permeability and Mg2+ sensitivity of NMDA receptors. cRNA for rat NMDA receptor subunits were injected into Xenopus oocytes and responses were recorded using two electrode voltage clamp at -100, -75 and -50 mV. G1uN1-1a/2A, GluN1-1a/2A/3A and G1uN1-1a/2A/3B containing receptors were characterised using Mgz+, memantine, philanthotoxin-343, methoctramine and MK-801. IC50 values were calculated and generally showed significant increases between those containing G1uN1-1a/2A/3 subunits and G1uN1-1a/2A, while those with G1uN3B were found to be significantly higher than G1uN3A. Activity was also typically shown to be partially restored with mutations at the N and N+1 site asparagines of G1uN3A. As the ICS0 was only partially restored the changes cannot be attributed to the loss of the N-site alone. Further differences may be due to a constricted threonine ring within the M3 vestibule region, or due to continued reduced flux through the channel. Another possibility is that to restore block it may require both the double N and N+1 mutation at the N-site.Multi-target-directed ligands combine two pharmacophores to produce drugs which retain the properties of the constituents. Memantine has been approved for use in Alzheimer's disease and there is a search for drugs that have similar actions. A range of multi-target compounds were tested to determine if NMDA receptor blockade activity was obtained. The pharmacophores explored were tacrine, donepezil, lipoic acid carvedilol and dimebon. The most promising compounds were carbacrine(3) (tacrine and carvedilol) and lipocrine (lipoic acid and tacrine), and it was found that the former was equipotent and the latter more potent than memantine. Potency was likely due to the tacrine moiety. These compounds should be further categorised to determine if they retain the kinetics that gives memantine its favourable side effect profile." @default.
- W1485553721 created "2016-06-24" @default.
- W1485553721 creator A5005376832 @default.
- W1485553721 date "2011-07-15" @default.
- W1485553721 modified "2023-09-27" @default.
- W1485553721 title "Exploring open channel block of the NMDA receptor" @default.
- W1485553721 hasPublicationYear "2011" @default.
- W1485553721 type Work @default.
- W1485553721 sameAs 1485553721 @default.
- W1485553721 citedByCount "0" @default.
- W1485553721 crossrefType "dissertation" @default.
- W1485553721 hasAuthorship W1485553721A5005376832 @default.
- W1485553721 hasConcept C12554922 @default.
- W1485553721 hasConcept C170493617 @default.
- W1485553721 hasConcept C185592680 @default.
- W1485553721 hasConcept C2779484449 @default.
- W1485553721 hasConcept C55493867 @default.
- W1485553721 hasConcept C67018056 @default.
- W1485553721 hasConcept C71240020 @default.
- W1485553721 hasConcept C86803240 @default.
- W1485553721 hasConcept C98274493 @default.
- W1485553721 hasConceptScore W1485553721C12554922 @default.
- W1485553721 hasConceptScore W1485553721C170493617 @default.
- W1485553721 hasConceptScore W1485553721C185592680 @default.
- W1485553721 hasConceptScore W1485553721C2779484449 @default.
- W1485553721 hasConceptScore W1485553721C55493867 @default.
- W1485553721 hasConceptScore W1485553721C67018056 @default.
- W1485553721 hasConceptScore W1485553721C71240020 @default.
- W1485553721 hasConceptScore W1485553721C86803240 @default.
- W1485553721 hasConceptScore W1485553721C98274493 @default.
- W1485553721 hasLocation W14855537211 @default.
- W1485553721 hasOpenAccess W1485553721 @default.
- W1485553721 hasPrimaryLocation W14855537211 @default.
- W1485553721 hasRelatedWork W1783376942 @default.
- W1485553721 hasRelatedWork W1947219617 @default.
- W1485553721 hasRelatedWork W1974902468 @default.
- W1485553721 hasRelatedWork W1983473217 @default.
- W1485553721 hasRelatedWork W1995683118 @default.
- W1485553721 hasRelatedWork W2003899301 @default.
- W1485553721 hasRelatedWork W2023811229 @default.
- W1485553721 hasRelatedWork W2025636335 @default.
- W1485553721 hasRelatedWork W2036547627 @default.
- W1485553721 hasRelatedWork W2056560960 @default.
- W1485553721 hasRelatedWork W2097194551 @default.
- W1485553721 hasRelatedWork W2103103822 @default.
- W1485553721 hasRelatedWork W2121504583 @default.
- W1485553721 hasRelatedWork W2139680626 @default.
- W1485553721 hasRelatedWork W2152072736 @default.
- W1485553721 hasRelatedWork W2402227851 @default.
- W1485553721 hasRelatedWork W2409768949 @default.
- W1485553721 hasRelatedWork W2802179882 @default.
- W1485553721 hasRelatedWork W2951127928 @default.
- W1485553721 hasRelatedWork W3104793255 @default.
- W1485553721 isParatext "false" @default.
- W1485553721 isRetracted "false" @default.
- W1485553721 magId "1485553721" @default.
- W1485553721 workType "dissertation" @default.