IDRA-21
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(IUPAC) ime | |||
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7-hloro-3-metil-3,4-dihidro-2H-1,2,4-benzotiadiazin 1,1-dioksid | |||
Klinički podaci | |||
Identifikatori | |||
CAS broj | 22503-72-6 | ||
ATC kod | nije dodeljen | ||
PubChem[1][2] | 3688 | ||
Hemijski podaci | |||
Formula | C8H9ClN2O2S | ||
Mol. masa | 232,68726 g/mol | ||
SMILES | eMolekuli & PubHem | ||
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Sinonimi | IDRA-21 | ||
Farmakoinformacioni podaci | |||
Trudnoća | ? | ||
Pravni status | Lek u razvoju |
IDRA-21 je ampakinski lek izveden iz aniracetama. IDRA-21 je hiralni molekul, pri čemu je (+)-IDRA-21 aktivna forma.[3]
IDRA-21 pokazuje nootropine efekte u životinjskim studijama, sa znatno poboljšanim učenjem i memorijom. On je oko 10-30 puta potentniji od aniracetama u reverznim kognitivnim deficitima indukovanim alprazolamom ili skopolaminom,[4][5] i proizvodi znatne efekte koji traju do tri dana nakon jedne doze.[6] Smatra se da je mehanizam akcije promovisanje indukcije dugotrajne potencijacije između sinapsi mozga.[7]
Reference
- ↑ Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519. edit
- ↑ Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1.
- ↑ Uzunov, DP; Zivkovich, I; Pirkle, WH; Costa, E; Guidotti, A (August 1995). „Enantiomeric resolution with a new chiral stationary phase of 7-chloro-3-methyl-3,4-dihydro-2H-1,2,4-benzothiadiazine S,S-dioxide, a cognition-enhancing benzothiadiazine derivative”. Journal of pharmaceutical sciences 84 (8): 937–42. DOI:10.1002/jps.2600840807. ISSN 0022-3549. PMID 7500277.
- ↑ Thompson, DM; Guidotti, A; Dibella, M; Costa, E (Aug 1995). „7-Chloro-3-methyl-3,4-dihydro-2H-1,2,4-benzothiadiazine S,S-dioxide (IDRA 21), a congener of aniracetam, potently abates pharmacologically induced cognitive impairments in patas monkeys”. Proceedings of the National Academy of Sciences of the United States of America 92 (17): 7667–71. DOI:10.1073/pnas.92.17.7667. ISSN 0027-8424. PMC 41206. PMID 7644474.
- ↑ Zivkovic, I; Thompson, DM; Bertolino, M; Uzunov, D; Dibella, M; Costa, E; Guidotti, A (Jan 1995). „7-Chloro-3-methyl-3-4-dihydro-2H-1,2,4 benzothiadiazine S,S-dioxide (IDRA 21): a benzothiadiazine derivative that enhances cognition by attenuating DL-alpha-amino-2,3-dihydro-5-methyl-3-oxo-4-isoxazolepropanoic acid (AMPA) receptor desensitization”. The Journal of Pharmacology and Experimental Therapeutics 272 (1): 300–9. ISSN 0022-3565. PMID 7815345.
- ↑ Buccafusco, JJ; Weiser, T; Winter, K; Klinder, K; Terry, AV (Jan 2004). „The effects of IDRA 21, a positive modulator of the AMPA receptor, on delayed matching performance by young and aged rhesus monkeys”. Neuropharmacology 46 (1): 10–22. DOI:10.1016/j.neuropharm.2003.07.002. ISSN 0028-3908. PMID 14654093.
- ↑ Arai, A; Guidotti, A; Costa, E; Lynch, G (Sep 1996). „Effect of the AMPA receptor modulator IDRA 21 on LTP in hippocampal slices”. NeuroReport 7 (13): 2211–5. DOI:10.1097/00001756-199609020-00031. ISSN 0959-4965. PMID 8930991.
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Agonisti: Neselektivni: ACPD • DHPG • Kuiskualinska kiselina; mGlu1-selektivni: Ro01-6128 • Ro67-4853 • Ro67-7476 • VU-71; mGlu5-selektivni: ADX-47273 • CDPPB • CHPG • DFB • VU-1545 Antagonisti: Neselektivni: MCPG • NPS-2390; mGlu1-selektivni: BAY 36-7620 • CPCCOEt • LY-367,385 • LY-456,236; mGlu5-selektivni: DMeOB • Fenobam • LY-344,545 • MPEP • MTEP • SIB-1757 • SIB-1893 | |
Agonisti: Neselektivni: CBiPES • DCG-IV • Eglumegad • LY-379,268 • LY-404,039 • LY-487,379 • MGS-0028; mGlu2-selektivni: BINA • LY-566,332 Antagonisti: Neselektivni: APICA • EGLU • HYDIA • LY-307,452 • LY-341,495 • MCPG • MGS-0039; mGlu2-selektivni: PCCG-4; mGlu3-selektivni: CECXG; Negativni alosterni modulatori: RO4491533 | |
transporta
DHKA • PDC • WAY-213,613 | |
vGluT |