IDRA-21

IDRA-21
(IUPAC) ime
	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	3688
Hemijski podaci
Formula	C8H9ClN2O2S
Mol. masa	232,68726 g/mol
SMILES	eMolekuli & PubHem
InChI
	InChI=1S/C8H9ClN2O2S/c1-5-10-7-3-2-6(9)4-8(7)14(12,13)11-5/h2-5,10-11H,1H3 ; Key: VZRNTCHTJRLTMU-UHFFFAOYSA-N
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 uredi

↑ 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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[1] 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

[2] 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.

[3] 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.

[4] 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.

[5] 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.

[6] 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.

[7] 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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