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Robalzotan

Izvor: Wikipedija
Robalzotan
(IUPAC) ime
(3R)-3-[di(ciklobutil)amino]-8-fluoro-3,4-dihidro-2H-hromen-5-karboksamid
Klinički podaci
Identifikatori
CAS broj 169758-66-1
ATC kod nije dodeljen
PubChem[1][2] 3055171
UNII I18M56OGME DaY
Hemijski podaci
Formula C18H23FN2O2 
Mol. masa 318,174 g/mol
SMILES eMolekuli & PubHem
Farmakoinformacioni podaci
Trudnoća ?
Pravni status Nije kontrolisan
Način primene Oralno

Robalzotan (NAD-299, AZD-7371) je selektivni antagonist 5-HT1A receptora.[3] Pokazano je u studijama na glodarima da robalzotan kompletno preokreće autoreceptorom posredovanu inhibiciju otpuštanja serotonina indukovanu administracijom selektivnih inhibitora serotoninskog preuzimanja poput citaloprama.[4] On je naknadno istraživan kao potencijalni antidepresiv ali su ta istraživanja poput mnogih drugih 5-HT1A agonista prekinuta.[5] On je isto tako istraživan za druge indikacije kao što je sindrom iritabilnih creva.[6]

Reference

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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. Jerning E, Svantesson GT, Mohell N. (1998). „Receptor binding characteristics of [3H]NAD-299, a new selective 5-HT1A receptor antagonist.”. Eur J Pharmacol. 360 (2-3): 219–225. DOI:10.1016/S0014-2999(98)00667-0. PMID 9851589. 
  4. Arborelius L, Wallsten C, Ahlenius S, Svensson TH. (1999). „The 5-HT(1A) receptor antagonist robalzotan completely reverses citalopram-induced inhibition of serotonergic cell firing.”. Eur J Pharmacol. 382 (2): 133–138. DOI:10.1016/S0014-2999(99)00592-0. PMID 10528148. 
  5. Mucke HA. (2000). „Robalzotan AstraZeneca.”. Curr Opin Investig Drugs. 1 (2): 236–240. PMID 11249580. 
  6. Drossman DA, Danilewitz M, Naesdal J, Hwang C, Adler J, Silberg DG (October 2008). „Randomized, double-blind, placebo-controlled trial of the 5-HT1A receptor antagonist AZD7371 tartrate monohydrate (robalzotan tartrate monohydrate) in patients with irritable bowel syndrome”. The American Journal of Gastroenterology 103 (10): 2562–9. DOI:10.1111/j.1572-0241.2008.02115.x. PMID 18775020. 

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