Repinotan

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Repinotan
(IUPAC) ime
(R)-(-)-2-[4-[(hroman-2-ilmetil)-amino]-butil]-1,1-diokso-benzo[d]izotiazolon
Klinički podaci
Identifikatori
CAS broj 144980-29-0
ATC kod nije dodeljen
PubChem[1][2] 198757
UNII 05PB82Z52L YesY
ChEMBL[3] CHEMBL1614652 YesY
Hemijski podaci
Formula C21H24N2O4S 
Mol. masa 400,491 g/mol
SMILES eMolekuli & PubHem
Farmakoinformacioni podaci
Trudnoća  ?
Pravni status Nije kontrolisana supstanca
Način primene Oralno

Repinotan (BAYx3702) je selektivni pun agonist 5-HT1A receptor visoke potentnosti i efikasnosti.[4][5] On ima neuroprotektivno dejstvo u životinjskim studijama,[6][7][8] i bio je u kliničkim ispitivanjima za primenu u redukovanju oštećenja mozga nakon povrede glave.[9] Naknadno je ispitivan u fazi II za tretman moždanog udara. Dok su nuspojave bile blage i sastojale se uglavnom od mučnine, repinotan nije bio dovoljno efikasan da bi se opravdala dalja klinička ispitivanja.[10][11][12]

Repinotan se i dalje istražuje za druge moguće primene. Utvrđeno je da je efektivan za tretiranje respiratorne depresije proizvedene morfinom, mada u proizvodi malo umanjenje analgetskog dejstva.[13]

Reference[uredi - уреди | uredi izvor]

  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. Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). "ChEMBL: a large-scale bioactivity database for drug discovery". Nucleic Acids Res 40 (Database issue): D1100–7. doi:10.1093/nar/gkr777. PMID 21948594.  edit
  4. De Vry, J.; Schohe-Loop, R.; Heine, H. G.; Greuel, J. M.; Mauler, F.; Schmidt, B.; Sommermeyer, H.; Glaser, T. (1998). "Characterization of the aminomethylchroman derivative BAY x 3702 as a highly potent 5-hydroxytryptamine1A receptor agonist". The Journal of Pharmacology and Experimental Therapeutics 284 (3): 1082–1094. PMID 9495870. 
  5. Dong, J.; De Montigny, C.; Blier, P. (1998). "Full agonistic properties of BAY x 3702 on presynaptic and postsynaptic 5-HT1A receptors electrophysiological studies in the rat hippocampus and dorsal raphe". The Journal of Pharmacology and Experimental Therapeutics 286 (3): 1239–1247. PMID 9732384. 
  6. Alessandri, B.; Tsuchida, E.; Bullock, R. M. (1999). "The neuroprotective effect of a new serotonin receptor agonist, BAY X3702, upon focal ischemic brain damage caused by acute subdural hematoma in the rat". Brain Research 845 (2): 232–235. doi:10.1016/S0006-8993(99)01948-4. PMID 10536203. 
  7. Kline, A. E.; Yu, J.; Horváth, E.; Marion, D. W.; Dixon, C. E. (2001). "The selective 5-HT(1A) receptor agonist repinotan HCl attenuates histopathology and spatial learning deficits following traumatic brain injury in rats". Neuroscience 106 (3): 547–555. doi:10.1016/S0306-4522(01)00300-1. PMID 11591455. 
  8. Mauler, F.; Horváth, E. (2005). "Neuroprotective efficacy of repinotan HCl, a 5-HT1A receptor agonist, in animal models of stroke and traumatic brain injury". Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism 25 (4): 451–459. doi:10.1038/sj.jcbfm.9600038. PMID 15674237. 
  9. Ohman, J.; Braakman, R.; Legout, V.; Traumatic Brain Injury Study Group (2001). "Repinotan (BAY x 3702): a 5HT1A agonist in traumatically brain injured patients". Journal of neurotrauma 18 (12): 1313–1321. doi:10.1089/08977150152725614. PMID 11780862. 
  10. Lutsep, H. L. (2005). "Repinotan, A 5-HT1A agonist, in the treatment of acute ischemic stroke". Current drug targets. CNS and neurological disorders 4 (2): 119–120. doi:10.2174/1568007053544165. PMID 15857296. 
  11. Berends, A. C.; Luiten, P. G.; Nyakas, C. (2005). "A review of the neuroprotective properties of the 5-HT1A receptor agonist repinotan HCl (BAYx3702) in ischemic stroke". CNS Drug Reviews 11 (4): 379–402. doi:10.1111/j.1527-3458.2005.tb00055.x. PMID 16614737. 
  12. Teal, P.; Davis, S.; Hacke, W.; Kaste, M.; Lyden, P.; Modified Randomized Exposure Controlled Trial Study Investigators; Fierus, M.; Bayer Healthcare, A. (2009). "A randomized, double-blind, placebo-controlled trial to evaluate the efficacy, safety, tolerability, and pharmacokinetic/pharmacodynamic effects of a targeted exposure of intravenous repinotan in patients with acute ischemic stroke: modified Randomized Exposure Controlled Trial (mRECT)". Stroke; a journal of cerebral circulation 40 (11): 3518–3525. doi:10.1161/STROKEAHA.109.551382. PMID 19745176. 
  13. Guenther U, Wrigge H, Theuerkauf N, Boettcher MF, Wensing G, Zinserling J, Putensen C, Hoeft A (October 2010). "Repinotan, a selective 5-HT1A-R-agonist, antagonizes morphine-induced ventilatory depression in anesthetized rats". Anesthesia and Analgesia 111 (4): 901–7. doi:10.1213/ANE.0b013e3181eac011. PMID 20802053. 

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