Repinotan

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Repinotan
Repinotan.png
IUPAC ime
(R)-(-)-2-[4-[(hroman-2-ilmetil)-amino]-butil]-1,1-diokso-benzo[d]izotiazolon
Klinički podaci
Način primeneOralno
Pravni status
Pravni status
  • Nije kontrolisana supstanca
Identifikatori
CAS broj144980-29-0 ДаY
ATC kodnone
PubChemCID 198757
UNII05PB82Z52L ДаY
ChEMBLCHEMBL1614652 ДаY
Hemijski podaci
FormulaC21H24N2O4S
Molarna masa400,491 g/mol

Repinotan (BAYx3702) je selektivni pun agonist 5-HT1A receptor visoke potentnosti i efikasnosti.[1][2] On ima neuroprotektivno dejstvo u životinjskim studijama,[3][4][5] i bio je u kliničkim ispitivanjima za primenu u redukovanju oštećenja mozga nakon povrede glave.[6] 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.[7][8][9]

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.[10]

Reference[уреди]

  1. ^ 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. 
  2. ^ 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. 
  3. ^ 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. PMID 10536203. doi:10.1016/S0006-8993(99)01948-4. 
  4. ^ 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. PMID 11591455. doi:10.1016/S0306-4522(01)00300-1. 
  5. ^ 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. PMID 15674237. doi:10.1038/sj.jcbfm.9600038. 
  6. ^ 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. PMID 11780862. doi:10.1089/08977150152725614. 
  7. ^ 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. PMID 15857296. doi:10.2174/1568007053544165. 
  8. ^ 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. PMID 16614737. doi:10.1111/j.1527-3458.2005.tb00055.x. 
  9. ^ 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. PMID 19745176. doi:10.1161/STROKEAHA.109.551382. 
  10. ^ Guenther U, Wrigge H, Theuerkauf N, Boettcher MF, Wensing G, Zinserling J, Putensen C, Hoeft A (2010). „Repinotan, a selective 5-HT1A-R-agonist, antagonizes morphine-induced ventilatory depression in anesthetized rats”. Anesthesia and Analgesia. 111 (4): 901—7. PMID 20802053. doi:10.1213/ANE.0b013e3181eac011. 

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