Repinotan

Repinotan
IUPAC ime
	(R)-(-)-2-[4-[(hroman-2-ilmetil)-amino]-butil]-1,1-diokso-benzo[d]izotiazolon
Klinički podaci
Način primene	Oralno
Pravni status
Pravni status	Nije kontrolisana supstanca;
Identifikatori
CAS broj	144980-29-0
ATC kod	none
PubChem	CID 198757
UNII	05PB82Z52L
ChEMBL	CHEMBL1614652
Hemijski podaci
Formula	C21H24N2O4S
Molarna masa	400,491 g/mol
	SMILES C1CC2=CC=CC=C2O[C@H]1CNCCCCN3C(=O)C4=CC=CC=C4S3(=O)=O; ;

Repinotan (BAYx3702) je selektivni pun agonist 5-HT_1A 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

^ 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.
^ 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.
^ 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.
^ 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.
^ 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.
^ 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.
^ 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.
^ 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.
^ 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.
^ 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.

Vidi još уреди

Robalzotan

Spoljašnje veze 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.

[pmid20802053-10] 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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