repinotan hydrochloride

5-HT(1A) receptor agonist; structure in first source

Also Known As:

2-(4-((chroman-2-ylmethyl)amino)butyl)-1,1-dioxobenzo(d)isothiazolone hydrochloride; BAY X 3702; BAY X-3702; repinotan; 1,2-Benzisothiazol-3(2H)-one, 2-(4-((((2R)-3,4-dihydro-2H-1-benzopyran-2-yl)methyl)amino)butyl)-, 1,1-dioxide, hydrochloride (1:1)

Networked: 17 relevant articles (4 outcomes, 5 trials/studies)

Relationship Network

Bio-Agent Context: Research Results

Experts

1.	Teal, Philip: 2 articles (11/2009 - 02/2005)
2.	Lutsep, Helmi L: 2 articles (04/2005 - 06/2002)
3.	Horváth, E: 2 articles (01/2001 - 01/2001)
4.	Boettcher, Michael F: 1 article (01/2012)
5.	Guenther, Ulf: 1 article (01/2012)
6.	Hoeft, Andreas: 1 article (01/2012)
7.	Huse, Daniel: 1 article (01/2012)
8.	Putensen, Christian: 1 article (01/2012)
9.	Theuerkauf, Nils U: 1 article (01/2012)
10.	Wensing, Georg: 1 article (01/2012)

Related Diseases

1.	Ischemic Stroke 01/01/2005 - "The dose- and time-dependent neuroprotective efficacy of repinotan indicates that the drug is a promising candidate for prevention of secondary brain damage in brain-injured patients suffering from acute ischemic stroke. " 01/01/2005 - "Unfortunately, however, the first, randomized, double blind, placebo-controlled clinical trial did not demonstrate the efficacy of repinotan in acute ischemic stroke." 11/01/2009 - "The purpose of this Phase IIb study was to investigate the efficacy, safety, and tolerability of a targeted exposure to repinotan in patients with acute ischemic stroke. " 11/01/2009 - "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)." 02/01/2005 - "This double-blind, placebo-controlled phase II study examined the safety, tolerability, and dose of repinotan in patients with acute ischemic stroke. "
2.	Traumatic Brain Injuries (Traumatic Brain Injury) 12/01/2001 - "This paper presents the results of a randomized, double-blind, placebo-controlled study examining the safety and tolerability of three different doses of repinotan in patients with severe traumatic brain injury. " 01/01/2001 - "Using a clinically relevant contusion model of traumatic brain injury, we tested the hypothesis that a 4-h continuous infusion of Repinotan HCl (10 microg/kg/h i.v.) commencing 5 min post-injury would ameliorate functional outcome and attenuate histopathology. " 01/01/2001 - "The selective 5-HT(1A) receptor agonist repinotan HCl attenuates histopathology and spatial learning deficits following traumatic brain injury in rats." 01/01/2005 - "Repinotan caused strong, dose-dependent infarct reductions in permanent middle cerebral artery occlusion, transient middle cerebral artery occlusion, and traumatic brain injury paradigms. " 04/01/2005 - "Neuroprotective efficacy of repinotan HCl, a 5-HT1A receptor agonist, in animal models of stroke and traumatic brain injury."
3.	Ischemia 11/01/2009 - "Repinotan hydrochloride is a serotonin (5-HT)(1A) receptor full agonist with evidence of neuroprotection in animal models of permanent and transient focal ischemia. " 02/01/2005 - "Repinotan is a potent, serotonin (5-HT1A) full receptor agonist that interferes with ischemia-mediated neuronal cell death in animal models. " 11/10/2000 - "Bay x 3702 (4 microg/kg i.v.) diminished DNA laddering in the hippocampus and striatum 4 days after 10 min forebrain ischemia. " 02/01/2005 - "Patients with acute hemispheric ischemia and a National Institutes of Health Stroke Scale of 4 to 25 were randomized to placebo or repinotan 0.5, 1.25, or 2.5 mg/day (d) given by continuous intravenous infusion for 72 hours. " 10/23/1998 - "Bay X 3702 (12 and 40 microg/kg), infused within a period of 4 h, immediately after induction of ischemia greatly reduced cortical infarct volume (57 and 55% of controls, respectively) suggesting that this drug might be useful for the treatment of acute cerebral infarction."
4.	Stroke (Strokes) 02/01/2005 - "The BRAINS study: safety, tolerability, and dose-finding of repinotan in acute stroke." 01/01/2005 - "These results indicate that gender does not affect the pharmacokinetics of repinotan in healthy subjects whose age (>/=65 years) was representative of the target patient population for repinotan in acute stroke." 02/01/2005 - "Patients with acute hemispheric ischemia and a National Institutes of Health Stroke Scale of 4 to 25 were randomized to placebo or repinotan 0.5, 1.25, or 2.5 mg/day (d) given by continuous intravenous infusion for 72 hours. " 11/10/2000 - "Since there is increasing evidence that apoptosis is involved in neurodegenerative diseases and stroke, we investigated whether the 5-HT(1A) agonist Bay x 3702 could protect neurons against apoptotic damage in a rat model of transient forebrain cerebral ischemia. " 04/01/2005 - "Neuroprotective efficacy of repinotan HCl, a 5-HT1A receptor agonist, in animal models of stroke and traumatic brain injury."
5.	Brain Injuries (Brain Injury) 01/01/2005 - "Experimental studies indicate that repinotan affects various mechanisms involved in the pathogenesis of brain injury. " 06/01/2002 - "Repinotan was being developed initially as an i.v. formulation for the treatment of ischemic stroke and brain injury and as an oral formulation for the treatment of depression; however, development has been discontinued for the latter indication [317452]. " 01/05/2001 - "The aminomethylchroman derivative BAY x 3702 is a novel neuroprotectant which shows pronounced beneficial effects in various animal models of ischemic brain injury. " 01/01/2001 - " findings extend the therapeutic efficacy of Repinotan HCl to a contusion model of experimental brain injury and demonstrate for the first time that 5-HT(1A) receptor agonists confer neuroprotection and attenuate spatial learning deficits following controlled cortical impact injury. " 01/01/2005 - "Repinotan HCl (repinotan, BAYx3702), a highly selective 5-HT1A receptor agonist with a good record of safety was found to have pronounced neuroprotective effects in experimental models that mimic various aspects of brain injury. "

Related Drugs and Biologics

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3.	N-Methyl-D-Aspartate Receptors (NMDA Receptors)
4.	Glutamic Acid (Glutamate)
5.	Potassium
6.	repinotan hydrochloride
7.	Neuroprotective Agents
8.	Serotonin 5-HT1 Receptor Agonists
9.	8-Hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT)
10.	Serotonin (5 Hydroxytryptamine)

Related Therapies and Procedures

1.	Intravenous Infusions