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tirilazad

a lazaroid; potent inhibitor of iron-dependent lipid peroxidation; has shown excellent activity in in vivo models of experimental central nervous system trauma & ischemia; structure given in first source; tradename Freedox

Also Known As:

21-(4-(2,6-di-1-pyrrolidinyl-4-pyrimidinyl)-1-piperazinyl)-16-methylpregna-1,4,9(11)-triene-3,20-dione monomethane sulfonate; Freedox; Pharmacia brand of tirilazad mesylate hydrate; U 74006F; U-74006; U-74006F; U74006F; tirilazad mesylate; tirilazad mesylate hydrate; Pregna-1,4,9(11)-triene-3,20-dione, 21-(4-(2,6-di-1-pyrrolidinyl-4-pyrimidinyl)-1-piperazinyl)-16-methyl-, (16alpha)-, monomethanesulfonate

Networked: 213 relevant articles (46 outcomes, 74 trials/studies)

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Bio-Agent Context: Research Results

Polycyclic Compounds: 56
- Steroids: 18537
  - Pregnanes: 3
    - Pregnatrienes
      - tirilazad: 213

Experts

1.	Macdonald, R Loch: 8 articles (06/2013 - 10/2003)
2.	Ilodigwe, Don: 3 articles (06/2013 - 01/2009)
3.	Steyerberg, Ewout W: 3 articles (10/2010 - 09/2002)
4.	Marshall, Lawrence F: 3 articles (02/2006 - 09/2002)
5.	Zausinger, Stefan: 3 articles (10/2004 - 06/2003)
6.	Schmid-Elsaesser, Robert: 3 articles (10/2004 - 06/2003)
7.	Torner, James: 2 articles (06/2013 - 01/2013)
8.	Murray, Gordon D: 2 articles (01/2013 - 02/2006)
9.	Tolentino, Jocelyn: 2 articles (02/2009 - 02/2007)
10.	Jang, Yeon Gyoe: 2 articles (02/2009 - 01/2009)

Related Diseases

1.	Spinal Cord Injuries (Spinal Cord Injury) 12/01/1995 - "Tirilazad and related compounds have been found to be highly beneficial in spinal cord trauma. " 06/01/1993 - "One of these, tirilazad mesylate (U-74006F), has been shown to be quite effective in animal models of brain and spinal cord injury and is the subject of phase III clinical trials. " 05/01/1992 - "One of these, tirilazad mesylate (U-74006F), has been shown to be effective in animal models of brain and spinal cord injury and is currently the subject of phase II clinical trials. " 03/01/1992 - "Efficacy of the 21-aminosteroid U74006F in improving neurological recovery after spinal cord injury in rats." 01/01/1991 - "These results suggest that after weight-induced spinal cord trauma, U74006F is associated with improved neurologic function in moderately injured, but not severely injured animals."
2.	Brain Ischemia (Cerebral Ischemia) 05/09/1994 - "The protective effects of the 21-aminosteroid tirilazad mesylate (U-74006F), one of the most efficacious inhibitors of free radical-initiated lipid peroxidation, against ischemic brain damage particularly in permanent focal cerebral ischemia still remain controversial. " 02/01/1997 - "These results document the neuroprotective efficacy of tirilazad mesylate in cerebral ischemia." 06/01/1999 - "Mortality rates and overall outcome, assessed using the Glasgow Outcome Scale at 3 months post-SAH, were not different between the two groups, despite a significantly lower incidence of delayed cerebral ischemia in patients given tirilazad. " 01/01/1996 - "Since tirilazad appears to have little or no behavioral or physiologic side effects, it appears to be an ideal agent for widespread brain ischemia prophylaxis. " 05/09/1994 - "Dose-response analysis of the effect of 21-aminosteroid tirilazad mesylate (U-74006F) upon neurological outcome and ischemic brain damage in permanent focal cerebral ischemia."
3.	Subarachnoid Hemorrhage (Aneurysmal Subarachnoid Hemorrhage) 06/01/1999 - "To test the safety and efficacy of high-dose (15 mg/kg/day) tirilazad mesylate in women suffering from aneurysmal subarachnoid hemorrhage (SAH), a prospective randomized, double-blind, vehicle-controlled trial (parallel to the one conducted in Europe, Australia, New Zealand, and South Africa) was performed at 65 North American neurosurgical centers. " 10/01/1997 - "These results suggest that gender differences do not significantly effect the blood-brain barrier protective efficacy of tirilazad following subarachnoid hemorrhage in the rat." 10/01/1997 - "The purpose of the present study was to compare the efficacy of tirilazad in attenuating early post-subarachnoid hemorrhage-induced blood-brain barrier damage in the rat, a species in which single-dose metabolism of the drug is comparable between males and females. " 03/01/1997 - "To test the safety and efficacy of tirilazad mesylate, a nonglucocorticoid 21-aminosteroid, in improving the outcome of patients with aneurysmal subarachnoid hemorrhage (SAH), 902 patients were enrolled in a prospective randomized, double-blind, vehicle-controlled trial at 54 North American neurosurgical centers. " 01/01/2013 - "The approach of Bayesian neural networks with fuzzy logic inferences was applied to data from five trials of Tirilazad for aneurysmal subarachnoid hemorrhage (3551 patients). "
4.	Ischemia 02/01/2007 - "Systematic review and meta-analysis of studies describing the efficacy of tirilazad in animal models of focal ischemia, in which outcome was measured as infarct volume and/or neurological score. " 10/01/1994 - "Treatment with U-74006F (two bolus doses of 3 mg/kg each; the first dose was injected i.v. 30 min before ischemia and the second dose, at the time of reflow) reduced the hepatic injury by 60% at 4 hr of reperfusion, improved the survival rate from 18% to 55% and decreased the degree of hepatic injury at 48 hr of reperfusion. " 05/01/1996 - "However, U-74006F protected hepatocytes significantly against membrane damage induced by cell swelling due to perfusion with hypotonic medium or ischemia-reperfusion. " 05/01/1996 - "Treatment with U-74006F (two bolus doses of 3 mg/kg each; the first dose was injected i.v. 30 min before ischemia and the second dose, at the time of reflow) reduced hepatic injury by 60% but had no significant effect on either parameter of lipid peroxidation. " 01/01/1995 - "Thus, tirilazad acts during early reperfusion to prevent secondary metabolic decay associated with severe acidotic ischemia.(ABSTRACT TRUNCATED AT 250 WORDS)"
5.	Stroke (Strokes) 01/01/2001 - "To assess whether tirilazad mesylate is safe and effective at improving outcome in patients with acute ischaemic stroke. " 09/01/2000 - "We performed a systematic review of randomized, controlled trials that assessed the safety and efficacy of tirilazad in patients with acute ischemic stroke. " 09/01/2000 - "As a result, clinical studies were undertaken to assess the safety and efficacy of tirilazad in the treatment of acute ischemic stroke. " 02/01/2007 - "Systematic review and meta-analysis of the efficacy of tirilazad in experimental stroke." 11/01/1992 - "The efficacy of U74006F in reducing cerebral infarct size was investigated in a rabbit model of thromboembolic stroke. "

Related Drugs and Biologics

1.	tirilazad
2.	Magnesium
3.	Methylprednisolone
4.	Mesylates (Mesylate)
5.	Glutamic Acid (Glutamate)
6.	Vitamin E
7.	Dizocilpine Maleate (Dizocilpine)
8.	N-Methyl-D-Aspartate Receptors (NMDA Receptors)
9.	Insulin (Novolin)
10.	Diazepam (Valium)

Related Therapies and Procedures

1.	Transplantation (Transplant Recipients)
2.	Drug Therapy (Chemotherapy)
3.	Axotomy
4.	Angioplasty (Angioplasty, Transluminal)
5.	Induced Hypothermia