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Chemical Compound Review

Repinotan     8-[4-[[(2R)-chroman-2- yl]methylamino]butyl...

Synonyms: SureCN678644, CHEMBL1614652, DNC000279, Bay x3702, AC1L55ZL, ...
 
 
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Disease relevance of Repinotan

 

Psychiatry related information on Repinotan

  • Neither Repinotan HCl nor the non-competitive N-methyl-D-aspartate receptor antagonist MK-801, which served as a positive control, improved vestibulomotor function on beam balance and beam walk tasks relative to the Injury/Vehicle group, but both did significantly attenuate spatial learning and memory deficits on a water maze task [3].
 

High impact information on Repinotan

  • Repinotan is a highly potent 5-HT1A receptor agonist with strong neuroprotective efficacy in animal models of middle cerebral artery occlusion and traumatic brain injury [1].
  • In the transient middle cerebral artery occlusion model, repinotan (10 microg/kg per hour) administered immediately after occlusion reduced infarct volume by 97%, and a delay to 5 hours reduced infarct volume by 81% [1].
  • Thus, BAY 639044 or repinotan treatment was initiated when there was 30% neuronal death in the substantia nigra pars compacta, and nerve terminal loss in the striatum was 40%, i.e., compatible with the clinical situation where early symptomatic patients would receive such a treatment [4].
  • 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 [5].
  • Repinotan treatment had no apparent adverse effects on intracranial pressure, hemodynamic parameters or laboratory parameters [5].
 

Chemical compound and disease context of Repinotan

 

Biological context of Repinotan

 

Anatomical context of Repinotan

  • The ability of repinotan to cross the blood-brain barrier (BBB) and penetrate into rat brain tissue was investigated, because rapid penetration into brain tissue is thought to be essential for neuroprotective efficacy [7].
 

Associations of Repinotan with other chemical compounds

  • The potent 5-HT1A agonist BAY x 3702, or repinotan, has reduced cortical infarct volume in pre-clinical models even when given 5 hours after injury [8].
 

Gene context of Repinotan

  • Repinotan is primarily metabolized by CYP2D6 which is known to be subject to polymorphism and ethnic differences in its quantitative and qualitative expression pattern [9].
  • Repinotan is a high-affinity, selective, full agonist of the 5HT1A-receptor subtype with neuroprotective properties [5].
  • The proposed neuroprotective mechanisms of repinotan are thought to be the result of neuronal hyperpolarization via the activation of G protein-coupled inwardly rectifying K(+) channels upon binding to both pre- and post-synaptic 5-HT(1A) receptors [6].
 

Analytical, diagnostic and therapeutic context of Repinotan

References

  1. Neuroprotective efficacy of repinotan HCl, a 5-HT1A receptor agonist, in animal models of stroke and traumatic brain injury. Mauler, F., Horváth, E. J. Cereb. Blood Flow Metab. (2005) [Pubmed]
  2. The BRAINS study: safety, tolerability, and dose-finding of repinotan in acute stroke. Teal, P., Silver, F.L., Simard, D. The Canadian journal of neurological sciences. Le journal canadien des sciences neurologiques. (2005) [Pubmed]
  3. The selective 5-HT(1A) receptor agonist repinotan HCl attenuates histopathology and spatial learning deficits following traumatic brain injury in rats. Kline, A.E., Yu, J., Horváth, E., Marion, D.W., Dixon, C.E. Neuroscience (2001) [Pubmed]
  4. 5-HT1A receptor agonist-mediated protection from MPTP toxicity in mouse and macaque models of Parkinson's disease. Bezard, E., Gerlach, I., Moratalla, R., Gross, C.E., Jork, R. Neurobiol. Dis. (2006) [Pubmed]
  5. Repinotan (BAY x 3702): a 5HT1A agonist in traumatically brain injured patients. Ohman, J., Braakman, R., Legout, V. J. Neurotrauma (2001) [Pubmed]
  6. A Review of the Neuroprotective Properties of the 5-HT(1A) Receptor Agonist Repinotan HCl (BAY x 3702) in Ischemic Stroke. Berends, A.C., Luiten, P.G., Nyakas, C. CNS drug reviews. (2005) [Pubmed]
  7. Pharmacokinetics of repinotan in healthy and brain injured animals. Schwarz, T., Beckermann, B., Buehner, K., Mauler, F., Schuhmacher, J., Seidel, D., Steinke, W., Weinz, C., Zimmerd, D. Biopharmaceutics & drug disposition. (2005) [Pubmed]
  8. Repinotan, A 5-HT1A agonist, in the treatment of acute ischemic stroke. Lutsep, H.L. Current drug targets. CNS and neurological disorders. (2005) [Pubmed]
  9. Evaluation of interethnic differences in repinotan pharmacokinetics by using population approach. Tanigawa, T., Heinig, R., Kuroki, Y., Higuchi, S. Drug Metab. Pharmacokinet. (2006) [Pubmed]
 
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