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Indeloxazine
Systematic (IUPAC) name
2-(3H-inden-4-yloxymethyl)morpholine
Identifiers
CAS number 60929-23-9
ATC code  ?
PubChem 3704
Chemical data
Formula C 14H17NO2  
Mol. mass 231.290 g/mol
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.  ?
Legal status
Routes Oral

Indeloxazine (Elen, Noin) is a so-called cerebral activator used in Japan for the treatment of cerebrovascular disease. [1] It was launched in 1988. [2]

Indeloxazine acts as a serotonin releasing agent and norepinephrine reuptake inhibitor.[3] It also acts as an NMDA receptor antagonist.[4] It enhances acetylcholine release through indirect activation of the 5-HT4 receptor.[5][6][7] Indeloxazine has nootropic,[8][9][6][7] neuroprotective,[10][11][12][13] anticonvulsant,[14] and antidepressant effects.[15][16][3]

References

  1. ^ "Index nominum, international drug ... - Google Books". http://books.google.com/books?id=5GpcTQD_L2oC&lpg=PA548&dq=indeloxazine&as_brr=3&pg=PA548#v=onepage&q=indeloxazine&f=false.  
  2. ^ "Dictionary of pharmacological agents - Google Books". http://books.google.com/books?id=A0THacd46ZsC&lpg=PA1469&ots=IIjkfFuc65&dq=%22SC-27%2C123%22%20octriptyline&pg=PA1128#v=onepage&q=antidepressant&f=false.  
  3. ^ a b Yamaguchi T, Ohyama M, Suzuki M, et al. (September 1998). "Neurochemical and behavioral characterization of potential antidepressant properties of indeloxazine hydrochloride". Neuropharmacology 37 (9): 1169–76. PMID 9833647. http://linkinghub.elsevier.com/retrieve/pii/S0028390898000094.  
  4. ^ Kaneko S, Sugimura M, Inoue T, Satoh M (June 1991). "Effects of several cerebroprotective drugs on NMDA channel function: evaluation using Xenopus oocytes and [3H]MK-801 binding". European Journal of Pharmacology 207 (2): 119–28. PMID 1652446.  
  5. ^ Yamaguchi T, Suzuki M, Yamamoto M (December 1997). "Facilitation of acetylcholine release in rat frontal cortex by indeloxazine hydrochloride: involvement of endogenous serotonin and 5-HT4 receptors". Naunyn-Schmiedeberg's Archives of Pharmacology 356 (6): 712–20. PMID 9453456. http://link.springer.de/link/service/journals/00210/bibs/7356006/73560712.htm.  
  6. ^ a b Yamamoto M, Takahashi K, Ohyama M, et al. (May 1994). "Possible involvement of central cholinergic system in ameliorating effects of indeloxazine, a cerebral activator, on disturbance of learning behavior in rats". Progress in Neuro-psychopharmacology & Biological Psychiatry 18 (3): 603–13. PMID 8078992.  
  7. ^ a b Yamamoto M, Ooyama M, Ozawa Y, et al. (July 1993). "Effects of indeloxazine hydrochloride, a cerebral activator, on passive avoidance learning impaired by disruption of cholinergic transmission in rats". Neuropharmacology 32 (7): 695–701. PMID 8395664.  
  8. ^ Ogawa N, Haba K, Sora YH, Higashida A, Sato H, Ogawa S (1988). "Comparison of the effects of bifemelane hydrochloride and indeloxazine hydrochloride on scopolamine hydrobromide-induced impairment in radial maze performance". Clinical Therapeutics 10 (6): 704–11. PMID 3219685.  
  9. ^ Yamamoto M, Shimizu M (July 1987). "Cerebral activating properties of indeloxazine hydrochloride". Neuropharmacology 26 (7A): 761–70. PMID 3627384.  
  10. ^ Ogawa N, Haba K, Yoshikawa H, Ono T, Mizukawa K (August 1988). "Comparison of the effects of bifemelane hydrochloride, idebenone and indeloxazine hydrochloride on ischemia-induced depletion of brain acetylcholine levels in gerbils". Research Communications in Chemical Pathology and Pharmacology 61 (2): 285–8. PMID 3187197.  
  11. ^ Yamamoto M, Shimizu M, Sakamoto N, Ohtomo H, Kogure K (November 1987). "Protective effects of indeloxazine hydrochloride on cerebral ischemia in animals". Archives Internationales De Pharmacodynamie Et De Thérapie 290 (1): 16–24. PMID 3446040.  
  12. ^ Shimizu-Sasamata M, Terai M, Harada M, Yamamoto M (1993). "Anti-hypoxic and anti-ischemic actions of indeloxazine hydrochloride and its optical isomers: possible involvement of cerebral energy metabolism". Archives Internationales De Pharmacodynamie Et De Thérapie 324: 33–46. PMID 8297184.  
  13. ^ Yamamoto M, Shimizu M (April 1987). "Effects of indeloxazine hydrochloride (YM-08054) on anoxia". Archives Internationales De Pharmacodynamie Et De Thérapie 286 (2): 272–81. PMID 3592867.  
  14. ^ Nakamura J, Anraku T, Shirouzu M, Iwashita Y, Nakazawa Y (June 1993). "Effects of indeloxazine HCl on kindled amygdaloid seizures in rats: comparison with the effects of phenytoin, diazepam, ethanol, and imipramine". Pharmacology, Biochemistry, and Behavior 45 (2): 445–50. PMID 8327550.  
  15. ^ Hayes AG, Chang T (January 1983). "Determination of indeloxazine, a new antidepressant agent, in human plasma by gas-liquid chromatography with electron-capture detection". Journal of Chromatography 272 (1): 176–80. PMID 6841538.  
  16. ^ Kojima T, Niigata K, Fujikura T, et al. (September 1985). "Syntheses of (+/-)-2-[(inden-7-yloxy)methyl]morpholine hydrochloride (YM-08054, indeloxazine hydrochloride) and its derivatives with potential cerebral-activating and antidepressive properties". Chemical & Pharmaceutical Bulletin 33 (9): 3766–74. PMID 4092278.  
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