Indeloxazine

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Indeloxazine
Indeloxazine.svg
Systematic (IUPAC) name
2-(3H-inden-4-yloxymethyl)morpholine
Clinical data
Legal status Prescription only
Routes Oral
Pharmacokinetic data
Half-life 2.2 hours
Identifiers
CAS number 60929-23-9 YesY
ATC code None
PubChem CID 3704
ChemSpider 3576 YesY
UNII 834M09R1KM YesY
KEGG D08077 YesY
Chemical data
Formula C14H17NO2 
Mol. mass 231.290 g/mol
 YesY (what is this?)  (verify)

Indeloxazine (Elen, Noin) is a so-called cerebral activator which has been used in Japan for the treatment of cerebrovascular disease since 1988.[1][2] It acts as a serotonin releasing agent,[3] norepinephrine reuptake inhibitor,[3] and NMDA receptor antagonist,[4] and enhances acetylcholine release through indirect activation of the 5-HT4 receptor.[5][6][7] It has nootropic,[6][7][8][9] neuroprotective,[10][11][12][13] anticonvulsant,[14] and antidepressant effects.[3][15][16]

See also[edit]

References[edit]

  1. ^ Index nominum, international drug ... - Google Books. 2000. ISBN 978-3-88763-075-1. 
  2. ^ r Ganellin, C; j Triggle, D; MacDonald, F. (1997). Dictionary of pharmacological agents - Google Books. ISBN 978-0-412-46630-4. 
  3. ^ a b c 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. doi:10.1016/S0028-3908(98)00009-4. PMID 9833647. 
  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. doi:10.1016/0922-4106(91)90086-W. 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. doi:10.1007/PL00005110. PMID 9453456. 
  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. doi:10.1016/0278-5846(94)90016-7. 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. doi:10.1016/0028-3908(93)90083-F. 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. doi:10.1016/0028-3908(87)90239-5. 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. doi:10.1016/0091-3057(93)90263-S. 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. doi:10.1016/S0378-4347(00)86115-0. 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. doi:10.1248/cpb.33.3766. PMID 4092278.