Indeloxazine Explained

Indeloxazine (INN) (Elen, Noin) is an antidepressant and cerebral activator[1] [2] that was marketed in Japan and South Korea by Yamanouchi Pharmaceutical Co., Ltd for the treatment of psychiatric symptoms associated with cerebrovascular diseases, namely depression resulting from stroke, emotional disturbance, and avolition.[3] [4] It was marketed from 1988[4] to 1998, when it was removed from the market reportedly for lack of effectiveness.[5]

Indeloxazine acts as a serotonin releasing agent, norepinephrine reuptake inhibitor, and NMDA receptor antagonist.[6] [7] It has been found to enhance acetylcholine release in the rat forebrain through activation of the 5-HT4 receptor via its action as a serotonin releasing agent.[8] [9] [10] The drug has been found to possess nootropic,[11] [12] neuroprotective,[13] [14] [15] [16] anticonvulsant,[17] and antidepressant-like effects in animal models.[6]

Notes and References

  1. Kojima T, Niigata K, Fujikura T, Tachikawa S, Nozaki Y, Kagami S, Takahashi K . 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 . 3766–3774 . September 1985 . 4092278 . 10.1248/cpb.33.3766 . free .
  2. Hayes AG, Chang T . Determination of indeloxazine, a new antidepressant agent, in human plasma by gas-liquid chromatography with electron-capture detection . Journal of Chromatography . 272 . 1 . 176–180 . January 1983 . 6841538 . 10.1016/s0378-4347(00)86115-0 .
  3. Book: Index nominum, international drug ... - Google Books . 978-3-88763-075-1 . 2000 . Taylor & Francis .
  4. Book: Dictionary of pharmacological agents - Google Books . 978-0-412-46630-4 . Ganellin CR, Triggle JD, MacDonald F . 1997 . CRC Press .
  5. Hayashi K, Hashimoto K, Yanagi M, Umeda T, Hama R . Drug approval in Japan questioned . Lancet . 352 . 9126 . 491 . August 1998 . 9708787 . 10.1016/s0140-6736(05)79232-1 . 43687432 . free .
  6. Yamaguchi T, Ohyama M, Suzuki M, Ozawa Y, Hatanaka K, Hidaka K, Yamamoto M . Neurochemical and behavioral characterization of potential antidepressant properties of indeloxazine hydrochloride . Neuropharmacology . 37 . 9 . 1169–1176 . September 1998 . 9833647 . 10.1016/s0028-3908(98)00009-4 . 12707551 .
  7. Kaneko S, Sugimura M, Inoue T, Satoh M . Effects of several cerebroprotective drugs on NMDA channel function: evaluation using Xenopus oocytes and [3H]MK-801 binding . European Journal of Pharmacology . 207 . 2 . 119–128 . June 1991 . 1652446 . 10.1016/0922-4106(91)90086-w .
  8. Peñas-Cazorla R, Vilaró MT . Serotonin 5-HT4 receptors and forebrain cholinergic system: receptor expression in identified cell populations . Brain Structure & Function . 220 . 6 . 3413–3434 . November 2015 . 25183542 . 10.1007/s00429-014-0864-z . free . 14116338 . 10261/124736 .
  9. Yamaguchi T, Suzuki M, Yamamoto M . 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 . 712–720 . December 1997 . 9453456 . 10.1007/pl00005110 . 2010-01-11 . dead . 7800009 . https://web.archive.org/web/19991008020023/http://link.springer.de/link/service/journals/00210/bibs/7356006/73560712.htm . 1999-10-08 .
  10. Yamamoto M, Takahashi K, Ohyama M, Sasamata M, Yatsugi S, Okada M, Endoh H . 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 . 603–613 . May 1994 . 8078992 . 10.1016/0278-5846(94)90016-7 . 11703415 .
  11. Ogawa N, Haba K, Sora YH, Higashida A, Sato H, Ogawa S . Comparison of the effects of bifemelane hydrochloride and indeloxazine hydrochloride on scopolamine hydrobromide-induced impairment in radial maze performance . Clinical Therapeutics . 10 . 6 . 704–711 . 1988 . 3219685 .
  12. Yamamoto M, Shimizu M . Cerebral activating properties of indeloxazine hydrochloride . Neuropharmacology . 26 . 7A . 761–770 . July 1987 . 3627384 . 10.1016/0028-3908(87)90239-5 . 46153252 .
  13. Ogawa N, Haba K, Yoshikawa H, Ono T, Mizukawa K . 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 . 285–288 . August 1988 . 3187197 .
  14. Yamamoto M, Shimizu M, Sakamoto N, Ohtomo H, Kogure K . Protective effects of indeloxazine hydrochloride on cerebral ischemia in animals . Archives Internationales de Pharmacodynamie et de Therapie . 290 . 1 . 16–24 . November 1987 . 3446040 .
  15. Shimizu-Sasamata M, Terai M, Harada M, Yamamoto M . 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 Therapie . 324 . 33–46 . 1993 . 8297184 .
  16. Yamamoto M, Shimizu M . Effects of indeloxazine hydrochloride (YM-08054) on anoxia . Archives Internationales de Pharmacodynamie et de Therapie . 286 . 2 . 272–281 . April 1987 . 3592867 .
  17. Nakamura J, Anraku T, Shirouzu M, Iwashita Y, Nakazawa Y . 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 . 445–450 . June 1993 . 8327550 . 10.1016/0091-3057(93)90263-s . 26761718 .

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