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Bifemelane

Antidepressant and cerebral activator drug

Antidepressant and cerebral activator drug

| Drugs.com =

Bifemelane (INN), sold under the brand names Alnert and Celeport, is an antidepressant and cerebral activator that was widely used in the treatment of cerebral infarction patients with depressive symptoms in Japan, and in the treatment of dementia as well. It also appears to be useful in the treatment of glaucoma. It has been discontinued in Japan since 1998, when it was removed from the market reportedly for lack of effectiveness.

Bifemelane acts as a monoamine oxidase inhibitor (MAOI) of both isoenzymes, with competitive reversible inhibition of MAO-A (Ki = 4.20 μM), making it a reversible inhibitor of monoamine oxidase A (RIMA) and non-competitive irreversible inhibition of MAO-B (Ki = 46.0 μM), and also acts (weakly) as a norepinephrine reuptake inhibitor (NRI). The drug has nootropic, neuroprotective, and antidepressant-like effects in animal models, and appears to enhance the cholinergic system in the brain.

References

References

  1. (1995). "Effects of bifemelane hydrochloride on plasma neuropeptide Y, 3-methoxy-4-hydroxyphenylethylene glycol and 5-hydroxy-indole acetic acid concentrations in patients with cerebral infarction". Drugs Under Experimental and Clinical Research.
  2. (1996). "Dictionary of Pharmacological Agents". Chapman & Hall/CRC.
  3. (1996). "Use of bifemelane hydrochloride in improving and maintaining the visual field of patients with glaucoma". Clinical Therapeutics.
  4. (August 1998). "Drug approval in Japan questioned". Lancet.
  5. (January 1988). "4-(O-benzylphenoxy)-N-methylbutylamine (bifemelane) and other 4-(O-benzylphenoxy)-N-methylalkylamines as new inhibitors of type A and B monoamine oxidase". Journal of Neurochemistry.
  6. (4 March 2011). "Drug Actions and Interactions". McGraw Hill Professional.
  7. (1994). "Amine Oxidases: Function and Dysfunction". Journal of Neural Transmission. Supplementum.
  8. (March 1996). "Preventive effects of bifemelane hydrochloride on decreased levels of muscarinic acetylcholine receptor and its mRNA in a rat model of chronic cerebral hypoperfusion". Neuroscience Research.
  9. (September 1996). "Effects of bifemelane on muscarinic receptors and choline acetyltransferase in the brains of aged rats following chronic cerebral hypoperfusion induced by permanent occlusion of bilateral carotid arteries". Japanese Journal of Pharmacology.
  10. (June 1993). "Potential antidepressive properties of amantadine, memantine and bifemelane". Pharmacology & Toxicology.
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secondary-amines antidepressants monoamine-oxidase-inhibitors nootropics norepinephrine-reuptake-inhibitors phenol-ethers reversible-inhibitors-of-mao-a benzhydryl-compounds cerebral-activators
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