Bifemelane (

INN Inns are generally establishments or buildings where travelers can seek lodging, and usually, food and drink. Inns are typically located in the country or along a highway; before the advent of motorized transportation they also provided accommo ...

) (Alnert, Celeport), or bifemelane hydrochloride (

JAN Jan, JaN or JAN may refer to: Acronyms * Jackson, Mississippi (Amtrak station), US, Amtrak station code JAN * Jackson-Evers International Airport, Mississippi, US, IATA code * Jabhat al-Nusra (JaN), a Syrian militant group * Japanese Article Num ...

), also known as 4-(''O''-benzylphenoxy)-''N''-methylbutylamine, is an antidepressant and

cerebral activator A cerebral activator, or cerebral metabolic enhancer, is a type of drug that "activates" the central nervous system in the context of cerebrovascular diseases such as stroke and dementia. The term has been used specifically to describe a few Japa ...

that is widely used in the treatment of

cerebral infarction A cerebral infarction is the pathologic process that results in an area of necrotic tissue in the brain (cerebral infarct). It is caused by disrupted blood supply ( ischemia) and restricted oxygen supply ( hypoxia), most commonly due to thromboemb ...

patients with depressive symptoms in Japan, and in the treatment of

senile dementia Dementia is a disorder which manifests as a set of related symptoms, which usually surfaces when the brain is damaged by injury or disease. The symptoms involve progressive impairments in memory, thinking, and behavior, which negatively affe ...

as well. It also appears to be useful in the treatment of

glaucoma Glaucoma is a group of eye diseases that result in damage to the optic nerve (or retina) and cause vision loss. The most common type is open-angle (wide angle, chronic simple) glaucoma, in which the drainage angle for fluid within the eye rem ...

. Bifemelane acts as a monoamine oxidase inhibitor (MAOI) of both

isoenzyme In biochemistry, isozymes (also known as isoenzymes or more generally as multiple forms of enzymes) are enzymes that differ in amino acid sequence but catalyze the same chemical reaction. Isozymes usually have different kinetic parameters (e.g. dif ...

s, with competitive (reversible) inhibition of

MAO-A Monoamine oxidase A, also known as MAO-A, is an enzyme that in humans is encoded by the ''MAOA'' gene. This gene is one of two neighboring gene family members that encode mitochondrial enzymes which catalyze the oxidative deamination of amines, s ...

(K_i = 4.20 ''μ''M) (making it a

reversible inhibitor of monoamine oxidase A Monoamine oxidase inhibitors (MAOIs) are a class of drugs that inhibit the activity of one or both monoamine oxidase enzymes: monoamine oxidase A (MAO-A) and monoamine oxidase B (MAO-B). They are best known as effective antidepressants, espe ...

(RIMA)) and non-competitive (irreversible) inhibition of

MAO-B Monoamine oxidase B, also known as MAOB, is an enzyme that in humans is encoded by the ''MAOB'' gene. The protein encoded by this gene belongs to the flavin monoamine oxidase family. It is an enzyme located in the outer mitochondrial membrane. I ...

(K_i = 46.0 ''μ''M), and also acts (weakly) as a

norepinephrine reuptake inhibitor A norepinephrine reuptake inhibitor (NRI, NERI) or noradrenaline reuptake inhibitor or adrenergic reuptake inhibitor (ARI), is a type of drug that acts as a reuptake inhibitor for the neurotransmitters norepinephrine (noradrenaline) and epin ...

. The drug has

nootropic Nootropics ( , or ) (colloquial: smart drugs and cognitive enhancers, similar to adaptogens) are a wide range of natural or synthetic dietary supplement, supplements or drugs and other substances that are claimed to improve cognitive function ...

neuroprotective Neuroprotection refers to the relative preservation of neuronal structure and/or function. In the case of an ongoing insult (a neurodegenerative insult) the relative preservation of neuronal integrity implies a reduction in the rate of neuronal los ...

, and antidepressant-like effects in

animal model An animal model (short for animal disease model) is a living, non-human, often genetic-engineered animal used during the research and investigation of human disease, for the purpose of better understanding the disease process without the risk of ha ...

s, and appears to enhance the

cholinergic Cholinergic agents are compounds which mimic the action of acetylcholine and/or butyrylcholine. In general, the word " choline" describes the various quaternary ammonium salts containing the ''N'',''N'',''N''-trimethylethanolammonium cati ...

system in the

brain A brain is an organ that serves as the center of the nervous system in all vertebrate and most invertebrate animals. It is located in the head, usually close to the sensory organs for senses such as vision. It is the most complex organ in a ve ...

References

Amines Antidepressants Monoamine oxidase inhibitors Nootropics Norepinephrine reuptake inhibitors Phenol ethers Reversible inhibitors of MAO-A Benzhydryl compounds {{nervous-system-drug-stub

See also

References