Monoamine oxidase: nootropics and compounds | sci-wiki

Rhodiola Rosea

Rhodiola rosea, commonly called golden root or roseroot, is a perennial flowering plant of the family Crassulaceae that grows in cold, high-altitude and Arctic regions. Its root has a long history of use in the traditional medicine of northern Europe and Asia, and it is popularly classed as an adaptogen, an herb said to help the body resist stress and fatigue. Its most characteristic studied constituents are the phenolic compounds rosavin and salidroside, though high-quality clinical evidence for its benefits is limited.

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MAOI

Banisteriopsis caapi

Banisteriopsis caapi is a South American vine that is the backbone of the traditional ayahuasca brew. Its psychoactivity comes from harmala alkaloids, which are reversible monoamine oxidase inhibitors (MAOIs); in ayahuasca they let orally-taken DMT reach the brain by blocking the enzyme that would otherwise destroy it. On its own the vine is mildly psychoactive and purgative, but its MAOI activity is the pharmacologically important and risky part.

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Deliriant

Nutmeg

Nutmeg is the culinary spice obtained from the seed of Myristica fragrans, the same tree whose seed covering yields mace. Culinary quantities are inert, but very large ingestions of the ground seed can cause a slow-onset, long-lasting intoxication attributed chiefly to the aromatic constituents myristicin, elemicin, and safrole, often accompanied by anticholinergic-like features such as tachycardia and agitation. Myristicin is additionally reported to possess weak monoamine oxidase inhibitory activity, and its structural resemblance to amphetamine precursors has prompted speculation about amphetamine- or MDMA-like metabolites, though such conversion in humans remains unproven. Case series and poisoning reports characterize the experience as unpredictable and generally unpleasant; documented exposures have required medical evaluation but have not typically been life-threatening, and toxicokinetic analysis of the psychoactive constituents in serum has been performed in overdose cases.

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MAOI

Phenelzine

Phenelzine, sold as Nardil, is a classic irreversible, non-selective monoamine oxidase inhibitor (MAOI), an older but powerful antidepressant. What sets it apart from other MAOIs is a second action: it also inhibits GABA-transaminase, the enzyme that breaks down GABA, so it raises brain GABA levels, and it metabolizes to phenylethylidenehydrazine (PEH), the compound thought to drive much of that GABA effect. That extra, calming mechanism is a big part of why phenelzine is unusually effective for anxiety as well as depression; it also raises phenylethylamine (PEA), a natural trace amine.

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Anxiolytic

Phenylethylidenehydrazine

Phenylethylidenehydrazine (PEH) is a metabolite of the antidepressant phenelzine and a research compound in its own right. Its main action is inhibition of GABA-transaminase (GABA-T), the enzyme that breaks down GABA, so it raises brain GABA levels; this GABA-boosting effect is thought to account for much of phenelzine's distinctive anti-anxiety character. It also influences phenylethylamine (PEA) metabolism. PEH is not a medicine you can be prescribed; it is studied mainly to tease apart which of phenelzine's effects come from raising GABA versus inhibiting monoamine oxidase.

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Supplement

Piperine

Piperine is the principal pungent alkaloid of black pepper (Piper nigrum) and long pepper (Piper longum), responsible for the spice's biting taste through activation of the capsaicin receptor TRPV1; structural studies show it occupies the same ligand-binding pocket as capsaicin but adopts a distinct binding pose, acting as a comparatively weak agonist. Its most exploited pharmacological property is bioenhancement, since it inhibits hepatic and intestinal glucuronidation as well as cytochrome P450 3A4 and the efflux transporter P-glycoprotein, thereby slowing first-pass metabolism and raising systemic exposure of co-administered compounds; the classic demonstration reported a roughly 2000 percent increase in curcumin bioavailability in humans. Piperine also inhibits monoamine oxidase and has shown antidepressant-like, anticonvulsant, and neuroprotective activity in animal models, with anti-seizure effects mediated through TRPV1. It is widely marketed as a standardized extract for use alongside poorly absorbed nutraceuticals.

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