Hordenine

Hordeum vulgare (barley) — primary source
Evidence Level
Preliminary
3 Clinical Trials
5 Documented Benefits
1/5 Evidence Score

Hordenine is a compound found in barley, certain cacti, and bitter orange, used in pre-workout and fat-burner supplements for a mild stimulant and focus effect. It is marketed for energy, alertness, and appetite control, often combined with PEA and caffeine, on the basis of its mild stimulant and norepinephrine-related activity, though hordenine on its own has never been tested in a human trial for energy, focus, appetite or weight. The route matters more than the dose here: horses given hordenine by mouth at 2 mg/kg showed no change in heart rate, breathing or behaviour, while the same dose injected caused sweating, doubled heart rate and respiratory distress. Doses on supplement labels are often around 30 to 75 mg within stimulant blends, but no human dose has been established. As a stimulant-like compound, hordenine may raise heart rate and blood pressure and could interact with MAO inhibitors and other stimulants, so those with heart conditions or on related medication should avoid it.

Studied Dose No human dose established; labels commonly list 25 to 100 mg per serving, but these are marketing amounts, not amounts shown to do anything in a human trial of hordenine on its own.
Active Compound Hordenine (N,N-dimethyltyramine), a phenethylamine alkaloid related to tyramine.

Benefits

Stimulant/sympathomimetic effects (animal evidence)

Animal studies in dogs and rats showed hordenine produced a positive inotropic effect on the heart, increased systolic and diastolic BP, and increased peripheral blood flow, via indirect adrenergic activity (norepinephrine release). Critical caveat: these effects were short-lived and needed high doses. In the one study that compared routes, horses given 2 mg/kg by mouth showed no change at all, while the same dose injected into a vein caused sweating, doubled heart rate and respiratory distress. Human translation has not been demonstrated.

Weak MAO-B inhibitor (potentiates other PEAs)

Hordenine is a selective substrate for MAO-B with weak inhibitory activity. Theoretical mechanism for potentiating phenylethylamine (PEA) and other monoamines that are MAO-B substrates; combined with PEA in some pre-workouts to extend duration. Not a clinically meaningful MAOI like prescription drugs (selegiline, etc.) — far weaker effect.

No direct lipolytic activity (Haj Ahmed and Carpene 2021)

A laboratory study tested hordenine directly on mouse fat cells and on human abdominal fat tissue and found it does not activate or inhibit lipolysis. Adipocytes were responsive to standard stimulants (isoprenaline, forskolin) and inhibitors (insulin) but unresponsive to hordenine. The conclusion was that hordenine is unlikely to increase lipid mobilization from fat depots. Direct evidence against fat-burner marketing claims.

Indirect adrenergic activity (norepinephrine release)

Hordenine acts as indirect adrenergic agonist by promoting norepinephrine release from sympathetic nerve terminals. Mechanism similar to (but weaker than) tyramine and amphetamines. The picture is not clean: in isolated rat vas deferens hordenine caused no contraction, and those authors concluded it was blocking noradrenaline reuptake rather than releasing it. Any contribution to focus and energy through sympathetic activation is theoretical, and no human trial has measured it.

No established respiratory use

Supplement marketing often repeats that hordenine was used in Traditional Chinese Medicine as 'mao gen' for asthma. That identification does not hold up. The barley material in Chinese medicine is mai ya, germinated barley, and its traditional uses are digestive and for reducing milk supply, not respiratory. Mao gen, or bai mao gen, is a different plant altogether, Imperata rhizome, traditionally used to cool blood and promote urination. Any bronchodilator effect would simply be part of the general sympathomimetic response, and it has not been measured in people. Hordenine is not a treatment for asthma or any other breathing condition, and anyone with asthma should rely on the medicines their doctor prescribes.

Mechanism of action

1

Indirect adrenergic activity via norepinephrine release

Hordenine, like tyramine and amphetamines, is an indirect-acting sympathomimetic — it promotes release of stored norepinephrine from sympathetic nerve terminals. The mechanism is not fully settled: release from stores is what Hapke observed in intact rats and dogs, but in isolated rat vas deferens hordenine caused no contraction at all, and those authors read it as blocking noradrenaline reuptake rather than releasing it. Neither mechanism appears to involve direct receptor binding (unlike epinephrine). Effects depend on existing sympathetic tone and norepinephrine stores. Tachyphylaxis can develop with repeated use.

2

Selective MAO-B inhibition (weak)

Selectively inhibits MAO-B isoenzyme over MAO-A. In context of PEA potentiation: PEA is rapidly metabolized by MAO-B; hordenine slows this metabolism. However, hordenine itself is also an MAO-B substrate at low concentrations — making it a 'mixed substrate/inhibitor.' Inhibitory activity is weak relative to selective MAOI drugs.

3

Crosses blood-brain barrier

This has now been tested rather than assumed. In a laboratory model using pig brain capillary cells, hordenine crossed the barrier quickly. Getting there is the problem: the same study found hordenine is pumped from the bloodstream back into the gut and broken down inside intestinal cells, and its authors concluded that a route other than swallowing would be needed to make use of that brain access. In four volunteers who drank beer, oral hordenine reached free plasma levels of only about 12 to 17 nanomolar, which those authors judged too low to interact directly with the dopamine D2 receptor. CNS effects in humans have not been rigorously characterized via PET imaging or microdialysis studies.

4

No direct beta-adrenergic agonism in adipocytes

Despite weight loss marketing, hordenine does not bind β-adrenergic receptors directly in adipocytes and cannot stimulate lipolysis directly. Any weight management effect would have to come from indirect sympathetic activation, and no human weight or body composition trial has ever measured that for hordenine.

Clinical trials

1
Hordenine Pharmacology in Horses

Veterinary pharmacology study (Frank M, Weckman TJ, Wood T, Woods WE, Tai CL, Chang SL, Ewing A, Blake JW, Tobin T, Equine Vet J 1990;22(6):437-41, doi:10.1111/j.2042-3306.1990.tb04312.x, PMID 2269269).

Horses given oral and intravenous hordenine. Pharmacokinetics (plasma concentration), behavioral effects, vital signs, and respiratory effects measured.

Intravenous administration caused immediate behavioral changes and significant respiratory distress, but symptoms subsided within 30 minutes. Oral administration produced no change in heart rate, respiratory rate, body temperature or behaviour at the same 2.0 mg/kg dose, consistent with poor oral bioavailability. Oral is the only route a supplement uses, so this is the half of the study that matters most to a supplement user. Pharmacokinetic analysis revealed rapid plasma clearance, with no lasting stimulant or depressive effects post-dosing. Foundational evidence that oral hordenine produces minimal systemic effects.

2
Hordenine Pharmacology in Dogs and Rats

Animal pharmacology study (Hapke HJ, Strathmann W, Dtsch Tierarztl Wochenschr 1995;102(6):228-32, PMID 8582256). This is a veterinary pharmacology paper in animals, not a human clinical trial.

Dogs and rats given hordenine orally and intravenously. Cardiovascular, gastrointestinal, and CNS effects assessed; isolated tissue experiments to elucidate mechanism.

Hordenine produced positive inotropic effect, increased BP, increased peripheral blood flow, inhibited GI movements. Effects characterized as indirectly acting adrenergic mechanism via norepinephrine release. Critical caveat: effects were short-lived and required high doses to be observed. The same paper also reports two findings the summary left out: hordenine had no effect on the psychomotor behaviour of mice, and in isolated organs and tissues with reduced adrenaline content the effect was very poor. The authors concluded that a measurable increase in the performance of racing horses is quite improbable from the amounts present in feed. Animal findings do not translate directly to human supplement doses.

3
Hordenine Is Not a Lipolysis Activator (Laboratory Study)

Laboratory study (Haj Ahmed W, Carpene C 2021. Hordenine does not directly activate triglyceride breakdown in adipocytes but is a MAO interacting agent. Integr Food Nutr Metab 8:1-7, doi:10.15761/IFNM.1000302). This journal is not indexed in PubMed or MEDLINE, so the paper carries no PMID and has not been through that filter.

Mouse fat cells (adipocytes) and human subcutaneous adipose tissue homogenates exposed to hordenine and assessed for lipolytic and antilipolytic responses, plus interaction with monoamine oxidase.

Direct evidence that hordenine does not activate or inhibit lipolysis in adipocytes. Cells were responsive to standard agents (isoprenaline, forskolin, insulin) but unresponsive to hordenine. Confirmed weak MAO interaction (substrate/inhibitor) but no direct fat-cell stimulation. Authors concluded: 'Hordenine consumption cannot likely increase lipid mobilization from fat depots.' Foundational counter-evidence against fat burner marketing claims.

Side effects and drug interactions

Common Potential side effects

Hypertension at high doses or in those with cardiovascular conditions.
Tachycardia, palpitations.
Anxiety, jitteriness, insomnia (typical stimulant effects).
Drug test interference: hordenine cross-reacts with ELISA and radioimmunoassay screens for opiates, with morphine assays the most sensitive, and it also interferes with thin layer chromatography for oxymorphone, hydromorphone and apomorphine. A confirmation test by GC-MS or HPLC can tell hordenine apart from opiates, but the initial screen can still come back positive. This is an important practical concern.
Pregnancy/lactation: avoid — insufficient safety data, sympathomimetic activity.
Hypertension/heart disease: avoid.
FDA treats hordenine as a new dietary ingredient with no notification on file, so it considers products containing it adulterated, and it has issued warning letters to companies selling it. Hordenine is also on the NCAA banned substance list and on the US Department of Defense prohibited dietary supplement ingredients list, so college athletes and service members should avoid it outright.

Important Drug interactions

MAOIs (selegiline, phenelzine): significant interaction risk, with hypertensive crisis potential. Hordenine is itself cleared mainly by MAO-B, so an MAO inhibitor would raise and prolong exposure to a sympathomimetic compound. Do not combine.
Stimulants (caffeine, ephedrine, ADHD medications): additive sympathomimetic effects, cardiovascular risk.
Antihypertensives: theoretical opposition to BP-lowering effects.
Tyramine-containing foods: theoretical additive effects (clinically usually mild).
Sympathomimetic decongestants (pseudoephedrine): additive effects.
Drug screening: causes immunoassay false positives for opiates.

Frequently asked questions about Hordenine

What is hordenine?

Hordenine is a compound found in barley, certain cacti, and bitter orange, used in pre-workout and fat-burner supplements for a mild stimulant and focus effect. It is structurally related to other stimulants.

What is hordenine used for?

It is marketed for energy, focus, and appetite control, often combined with PEA and caffeine in pre-workouts. Those claims rest on animal and test-tube work. Hordenine on its own has never been tested in a human trial for any of these uses, it has only been studied inside multi-ingredient blends that also contain caffeine, and when hordenine was given by mouth to horses it produced no measurable effect.

How much hordenine is used?

Labels often list around 30 to 75 mg, usually within stimulant blends, but no human dose has been established and no trial has tested hordenine on its own at any dose for energy or fat loss. Avoid stacking many stimulants.

Is hordenine safe?

Human data is limited. As a stimulant-like compound, it may raise heart rate and blood pressure and could interact with MAO inhibitors and other stimulants, so those with heart conditions or on related medication should avoid it and speak with a doctor. It is also worth knowing that the FDA considers hordenine-containing supplements adulterated, that hordenine is banned by the NCAA and prohibited for US service members, and that it can trigger a positive result on an initial opiate screening test.

What is the recommended dosage of Hordenine?

The clinically studied dose is No human dose established; labels commonly list 25 to 100 mg per serving, but these are marketing amounts, not amounts shown to do anything in a human trial of hordenine on its own. Always follow the product label and check with a healthcare provider for personal advice.

Is Hordenine safe, and does it have side effects?

For most healthy adults, Hordenine is well tolerated at studied doses. Reported effects can include: Hypertension at high doses or in those with cardiovascular conditions. Tachycardia, palpitations. It may also interact with some medications. Hordenine is not right for everyone, so check with a healthcare provider first if you are pregnant or breastfeeding, have a medical condition, or take prescription medication.

Does Hordenine interact with any medications?

Possible interactions include: MAOIs (selegiline, phenelzine): significant interaction risk, with hypertensive crisis potential. Hordenine is itself cleared mainly by MAO-B, so an MAO inhibitor would raise and prolong exposure to a sympathomimetic compound. Do not combine. If you take prescription medication, check with a pharmacist or doctor before using it.

How strong is the scientific evidence for Hordenine?

NutraSmarts rates the evidence for Hordenine as Preliminary (1 out of 5). It is backed by 3 clinical trials and 7 cited references summarized on this page. A higher rating reflects more, larger, and better-designed human studies.

References(7 citations)

Evidence ratings on NutraSmarts are based on the totality of human clinical research, with emphasis on randomized controlled trials, meta-analyses, and systematic reviews. The references below directly support claims made throughout this page.

  1. Barwell CJ, Basma AN, Lafi MA, Leake LD Deamination of hordenine by monoamine oxidase and its action on vasa deferentia of the rat The Journal of Pharmacy and Pharmacology. 1989;41(6):421-3. doi:10.1111/j.2042-7158.1989.tb06492.x.PubMedUsed to support: In vitro and isolated tissue study demonstrating that hordenine is a highly selective substrate for MAO-B and is not deaminated by the MAO-A of intestinal epithelium, and acts on rat vas deferens as an inhibitor of noradrenaline uptake. The paper reports close to the opposite of a releasing effect: unlike tyramine, hordenine did not itself contract the vas deferens, though it potentiated responses to added noradrenaline and inhibited responses to tyramine. Mechanistic basis for 'Weak MAO-B inhibitor (potentiates other PEAs)' and 'Indirect adrenergic activity (norepinephrine release)' benefits. Data are preclinical (in vitro/animal); no human data.
  2. Frank M, Weckman TJ, Wood T, Woods WE, Tai CL, Chang SL, Ewing A, Blake JW, Tobin T Hordenine: pharmacology, pharmacokinetics and behavioural effects in the horse Equine Veterinary Journal. 1990;22(6):437-41. doi:10.1111/j.2042-3306.1990.tb04312.x.PubMedUsed to support: Pharmacokinetics and behavioral pharmacology study of hordenine in horses; Intravenous hordenine at 2.0 mg/kg in 10 horses raised respiratory rates about 250 percent and roughly doubled heart rates, with sweating and a flehmen response, all resolving within 30 minutes. The same 2.0 mg/kg dose given by mouth produced no change in heart rate, respiratory rate, body temperature or behaviour. Read honestly, this paper is evidence that oral hordenine is inactive rather than evidence that it is a stimulant. Cited for 'Stimulant/sympathomimetic effects' and 'Indirect adrenergic activity' benefit claims. Data are equine only. Human pharmacokinetics have since been measured after beer consumption (Sommer 2020), but no human trial has tested hordenine on its own for energy, focus or weight.
  3. Hapke HJ, Strathmann W [Pharmacological effects of hordenine]. Dtsch Tierarztl Wochenschr. 1995;102(6):228-32..PubMedUsed to support: Veterinary pharmacology study in rats, dogs and mice. Hordenine acted as an indirectly acting adrenergic drug that liberates norepinephrine from stores, producing a positive inotropic effect on the heart, higher systolic and diastolic blood pressure and peripheral blood flow, and inhibited gut movements, but it had no effect on the psychomotor behaviour of mice, and in isolated organs and structures with reduced adrenaline content the effect was very poor. All effects were short and only possible after high doses, and the authors concluded that a measurable increase in the performance of racing horses is quite improbable. This is the study summarised in the trial card on hordenine pharmacology in dogs and rats. Animal data only; no human evidence.
  4. Singh AK, Granley K, Misrha U, et al. Screening and confirmation of drugs in urine: interference of hordenine with the immunoassays and thin layer chromatography methods. Forensic Sci Int. 1992;54(1):9-22..PubMedUsed to support: Forensic laboratory study of urine drug screening. Hordenine cross-reacted with several ELISA and radioimmunoassay kits used to screen urine, with the morphine ELISA kit the most sensitive to the cross-reactivity and the etorphine and buprenorphine kits the least sensitive, and hordenine also interfered with thin layer chromatography of oxymorphone, hydromorphone and apomorphine. Gas chromatography with mass spectrometry and high performance liquid chromatography could distinguish hordenine from opiates. Source for the drug test interference warning in the side effects and drug interactions.
  5. Sommer T, Göen T, Budnik N, et al. Absorption, Biokinetics, and Metabolism of the Dopamine D2 Receptor Agonist Hordenine (N,N-Dimethyltyramine) after Beer Consumption in Humans. J Agric Food Chem. 2020;68(7):1998-2006..PubMedUsed to support: Human pharmacokinetic study, the only oral human data on hordenine. Four volunteers consumed beer supplying about 0.075 mg hordenine per kg bodyweight. Maximum free plasma concentrations were 12.0 to 17.3 nM within 0 to 60 minutes, the elimination half-life of free hordenine was 52.7 to 66.4 minutes, phase II metabolism proceeded by sulfation and then glucuronidation, and 9.9 percent of the ingested dose was recovered in urine within 24 hours. The authors concluded that these plasma levels seem too low to provoke direct interaction with the dopamine D2 receptor. Supports the blood brain barrier and absorption text, and corrects the earlier statement that human pharmacokinetics were not established. Measures absorption, not any health effect.
  6. Hahn M, Lindemann V, Behrens M, et al. Permeability of dopamine D2 receptor agonist hordenine across the intestinal and blood-brain barrier in vitro. PLoS One. 2022;17(6):e0269486..PubMedUsed to support: Laboratory permeability study. Hordenine transferred quickly through a Caco-2 intestinal cell monolayer, but the authors report efflux transport of hordenine from the bloodstream back into the intestinal lumen and first pass metabolism inside intestinal epithelial cells, both of which limit oral bioavailability, and in a primary porcine brain capillary endothelial cell model hordenine rapidly penetrated the blood brain barrier. The authors concluded that a dopamine D2 receptor interaction would depend on circumventing the intestinal barrier with a route of administration other than oral intake. This is the evidence behind the blood brain barrier mechanism and supplies the oral-route caveat that mechanism was missing. In vitro only.
  7. Kaczka P, Batra A, Kubicka K, et al. Effects of Pre-Workout Multi-Ingredient Supplement on Anaerobic Performance: Randomized Double-Blind Crossover Study. Int J Environ Res Public Health. 2020;17(21)..PubMedUsed to support: Randomized double-blind crossover trial in 23 resistance-trained men of a multi-ingredient pre-workout supplement containing 150 mg barley-derived hordenine extract together with 300 mg anhydrous caffeine, 200 mg guarana extract, 3 g citrulline, 2 g beta-alanine and other ingredients. The supplement improved bench press strength and Wingate mean power against placebo. This is the only human trial in which hordenine has been administered for a performance outcome, and nothing in it can be attributed to hordenine, because the formula also delivered a large caffeine dose. Cited only to support the statement that hordenine has been studied in humans solely inside caffeinated blends, never on its own.