Anatabine is an alkaloid similar to Nicotine that is found in the same sources, and is currently being investigated for its antiinflammatory properties. It appears to work via inhibiting the STAT3 protein which then inhibits nF-kB activation (a mechanism of action similar to Boswellia serrata and Feverfew, among other antiinflammatory agents) and preliminary evidence in animals suggests that these benefits may be useful for autoimmune diseases and Alzheimer's disease.
Unfortunately, currently the dosages being used are much higher than the doses currently on the supplement market. While dietary supplements of anatabine tend to be dosed at 1mg per serving, the lowest effective dose in mice was a 2mg/kg injection (0.16mg/kg in humans, or 11mg for a 150lb person) while oral studies have used a dosage that is equivalent to 1-1.6mg/kg in humans (for our 150lb person, this would be a dosage range of 68-110mg). While this is a dosage that is significantly lower than other supplements (which usually have an active dose in the 300-500mg range), it is still much lower than is currently available, and the one human study failed to find any anti-inflammatory effects even at a dose that was 6-12 times higher than the currently sold doses.
Due to the limitations in the market at the moment, anatabine may not be a practical antiinflammatory to use.
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Anatabloc (Brand Name)
Animal research on anatabine have used oral intakes of 12.5-20mg/kg in mice for the purpose of reducing autoimmune diseases, which suggests a human preliminary dosage of:
The Human Effect Matrix looks at human studies (excluding animal/petri-dish studies) to tell you what effect Anatabine has in your body, and how strong these effects are.
|Grade||Level of Evidence|
|A||Robust research conducted with repeated double blind clinical trials|
|B||Multiple studies where at least two are double-blind and placebo controlled|
|C||Single double blind study or multiple cohort studies|
|D||Uncontrolled or observational studies only|
|Level of Evidence ||Effect||Change||Magnitude of Effect Size ||Scientific Consensus||Comments|
The progression of recovery after a novel workout (when measured over three days) was unaffected by 6-12mg anatabine
Strength recovery over the course of three days recovery was not significantly improved by 6-12mg anatabine
Perceived muscle soreness and pain from a workout was unaffected by anatabine supplementation.
6-12mg anatabine does not appear to significantly influence blood pressure in otherwise healthy persons.
There is no significant influence on heart rate seen with 6-12mg anatabine in otherwise healthy persons
Anatabine is an alkaloid found in tobacco and the solanaceae family of plants. This alkaloid is structurally similar to Nicotine, and is an analogue of both nornicotine and anabasine (other alkaloids in the same plant family).
It is found in:
Anatabine is a tobacco alkaloid similar to nicotine, and is found in the same plants
Anatabine is an alkaloid with structural similarity to Nicotine, and closer structure similarity to anabasine (which is anatabine without the double bond in the right ring pictured below).
May interact with nicotinic cholinergic receptors, although this is not well researched
Anatabine has been found to reduce Aβ production (both Aβ1–40 and Aβ1–42) with an IC50 of around 640µg/mL, and it appeared to mostly inhibit β-cleavage of APP. As this is known to occur with nF-kB inhibition anatabine was then tested on the protein and it was found to inhibit nF-kB activation from TNF-α with a similar IC50 value and nicotine was found to be inactive at the same concentrations tested. It has been noted elsewhere that this inhibitory effect on nF-kB is secondary to inhibiting STAT3 phosphorylation at 600-800µg/mL although concnetrations as low as 10µg/mL can inhibit LPS-induced nF-kB activity and 400µg/mL can fully abolish IL-1β secretion induced by LPS.
Nicotine has been found to inhibit Aβ production by regulating BACE-1 transcription in cells that express its receptor (α4β2 nicotinic acetylcholine receptor) and anatabine has also been found to downregulate BACE-1 mRNA, which was credited to nF-kB inhibition (known to regulate BACE-1). Activation of the nicotinic receptors can inhibit nF-kB via STAT3 but nicotine seems to require a cholinergic receptor whereas anatabine does not.
When injected into mice at 0.5-2mg/kg, only the higher dose was able to reduce brain and plasma Aβ concentrations to near control levels (in plasma) and by about 25% (brain) and this dose has been noted to exert anti-inflammatory effects by reducing C-reactive protein as well as IL-1β, IL-6, and TNF-α.
Anatabine is a STAT3 inhibitor, which then inhibits nF-kB and exerts an anti-inflammatory effect. This appears to be active following injections of anatabine and may be of therapeutic benefit to Alzheimer's Disease
Anatabine has structural similarity to Nicotine, and since nicotine is able to acutely increase heart rate and blood pressure anatabine has been investigated for its ability to do the same; it has since failed to significantly influence blood pressure or heart rate.
Currently no significant interactions between anatabine and cardiovascular function are known
Incubation of macrophages with 250-350μM was able to inhibit an IFN-γ and LPS induced increases in iNOS and COX-2 mRNA levels, suggesting antiinflammatory effects.
May have general antiinflammatory properties at moderately high concentrations
Despite the large amount of adverse health effects associated with tobacco smoking, both ulcerative colitis and autoimmune (Hashimoto's) thyroiditis have noted benefits associated with smoking. This is currently thought to be due to the antiinflammatory properties of nicotine via the α7 nicotinic receptor (inhibits STAT3 and then nF-kB), but anatabine is also being tested.
In mice inflicted with experimental autoimmune thyroiditis and concurrently supplemented orally with approximately 12.5mg/kg anatabine, occurrence of thyroiditis and the antibody response were significantly reduced. Autoimmune encephalomyelitis (research model for Multiple sclerosis) also sees clinical benefit in response to 20mg/kg anatabine in mice, although antibodies were not affected in this study.
Appears to be beneficial for rodents with autoimmune diseases in high oral doses
Supplementation of 6-12mg anatabine (via lozenges that also conferred 834-1668IU vitamin A and 66-132IU Vitamin D) for ten days prior to physical exercise testing in otherwise healthy young men failed to outperform placebo (which contained the vitamins) in reducing muscle soreness or power output when measured over the next three days.
The lone study in humans assessing the antiinflammatory properties of anatabine failed to find any significant influence of supplementation
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