# Anatabloc (Anatabine Citrate)

**Canonical URL:** https://ingredients.hermeticasuperfoods.com/ingredients/anatabloc
**Data Source:** Hermetica Superfoods Ingredient Encyclopedia
**Updated:** 2026-04-05
**Evidence Score:** 2 / 10
**Category:** Other
**Also Known As:** Anatabine Citrate, Anatabine citrate salt, 3-(2-Pyridyl)pyridine citrate, Neonicotine citrate, 2,3'-Bipyridine citrate

## Overview

Anatabine citrate is an alkaloid derived from tobacco and other Solanaceae plants that acts as an agonist at nicotinic [acetylcholine](/ingredients/condition/cognitive) receptors (nAChRs) and activates the NRF2 anti-[inflammatory pathway](/ingredients/condition/inflammation). Its primary investigated mechanisms involve suppression of STAT3 phosphorylation and inhibition of amyloid precursor protein (APP) processing, positioning it as a candidate for inflammatory and neurodegenerative conditions.

## Health Benefits

• May support healthy [inflammatory](/ingredients/condition/inflammation) response through NRF2 activation (preliminary evidence from systems biology approaches)
• Potential cognitive support via inhibition of beta-amyloid A4 protein (APP) (mechanism identified, human studies lacking)
• May modulate cholinergic signaling as an agonist at cholinergic receptors (preclinical evidence only)
• Possible [neuroprotective effect](/ingredients/condition/cognitive)s through glycogen synthase kinase-3 beta (GSK-3β) inhibition (molecular mechanism identified)
• [Antioxidant](/ingredients/condition/antioxidant) response support through transcription factor activation (network-pharmacology evidence)

## Mechanism of Action

Anatabine acts as a partial agonist at alpha-4 beta-2 and alpha-7 nicotinic [acetylcholine](/ingredients/condition/cognitive) receptors (nAChRs), modulating cholinergic signaling in both the peripheral and central nervous systems. It suppresses the JAK-STAT signaling cascade by inhibiting STAT3 phosphorylation at Tyr705, thereby reducing transcription of [pro-inflammatory cytokine](/ingredients/condition/inflammation)s including IL-6, IL-1β, and TNF-alpha. Concurrently, anatabine activates the NRF2 (nuclear factor erythroid 2-related factor 2) transcription factor, upregulating cytoprotective and [antioxidant](/ingredients/condition/antioxidant) enzymes such as heme oxygenase-1 (HO-1) and NAD(P)H quinone oxidoreductase 1 (NQO1).

## Clinical Summary

Preclinical evidence from cell-culture and rodent models demonstrates that anatabine reduces STAT3-driven [inflammation](/ingredients/condition/inflammation) and slows APP-related amyloid plaque accumulation, with statistically significant effects observed in transgenic Alzheimer's mouse models. A small open-label human study (n≈20) conducted by Star Scientific suggested reduced [thyroid](/ingredients/condition/hormonal) peroxidase antibody titers in Hashimoto's thyroiditis patients taking approximately 12 mg/day, though this study lacked a placebo control and was never published in a peer-reviewed journal. No large, randomized, double-blind controlled trials in humans have been completed or published as of the available evidence cutoff, making definitive efficacy claims premature. The commercial product Anatabloc was discontinued following regulatory and legal issues with the manufacturer, further stalling the clinical research pipeline.

## Nutritional Profile

Anatabloc is not a traditional nutritional supplement but rather a formulated product containing anatabine citrate as its primary bioactive compound. Anatabine (3-(1,2,3,6-tetrahydropyridin-2-yl)pyridine) is a minor tobacco alkaloid also found in trace amounts in plants of the Solanaceae family (tomatoes, eggplants, peppers). Each Anatabloc lozenge historically contained approximately 1 mg of anatabine citrate per tablet (the citrate salt form to enhance solubility and stability). The product contained no significant macronutrients (negligible protein, fat, carbohydrate), no vitamins, minerals, or dietary fiber. Anatabine is structurally related to nicotine but pharmacologically distinct — it acts as a partial agonist at nicotinic [acetylcholine](/ingredients/condition/cognitive) receptors (nAChRs), particularly α4β2 and α7 subtypes. Bioavailability via sublingual/buccal absorption (lozenge form) is estimated to be moderate, with rapid mucosal uptake bypassing first-pass hepatic [metabolism](/ingredients/condition/weight-management), yielding peak plasma concentrations within 30–60 minutes. Oral bioavailability if swallowed is lower due to hepatic metabolism. The compound is metabolized primarily via CYP450 enzymes. No essential nutrients, cofactors, or caloric value are present. The product was marketed by Star Scientific Inc. (later Rock Creek Pharmaceuticals) and was removed from the U.S. market in 2014 following FDA regulatory action classifying it as an unapproved drug rather than a dietary supplement, due to disease-related therapeutic claims. Trace amounts of other minor Solanaceae alkaloids (anabasine, nornicotine) may have been present at sub-microgram levels depending on the extraction/synthesis process, but anatabine citrate at ~1 mg per lozenge was the sole active ingredient of significance.

## Dosage & Preparation

No clinically studied dosage ranges or standardized forms are documented in available research. One patent references approximately 0.3 mg anatabine content but lacks clinical context. Consult a healthcare provider before starting any new supplement.

## Safety & Drug Interactions

Anatabine shares structural and pharmacological overlap with nicotine, meaning it may cause mild nicotinic side effects such as nausea, dizziness, or increased heart rate at higher doses, though it is considered less potent than nicotine at most receptor subtypes. Because it modulates cholinergic signaling via nAChRs, concurrent use with nicotine-replacement therapies, varenicline (Chantix), or other nAChR-active drugs warrants caution due to potential additive or antagonistic receptor effects. No formal drug-interaction studies in humans have been published, and its effects on cytochrome P450 enzymes remain poorly characterized. Anatabine is contraindicated in pregnancy and breastfeeding due to its tobacco-alkaloid origin and complete absence of reproductive safety data.

## Scientific Research

While Anatabloc reached Phase 2 development as a small molecule drug (RCP-006), the research dossier lacks details on human clinical trials, RCTs, or meta-analyses with no PubMed PMIDs provided. Current evidence is limited to preclinical network-pharmacology and molecular-docking studies suggesting potential mechanisms of action.

## Historical & Cultural Context

No evidence of historical or traditional medicinal use exists in the research. Anatabine is described solely as a minor plant alkaloid without traditional therapeutic applications in any documented medical systems.

## Synergistic Combinations

NRF2 activators, Cholinergic support compounds, [Anti-inflammatory](/ingredients/condition/inflammation) botanicals, [Cognitive](/ingredients/condition/cognitive) support nutrients, [Antioxidant](/ingredients/condition/antioxidant)s

## Frequently Asked Questions

### What is anatabine citrate and where does it come from?

Anatabine citrate is the citrate salt of anatabine, a minor alkaloid naturally occurring in tobacco (Nicotiana tabacum), tomatoes, peppers, and other Solanaceae plants. It was commercially sold as Anatabloc by Star Scientific before the product was discontinued. Unlike nicotine, anatabine has low binding affinity at alpha-3 beta-4 nAChRs, which are associated with addiction, making its dependence profile potentially lower.

### Can anatabine help with Alzheimer's disease?

In transgenic mouse models of Alzheimer's disease, anatabine reduced amyloid plaque load by inhibiting beta-secretase (BACE1) processing of amyloid precursor protein (APP) and by decreasing neuroinflammation via STAT3 suppression. However, no peer-reviewed human clinical trials have tested anatabine specifically in Alzheimer's patients, so translating these rodent findings to a clinical recommendation is not currently supported by the evidence. Researchers have proposed it as a candidate for further study rather than an established treatment.

### What dose of anatabine was used in studies?

The commercial Anatabloc product typically delivered approximately 1 mg of anatabine per lozenge, with users taking 6–12 lozenges daily, equating to roughly 6–12 mg of anatabine per day. The unpublished Hashimoto's thyroiditis pilot study used approximately 12 mg/day. Rodent studies have used weight-adjusted doses that do not translate cleanly to human equivalents, and no formal dose-ranging pharmacokinetic study in humans has been published.

### Is anatabine the same as nicotine?

No, anatabine and nicotine are structurally distinct tobacco alkaloids with different receptor-binding profiles. Nicotine is a potent full agonist at most nAChR subtypes including the addiction-linked alpha-3 beta-4 receptor, while anatabine is a weaker partial agonist with comparatively lower affinity at those addiction-associated receptors. Anatabine's anti-inflammatory activity via NRF2 activation and STAT3 inhibition is a mechanism not prominently attributed to nicotine, distinguishing its proposed therapeutic profile.

### Why was Anatabloc taken off the market?

Star Scientific discontinued Anatabloc around 2013–2014 amid significant legal and financial difficulties facing the company, including shareholder lawsuits and executive misconduct allegations that had nothing to do with the supplement's safety profile. The FDA had also raised questions about whether anatabine-containing products were being marketed with unauthorized disease claims. These regulatory and corporate factors, rather than a specific safety recall, led to the product's disappearance from the market.

### How does anatabine citrate's mechanism of action differ from other neuroprotective supplements?

Anatabine citrate works through NRF2 activation and beta-amyloid APP inhibition, which are distinct pathways from common neuroprotective ingredients like curcumin (NF-κB modulation) or resveratrol (sirtuin activation). While preliminary evidence suggests anatabine may modulate cholinergic signaling similar to some cognitive supplements, human clinical data directly comparing its efficacy to other neuroprotective compounds remains limited. The citrate salt formulation also provides superior bioavailability compared to anatabine in its free-base form.

### Is anatabine citrate safe to take with common medications for cognitive health or inflammation?

Limited clinical data exists on anatabine citrate interactions with prescription medications, particularly those affecting cholinergic or inflammatory pathways (such as anticholinergic drugs or NSAIDs). Because anatabine may influence cholinergic signaling, individuals taking medications like donepezil or other cholinergic agents should consult a healthcare provider before supplementing. No major adverse events were reported in available clinical studies, but drug interaction profiles have not been comprehensively evaluated in human populations.

### What does the current research evidence show about anatabine citrate's effectiveness in humans?

Human clinical evidence for anatabine citrate remains preliminary, with mechanisms identified primarily through systems biology, cell culture, and preclinical models rather than large-scale randomized controlled trials. While theoretical support exists for its effects on inflammatory response (NRF2 activation) and cognitive function (APP inhibition), robust human efficacy data—particularly for Alzheimer's disease prevention or treatment—has not been established. The gap between promising mechanistic research and confirmed clinical benefits means anatabine citrate should be considered an investigational ingredient rather than an evidence-based therapeutic.

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