Nicotine
3-[(2S)-1-methylpyrrolidin-2-yl]pyridine
Overview
Nicotine belongs to Stimulants.
Effects
- A quick, mild lift: increased alertness, concentration and arousal, a faster heart rate, and appetite suppression: often experienced as relaxing, especially in dependent users for whom it relieves craving.
- Physical effects: raised heart rate and blood pressure, and, with inhaled forms, airway irritation. Nausea, dizziness and a 'head rush' in naïve users or at higher doses.
- The reward is brief and quickly followed by wanting more. Withdrawal on stopping brings irritability, anxiety, restlessness, poor concentration, increased appetite and strong craving.
Dosing & duration
Inhaled (smoked/vaped), oral/buccal (snus, gum, lozenge), transdermal (patch) or nasal. Nicotine is not dosed in discrete 'recreational tiers': the figures below are context, not a recommendation.. Nicotine delivery depends heavily on the product and how it is used. A cigarette contains roughly 10–15 mg of nicotine but delivers only about 1–2 mg to the smoker. NRT products are labelled by nicotine content (e.g. patches ~7–21 mg/24 h, gum 2–4 mg per piece). E-liquid strength varies enormously (from a few mg/mL to very high 'nic-salt' concentrations). Pure nicotine and concentrated e-liquid are acutely toxic if swallowed and must be kept away from children and pets. There is no safe way to use it that avoids its high dependence potential. If used, prefer non-combusted forms and the lowest strength that controls craving.
Dose ranges
≈1–2 mg absorbed (of ~10–15 mg content)
2–4 mg per piece
≈7–21 mg over 24 h
Duration
Chemical & Physical Properties
| Formula | C10H14N2 |
| Molar mass | 162.23 g/mol |
| State | Liquid |
| Melting point | -79 °C |
| Boiling point | 247 °C |
| Density | 1.0097 g/cm³ at 20 °C (EPA, 1998) |
| Vapor pressure | 1 mmHg at 62 °C (EPA, 1998) |
| pKa | 8.11 |
| LogP | 1.17 |
| Solubility | Miscible (NTP, 1992), 1000000 mg/L, Miscible with water below 60 °C. Very sol in alcohol, chloroform, ether, petroleum ether, kerosene, oils |
| Refractive index | 1.5282 at 20 °C (D line) |
Identifiers & Synonyms
| CAS | 54-11-5 |
| CAS (enantiomer) | |
| PubChem CID | 89594 |
| InChIKey | SNICXCGAKADSCV-JTQLQIEISA-N |
| InChI | InChI=1S/C10H14N2/c1-12-7-3-5-10(12)9-4-2-6-11-8-9/h2,4,6,8,10H,3,5,7H2,1H3/t10-/m0/s1 |
| SMILES | CN1CCC[C@H]1c1cccnc1 |
Synonyms
- (S)-Nicotine
- 3-(1-methylpyrrolidin-2-yl)pyridine
- Nicotine
Pharmacodynamics & Biochemistry
Nicotine is the principal psychoactive alkaloid of tobacco (Nicotiana) and an agonist at nicotinic acetylcholine receptors (nAChRs): ligand-gated cation channels. Its high-affinity central target is the α4β2 subtype (Kᵢ in the low-nanomolar range), with additional activity at the α7 subtype (low affinity, rapidly desensitising) and at ganglionic α3β4 and neuromuscular receptors. Opening these channels depolarises neurons and, importantly, drives dopamine release in the mesolimbic reward pathway: the basis of nicotine's reinforcing, dependence-forming effect. The subjective effect is biphasic and situational: nicotine is a mild stimulant (increased alertness, concentration and heart rate, appetite suppression) but is also experienced as relaxing, partly because it relieves the withdrawal of dependent users. nAChRs desensitise quickly and then up-regulate with repeated exposure, which underlies rapid tolerance and the craving–withdrawal cycle. Peripheral actions include activation of the airway irritant receptor TRPA1 (contributing to the harshness of inhaled nicotine) and sympathetic/ganglionic stimulation. It is a weak base absorbed rapidly across the lungs (and buccal/nasal mucosa at suitable pH), reaching the brain within seconds of inhalation: the fast delivery that makes smoking and vaping so addictive. It is metabolised in the liver mainly by CYP2A6 to cotinine (itself long-lived, t½ ≈16 h, and used as an exposure biomarker). The nicotine plasma half-life is only ~1–2 h, which drives frequent redosing through the day.
Biological targets
- nAChR
Binding & functional measurements
| Target | Measurement | Species |
|---|---|---|
| nicotinic acetylcholine receptor α4 subunit | pKi 8.7 | Human |
| nicotinic acetylcholine receptor α3 subunit | pKi 5.8 | Human |
Pharmacokinetics
| Bioavailability | Inhaled ≈80–90%, oral low (first-pass) |
| Tmax | Smoked ≈minutes, gum/patch slower |
| Half-life | ≈1–2 h (metabolite cotinine ≈16 h) |
| Vd | Not reported |
| Protein binding | Not reported |
| Metabolism | Hepatic CYP2A6 to cotinine |
| Excretion | Renal |
Toxicology & Safety
Not reported
Nicotine is strongly dependence-forming, one of the most addictive drugs in common use, through fast delivery to the brain and mesolimbic dopamine release. Most people who use it regularly find it hard to stop. It raises heart rate and blood pressure and constricts blood vessels, so it stresses the cardiovascular system (caution after a recent heart attack, in unstable angina, uncontrolled hypertension or serious arrhythmia). It is genuinely toxic in overdose: concentrated e-liquids and pure nicotine can cause acute poisoning (nausea, vomiting, salivation, sweating, tremor, seizures and, at high doses, respiratory failure), which is a real hazard for children and pets who swallow refill liquid: such products must be stored safely. In pregnancy it harms fetal development. Two important caveats, though: the great majority of tobacco-related death and disease comes from the combustion products of smoking, NOT from nicotine itself, and nicotine is not a meaningful cause of cancer, and nicotine-replacement therapy is an established, comparatively safe way to deliver it for quitting. Youth use of high-strength vapes is a particular dependence concern.[4][6]
Legal Status
US: Legal (tobacco). UK: Legal. Regulated, age 18. DE: Legal (18+)
Interactions & Contraindications
Drug interactions
Contraindications
No interactions or contraindications listed.
Usage & Context
- Used overwhelmingly as a recreational/dependence drug: smoked (cigarettes, cigars), vaped (e-cigarettes), or taken as oral/nasal tobacco (snus, chewing tobacco, snuff): for its stimulant-yet-relaxing effect and, in dependent users, to relieve withdrawal.
- Also a medicine: nicotine-replacement therapy (patches, gum, lozenges, inhalers, nasal spray) delivers nicotine without tobacco smoke as an aid to stopping smoking.
- Historically an agricultural insecticide, and a foundational molecule in pharmacology: the receptors it defines (the 'nicotinic' acetylcholine receptors) are named after it.
Sources & Evidence
- PubChem: Nicotine (CID 89594) — identifiers & experimental properties
- IUPHAR/BPS Guide to PHARMACOLOGY (GtoPdb): nicotine (ligand 2585) — human nAChR α4/α3 binding CC BY-SA 4.0
- Picciotto MR, Zoli M, Rimondini R, et al. (1998). Acetylcholine receptors containing the beta2 subunit are involved in the reinforcing properties of nicotine. Nature 391:173-7.
PMID 9428762 · doi:10.1038/34413
- Benowitz NL (2009). Pharmacology of nicotine: addiction, smoking-induced disease, and therapeutics. Annu Rev Pharmacol Toxicol 49:57-71.
PMID 18834313 · doi:10.1146/annurev.pharmtox.48.113006.094742
- FDA / DailyMed: Nicotine prescribing information — pharmacokinetics & metabolism
- U.S. FDA: Tobacco Products — regulation of tobacco, nicotine and e-cigarettes, and youth-use/poisoning concerns
- Nirogi R, Mohammed AR, Shinde AK, et al. (2020). Discovery and Development of 3-(6-Chloropyridine-3-yloxymethyl)-2-azabicyclo[3.1.0]hexane Hydrochloride (SUVN-911): A Novel, Potent, Selective, and Orally Active Neuronal Nicotinic Acetylcholine α4β2 Receptor Antagonist for the Treatment of Depression. J Med Chem 63:2833-2853.
PMID 32026697 · doi:10.1021/acs.jmedchem.9b00790