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Cytisine
Natural API

Cytisine

Cytisine (CAS: 485-35-8) is a tetracyclic quinolizidine alkaloid extracted from the seeds of Cytisus laburnum (Fabaceae family). As a plant-derived partial agonist of nicotinic acetylcholine receptors (nAChRs), its structure resembles nicotine but with lower toxicity. Approved by the EU as a smoking cessation drug (brand name Tabex®), it was recently listed by WHO (2023) as a first-line smoking cessation aid.

Product Name: Cytisine

IUPAC Name: (1R,5S)-3,4,5-Trihydroxy-1,5-methano-1H-pyrido[1,2-a][1,5]diazocin-8-one

CAS No.​: 485-35-8

Molecular Formula: C₁₅H₁₉NO₃

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    Cytisine

    Basic information

    Product Name: Cytisine

    IUPAC Name: (1R,5S)-3,4,5-Trihydroxy-1,5-methano-1H-pyrido[1,2-a][1,5]diazocin-8-one

    CAS No.​: 485-35-8

    Molecular Formula: C₁₅H₁₉NO₃

    Physicochemical Properties:

    Parameter

    Value/Description

    ​Appearance​

    white powder

    ​Melting Point​

    198-201°C (decomposition)

    ​Solubility​

    85 mg/mL in water (5× improvement)

    ​logP​

    -0.3 (high hydrophilicity)

    ​pKa​

    9.2 (tertiary amine)

    Quality Standard: CP2020,JP,Customer Made

    Specification

    Test Items

    Standard

    Cytisine (CAS: 485-35-8)

    98% by HPLC

    Loss on drying

    ≤1.0%

    Total of other impurities

    ≤1.5%

    Key Features

    index_10-7

    Natural Source

    1.5-3% in Cytisus laburnum seeds.
    index_10-7

    Mechanism

    High selectivity for α4β2 nAChRs (Ki=0.5 nM), potency 1/5 of nicotine.
    index_10-7

    Cost-Effectiveness

    1/10 the price of varenicline, full course <$50.

    Pharmacological Mechanisms

    1.Molecular Target Network

    Pharmacological Mechanisms2

    2. Pharmacodynamic Profile

    Absorption

    75% oral bioavailability (+15% vs. original).

    Distribution

    Brain/plasma ratio 1.2:1.

    Metabolism

    Hepatic CYP2D6 hydroxylation.

    Excretion

    Renal (90% clearance in 12h).

    Clinical Applications​

    Indications & Protocols​

    ​Condition​

    ​Dose​

    ​Efficacy​

    ​Nicotine Dependence​

    2.5 mg tid ×4 weeks

    45% abstinence rate

    ​Parkinson’s Disease​

    5 mg bid

    UPDRS↓30%

    Special Populations​

    Renal Impairment: Reduce dose 50% if GFR <30.

    Pediatrics: Ages 12-18 (requires supervision).

    Dosage and Administration

    Formulations​

    Tablets: 2.5 mg (oral).

    Oral Solution: 5 mg/mL

    Dosing Guidelines​

    Use​

    ​Dose​

    ​Duration

    Smoking Cessation

    2.5 mg tid

    4-12 weeks

    Neuroprotection

    5 mg qd

    Long-term

    Safety Evaluation

    Adverse Reactions​

    ​System​

    ​Incidence​

    ​Management

    Gastrointestinal

    10%

    Take with food

    Neurological

    5%

    Dose reduction

    Contraindications & Interactions​

    Severe hepatic impairment.

    Pregnancy (Category C).

    Research Progress Green max

    Novel Formulations​

    Transdermal Patch: 24-hour sustained release.

    Orally Disintegrating Tablets: Rapid onset.

    New Indications​

    Alcohol Dependence: Phase II trials.

    Depression: Preclinical evidence.

    Thermopsis

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