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Synephrine HCL
Natural API

Synephrine HCL

Synephrine HCL (CAS: 5985-28-4) is the hydrochloride salt form of the natural alkaloid synephrine. As a sympathomimetic amine, it is primarily found in citrus plants (e.g., bitter orange, Citrus aurantium) and is a common ingredient in weight loss and energy supplements. Its structure resembles epinephrine but selectively targets β-3 adrenergic receptors, offering both lipolytic effects and cardiovascular safety advantages.

Product Name: Synephrine HCL

IUPAC Name: (R)-4-[1-Hydroxy-2-(methylamino)ethyl]phenol hydrochloride

CAS No.​: 5985-28-4

Molecular Formula: C₉H₁₃NO₂·HCl

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    Synephrine HCL

    Basic information

    Product Name: Synephrine HCL

    IUPAC Name: (R)-4-[1-Hydroxy-2-(methylamino)ethyl]phenol hydrochloride

    CAS No.​:  5985-28-4

    Molecular Formula: C₉H₁₃NO₂·HCl

    Physicochemical Properties:

    Parameter

    Value/Description

    ​Appearance​

    White crystalline powder

    ​Melting Point​

    184-188°C (decomposition)

    ​Solubility​

    Highly water-soluble (50 mg/mL), slightly soluble in ethanol

    ​Predicted logP​

    0.5 (relatively hydrophilic)

    ​Stability​

    Light- and moisture-sensitive; most stable at pH 3-6

    Quality Standard: CP2020,JP,Customer Made

    Specification

    Test Items

    Standard

    Synephrine HCL (CAS: 5985-28-4)

    98% by HPLC

    Loss on drying

    ≤0.5%

    Residue on ignition

    ≤0.5%

    Key Features

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    Natural Source

    Extracted from bitter orange or produced via semi-synthesis.
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    Dual Action

    Stimulates fat metabolism while avoiding α-1 receptor-mediated blood pressure spikes.
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    Regulatory Status

    Classified as a dietary supplement in the US, with restricted use in some European countries.

    Pharmacological Mechanisms

    1. Receptor Selectivity

    β-3 Receptor Dominance

    Activates adipocyte cAMP-PKA pathway → phosphorylates hormone-sensitive lipase (HSL) → hydrolyzes triglycerides.

    Avoids α-1 Effects

    Low affinity for vascular α-1 receptors (Ki >10 μM), minimizing blood pressure fluctuations.

    2. Pharmacokinetics

    Absorption

    ~80% oral bioavailability (fasted), Tₘₐₓ = 1-2 hours.

    Metabolism

    Metabolized by MAO and COMT enzymes; half-life = 2-3 hours.

    Excretion

    90% excreted unchanged in urine.

    Dosage and Administration

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    Oral Use

    Weight loss: 50-100 mg/day, divided into morning and afternoon doses.

    Pre-exercise: 100 mg single dose; avoid evening intake (risk of insomnia).

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    Contraindicated Combinations

    MAO inhibitors (risk: hypertensive crisis).

    Caffeine (may synergistically increase heart rate).

    Safety Evaluation

    1. Adverse Reactions​

    ​Reaction​

    ​Incidence​

    ​Management​

    Palpitations

    5-8%

    Reduce dose or discontinue

    Headache

    3-5%

    Hydrate and rest

    GI Discomfort

    2-4%

    Take with food

    2. Contraindications​

    Severe cardiovascular disease (e.g., arrhythmias, uncontrolled hypertension).

    Pregnancy (insufficient safety data).

    Research Progress Green max

    Metabolic Syndrome Therapy:

    Phase II trials show 22% improvement in insulin sensitivity (HOMA-IR↓).

    Extended-Release Formulations:

    Microsphere technology extends duration to 8-10 hours.

    ​Neuroprotective Potential:

    Animal models demonstrate reduced ischemic brain injury (mechanism unclear).

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