Description

Technical Parameters

Introduction

raws

product-1400-1400

Products Description

#### **1. Basic information**

**1.1 Chemical name and structure**

- **Common name**: Yohimbine Hydrochloride

- **IUPAC name**: Methyl 17α-hydroxyyohen-16α-carboxylate hydrochloride

- **Molecular formula**: C21H26N2O3·HCl

- **Molecular weight**: 390.9 g/mol

- **CAS number**: 65-19-0

**1.2 Source and history**

Yohimbe hydrochloride is an alkaloid extracted from the bark of the African Rubiaceae plant Yohimbe tree (*Pausinystalia johimbe*), which is chemically modified into a hydrochloride form to improve stability. In the late 19th century, local tribes used it in traditional medicine, and in the early 20th century it was introduced to the West as a nerve stimulant and aphrodisiac.

#### **2. Chemical and physical properties**

**2.1 Physical properties**

- **Appearance**: White to off-white crystalline powder, odorless.

- **Solubility**: Easily soluble in water (about 1:1), ethanol (1:10), slightly soluble in chloroform, almost insoluble in ether.

- **Melting point**: About 300°C (decomposition).

- **Stability**: Light-sensitive, need to be stored away from light; strong hygroscopicity, need to be sealed and moisture-proof.

**2.2 Chemical properties**

- **Acidity**: pH 4.5–6.0 (1% aqueous solution).

- **Optical rotation**: Dextrorotatory, [α]D²⁵ = +50° to +60° (aqueous solution).

- **Spectral characteristics**: UV absorption peaks are approximately at 226 nm and 282 nm (in ethanol).

#### **3. Classification and specifications**

**3.1 Classification by source**

1. **Natural extract**

- **Process**: Made from yohimbine bark by ethanol extraction, acid-base purification, and crystallization.

- **Advantages**: Natural source, suitable for "plant-based" product needs; may contain trace amounts of synergistic alkaloids.

- **Disadvantages**: High cost, purity depends on extraction technology (usually 95–98%).

2. **Chemical synthesis**

- **Process**: Using indole compounds as precursors, through multi-step organic synthesis (such as Mannich reaction).

- **Advantages**: Higher purity (≥99%), strong batch stability, suitable for pharmaceutical-grade applications.

- **Disadvantages**: High environmental pressure, need to deal with synthetic by-products.

**3.2 Classification by purity level**

1. **Pharmaceutical Grade**

- **Purity**: ≥99.5% (in line with USP/EP pharmacopoeia standards).

- **Use**: Prescription drug raw materials, used for ED treatment.

- **Testing standards**: HPLC, heavy metals (≤10 ppm), residual solvents (such as methanol <0.1%).

2. **Research Grade**

- **Purity**: 95–99%, containing a small amount of impurities (such as other yohimbine alkaloids).

- **Use**: Laboratory research, such as exploration of the mechanism of α2-adrenergic receptors.

3. **Industrial Grade**

- **Purity**: 90–95%, may contain plant residues or synthetic intermediates.

- **Use**: Health care product raw materials, requiring further processing.

#### **4. Core advantages**

**4.1 Pharmacological advantages**

- **Targeting α2-adrenaline receptors**: Selectively antagonizes α2 receptors, enhances norepinephrine release, and promotes fat decomposition (lipolysis).

- **Central nervous system stimulation**: Low doses can improve alertness, and high doses may cause anxiety (dose-dependent).

**4.2 Application field advantages**

- **Medical**: FDA approved for the treatment of psychological erectile dysfunction (ED), with an effective rate of about 30–40%.

- **Sports supplement**: As a "fat loss booster", it synergizes with caffeine to enhance metabolism (commonly found in Pre-workout formulas).

- **Scientific research tools**: Used to study the sympathetic nervous system and anxiety model construction.

**4.3 Production and market advantages**

- **Mature synthesis technology**: The yield of the mainstream process is more than 70%.

- **Market demand growth**: The global ED drug market has a compound annual growth rate of 5.2% (2023-2030), and the demand for fat-reducing supplements has surged.

#### **5. Detailed explanation of application scenarios**

**5.1 Medical field**

- **ED treatment**: Oral dose 5-10 mg/time, 3 times a day, doctor supervision is required (may cause blood pressure fluctuations).

- **Auxiliary application**: Research on antidepressant (regulating monoamine neurotransmitters) and diabetic neuropathy (improving microcirculation).

**5.2 Health products and sports nutrition**

- **Fat-reducing formula**: Often combined with caffeine (1:2 ratio), it enhances the cAMP signaling pathway by inhibiting phosphodiesterase.

- **Dosage range**: 2-5 mg/portion, overdose may cause palpitations (warning label required).

**5.3 Scientific research use**

- **Receptor research**: Used for functional differentiation experiments of α2 receptor subtypes (such as α2A, α2B).

- **Animal model**: Inducing anxiety-like behavior (mouse elevated plus maze test).

#### **6. Market and regulations**

**6.1 Global market landscape**

- **Major manufacturers**:

- **Europe and the United States**: Sigma-Aldrich (research grade), Spectrum Chemical (pharmaceutical grade).

- **Asia**: China Yirui Technology, India Sun Pharma (low-cost synthetic products).

- **Price range**:

- Research grade: $50–100/g (HPLC verification).

- Industrial grade: $10–20/g (bulk purchase).

**6.2 Regulatory restrictions**

- **USA**: Legal as a dietary supplement, but the FDA warns of its potential cardiovascular risks.

- **EU**: Some countries (such as Germany) list it as a prescription drug and prohibit non-medical sales.

- **China**: Not approved as a drug, and the import and export of raw materials requires a "Psychotropic Drug Import and Export Permit".

#### **7. Safety and side effects**

**7.1 Common side effects**

- **Mild**: dizziness, skin flushing, gastrointestinal discomfort (incidence of about 15%).

- **Severe**: hypertensive crisis, tachycardia (rare, more common in overdose).

**7.2 Contraindications**

- **Absolute contraindications**: severe cardiovascular disease, kidney disease, mental illness (such as anxiety).

- **Relative contraindications**: Combination with SSRI antidepressants may induce serotonin syndrome.

**7.3 Toxicology data**

- **LD50** (rat oral): about 150 mg/kg.

- **Long-term toxicity**: Animal experiments show hepatocyte cavitation (dose ≥ 20 mg/kg/day, for 90 days).

#### **8. Research progress and future trends**

**8.1 Frontier research**

- **Deepening of fat reduction mechanism**: Analysis of molecular pathways that activate thermogenesis in brown adipose tissue (BAT).

- **Nano delivery system**: Liposome encapsulation technology improves oral bioavailability (currently only 15–20%).

**8.2 Market trends**

- **Natural extraction revival**: Consumer preferences drive "clean label" products, but production capacity bottlenecks need to be resolved.

- **Combination preparation development**: Combined with low-dose sildenafil, balance ED treatment effect and safety.

#### **9. Summary**

As a versatile compound, yohimbine hydrochloride raw material powder spans the fields of medicine, health products and scientific research. Its core value lies in its unique α2 receptor antagonism mechanism, but safety risks require strict dosage control. In the future, with the breakthrough of precision drug delivery technology, its potential in the treatment of metabolic diseases is expected to be further released. Manufacturers need to balance compliance, purity and cost to meet the diverse needs of the global market.