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Synonym name: Allapinin; Allapinin
Catalogue No.: BP0843
Cas No.: 97792-45-5
Formula: C32H45BrN2O8
Mol Weight: 665.622
Botanical Source:
Purity: 95%~99%
Analysis Method: HPLC-DAD or/and HPLC-ELSD
Identification Method: Mass, NMR
Packing: Brown vial or HDPE plastic bottle
Can be supplied from milligrams to grams.
For Reference Standard and R&D, Not for Human Use Directly.
Inquire for bulk scale.
HPLC of Lappaconitine hydrobromide
Storage conditions：Short-term storage at 2~8℃, long-term storage at -20 ~ -80℃
126.7900
2.4138
2.3520
.1068
1.7842
5.2915
Low
75.3297
7.1444
No
No
Yes
No
No
No
0.0
No
No
Yes
No
Lappaconitine hydrobromide (CAS number: 97792-45-5) is a natural alkaloid compound derived from Aconitum plants, exhibiting significant analgesic activity. As an important alkaloid component in traditional Chinese medicine, Gao Wujia and its salt derivatives have attracted widespread attention in the field of natural product pharmacology in recent years due to their unique pharmacological effects and relatively low toxicity side effects. Hydrobromic acid hyperoxamethylene not only demonstrates effective inhibitory effects on various pain models but also demonstrates multi-target regulatory capability at the molecular level, especially interactions with various pain-related receptors and enzymes, providing a theoretical and experimental basis for the development of new analgesic drugs.
This paper aims to systematically review the chemical structure and physicochemical properties, plant origin and extraction methods, pharmacological activity and mechanism of action, druggability evaluation, and pharmacokinetic characteristics of Hydrobromide Gaoxaji, and to explore its clinical application prospects and development trends, providing a reference for in-depth research and clinical translation of this natural product.
Hydrobromic acid hyperoxamethylene is a complex bicyclic dihydroalkaloid with a molecular formula of C36H50N2O9 and a molecular weight of 584.7100. Its structural core is a typical aconite alkaloid backbone, containing multiple chiral centers and various functional groups, including ester, ether bonds, and amino groups, giving it unique chemical activity. The hydrobromide form improves its water solubility, with a water solubility of about 0.1068 mg/mL, making it suitable for formulation development.
In terms of physicochemical properties, the LogP value of Hydrobromide Glycatin is 2.4138, indicating moderate lipid solubility, which facilitates cell membrane penetration without excessive hydrophobicity. The polar surface area (TPSA) was 126.79 Ų, indicating high molecular polarity, which may affect its oral absorption and blood-brain barrier penetration ability. The blood-brain barrier permeability was assessed as low, indicating its limited distribution in the central nervous system, a characteristic that helps reduce central-related side effects. The hERG ion channel inhibition test was negative, indicating a low risk of cardiotoxicity. The Ames-induced mutagenic test result was 0.0, indicating a low genotoxicity risk and good safety.
Hydrobromic acid (Aconitum spp.) mainly comes from plants of the genus Aconitum (Aconitum spp.), especially species rich in high aconite content such as Aconitum lappaceum and other related species. Aconite plants are widely distributed in southwestern China and the Himalayan mountains, and are an important part of traditional Chinese medicine.
The extraction process typically involves extracting dried plant roots and stems with acidic aqueous solutions or organic solvents, followed by separation and purification by liquid-liquid separation and column chromatography. The specific steps include:
In recent years, the application of ultrasound-assisted extraction and microwave-assisted extraction technologies has improved extraction efficiency and purity, reduced the use of organic solvents, and aligned with the concept of green chemistry.
The main pharmacological activity of Oxymethyl Hydrobromide is focused on analgesic effects, showing good analgesic effects in various animal models, including models of inflammatory pain, neuropathic pain, and cancer pain. Compared to traditional opioid analgesics, oxymethyl hydrobromide has lower addictiveness and resistance, demonstrating potential clinical advantages.
Animal experiments have shown that high-auromethyl hydrobromide can significantly prolong reaction time in hot plate experiments and reduce pain reactions caused by mechanical and chemical stimuli. Its analgesic effects involve both the central nervous system and peripheral nerve endings, demonstrating a multi-layered analgesia mechanism.
Some studies indicate that glycoxyl hydrobromide inhibits the release of inflammatory mediators, reducing the expression of inflammatory factors such as prostaglandins (PGE2) and cyclooxygenases (COX-1, COX-2), thereby relieving pain and tissue swelling caused by inflammation.
In neurodamage models, methyl oxymethyl hydrobromide shows certain neuroprotective effects, possibly by regulating neurotransmitter release and suppressing neuroinflammatory responses, reducing neuronal damage and promoting neurological function recovery.
The analgesic effect of hyperoxamethyl hydrobromide involves multiple molecular targets, reflecting its pharmacological characteristics of multi-target regulation. The main targets include:
TRPV1 (Transient receptor potential vanillic acid receptor 1): As an important ion channel for pain perception, TRPV1 is involved in the transmission of heat and inflammatory pain. Hydrobromide glycoxyl can regulate TRPV1 activity, inhibit its over-activation, and reduce pain signaling.
CNR1 (Cannabinoid Receptor 1): CNR1 regulates pain and emotional responses in the central nervous system. Hydrobromide glycoxyl may activate or regulate CNR1, exerting analgesic and anti-anxiety effects.
OPRD1, OPRM1, OPRK1 (δ, μ, κ opioid receptors): These opioid receptors are the main targets of action in traditional analgesics. The interaction between hydrobromide and oxymethyl acutane and opioid receptors enhances the analgesic effect of the endogenous opioid system while avoiding the side effects of typical opioids.
PTGS1 and PTGS2 (cyclooxygenases 1 and 2): As key enzymes in prostaglandin synthesis, PTGS1 and PTGS2 play important roles in inflammation and pain processes. Oxymethyl hydrobromide inhibits the activity of these two enzymes, reducing the production of inflammatory mediators.
TRPA1 (Transient Receptor Potential A1): TRPA1 is involved in the perception of chemical and mechanical pain. The regulation of TRPA1 by methanol hydrobromide helps relieve various types of pain.
SLC6A4 (serotonin transporter): By regulating serotonin reuptake, hyperoxamethylene hydrobromide may affect central nervous system analgesia and mood regulation.
DRD2 (Dopamine Receptor D2): The dopamine system is involved in pain regulation and emotional states. The effect of hyperoxamethyl hydrobromide on DRD2 may enhance its analgesic and antidepressant effects.
Overall, high-auromethyl hydrobromic acid regulates pain signal transduction and inflammatory responses through multi-target and multi-pathway synergistic effects, demonstrating its complex and effective analgesic mechanism.
The druggability evaluation of Gaoxajia hydrobromide indicates its promising potential for drug development. Its molecular weight is 584.7, slightly above the 500 recommended by Lipinski's rules, but moderate LogP and higher TPSA suggest some limitations in its in vivo distribution, especially due to its low blood-brain barrier permeability, which helps reduce central nervous system side effects.
In terms of safety, the hERG ion channel inhibition test was negative, indicating a low risk of cardiotoxicity; The Ames test result was zero, indicating a low genotoxicity risk and a solid safety foundation.
Pharmacokinetic studies show that oral absorption of glycomethylene hydrobromide is relatively slow, with limited bioavailability, possibly related to its higher polarity and lower water solubility. In vivo distribution is mainly limited to peripheral tissues, with a high plasma protein binding rate. The metabolic pathway mainly involves oxidation and hydrolysis through the hepatic cytochrome P450 enzyme system, and the metabolites are safe. Excretion is mainly through urine and bile.
To improve its pharmacokinetic performance, researchers have attempted to enhance its bioavailability and targeting through formulation modifications (such as nanocarriers and liposome encapsulation) and structural modifications.
As a natural multi-target analgesic, high-aurogen hydrobromide has broad clinical application prospects. Its low addictiveness, low drug resistance, and good safety give it potential advantages in chronic pain management, neuropathic pain, and inflammatory pain treatment.
Currently, preclinical and early clinical trials of Hydrobromic Acid Gaolixin have been conducted in some countries and regions, demonstrating good analgesic effects and tolerability. Future research directions include:
In summary, as a natural analgesic with unique advantages, high-oxalurogen hydrobromide is expected to become one of the key drugs in the future field of pain management.
With its complex chemical structure, multi-target pharmacological effects, and good safety, it has become a research hotspot in the development of natural product analgesics. Its multiple activities in pain relief, anti-inflammation, and neuroprotection provide new ideas and strategies for pain management. Although challenges such as pharmacokinetic performance and clinical validation still exist, with advances in modern drug development technology, Gaoxajia hydrobromide is expected to successfully transition from laboratory to clinical practice, benefiting a wide range of patients. Future research should focus on mechanism analysis, formulation optimization, and clinical application, promoting the development of safe and effective new analgesic drugs.
Shenshuai
Wenjing
Hedandan
