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Product name: O-Methylbulbocapnine
Synonym name: (+)-O-Methylbulbocapnine; Bulbocapnine methyl ether
Catalogue No.: BP4685
Cas No.: 2490-83-7
Formula: C20H21NO4
Mol Weight: 339.391
Botanical Source:
Type of Compound: Alkaloids
Purity: 95%~99%
Analysis Method: HPLC-DAD or/and HPLC-ELSD
Identification Method: Mass, NMR
Packing: Brown vial or HDPE plastic bottle
Storage: Store in a well closed container, protected from air and light. Put into refrigerate or freeze for long term storage.
Whenever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20℃. Generally, these will be useable for up to two weeks.
The product could be supplied from milligrams to grams
Inquire for bulk scale.
For Reference Standard and R&D, Not for Human Use Directly.
HPLC of O-Methylbulbocapnine
Storage conditions：Short-term storage at 2~8℃, long-term storage at -20 ~ -80℃
40.1600
3.1471
2.8017
.0308
4.7361
25.3463
High
78.2188
3.1706
No
No
Yes
Yes
Yes
No
1.2
Yes
No
No
No
O-methylbulbocapnine (CAS No.: 2490-83-7) is a natural base compound with significant pharmacological activity, belonging to the isoquinoline alkaloid family. As an important active ingredient in traditional Chinese medicinal plants, O-methyl globule purpline alkaloid demonstrates broad research value in analgesic and neuromodulation fields due to its unique chemical structure and multi-target mechanism. In recent years, with in-depth exploration of natural product pharmacology, the pharmacological activity and target effects of O-methyl globule purine have gradually been revealed, especially its potential applications in pain management have attracted widespread attention.
This paper aims to systematically review the chemical structure and physicochemical properties, plant origin and extraction methods, pharmacological activity and mechanism of action of O-methyl globular puricosine, druggability evaluation and pharmacokinetic characteristics, and to explore its clinical application prospects and research prospects, providing theoretical basis and research directions for subsequent drug development and clinical translation.
O-methyl spherical purpline has the molecular formula C20H21NO4 and molecular weight of 339.3910, belonging to the isoquinoline alkaloids. Its structural features include a typical tetracyclic framework containing methoxy substituents, giving it a unique spatial configuration and chemical reactivity. The compound's LogP value was 3.1471, indicating moderate lipid solubility, which facilitates penetration of cell membranes and the blood-brain barrier. The polar surface area (TPSA) is 40.16 Ų, indicating low molecular polarity, further supporting its good membrane permeability.
Low water solubility (0.0308 mg/mL) suggests possible solubility limits in vivo, requiring appropriate formulation techniques to improve bioavailability. The high permeability of the blood-brain barrier indicates that this compound can effectively enter the central nervous system and exert neuroregulatory effects. However, O-methyl globule violine has hERG channel inhibitory activity, suggesting potential risks in cardiotoxicity and requiring special attention during drug development. The Ames test value was 1.2, indicating a low genotoxicity risk and a certain safety basis.
O-methyl Corydalis is mainly found in the poppy family plant Corydalis spp., especially in the rhizome parts of Corydalis species. In traditional Chinese medicine, Cypine Violet is widely used for promoting blood circulation, removing blood stasis, relieving pain, and anti-inflammatory. Its active ingredients include various isoquinoline alkaloids, with O-methyl Violet Alkaloid being an important representative.
The extraction method usually uses organic solvent extraction technology. Common steps include:
In recent years, the application of ultrasound-assisted extraction and microwave-assisted extraction technologies has improved extraction efficiency and purity, reduced solvent usage, and aligned with green chemistry principles.
The pharmacological activity of O-methylglobulin puruline mainly focuses on analgesic effects and nervous system regulation. Multiple in vivo and in vitro studies have shown that this compound provides significant relief for various pain models, including inflammatory pain, neuropathic pain, and acute pain.
Experimental studies have shown that O-methyl globular purine can significantly reduce pain responses in mouse hot plate experiments and acetate torsion experiments, demonstrating good central and peripheral analgesic activity. Its analgesic effect is similar to classic opioids, but with milder side effects and better safety.
Additionally, O-methyl globule puricoline regulates dopamine D2 receptor (DRD2), potentially affecting neurotransmitter release and neuroexcitability, suggesting its potential application in neurodegenerative and psychiatric diseases.
By inhibiting cyclooxygenase (PTGS1 and PTGS2) activity, O-methyl globule violetine exhibits certain anti-inflammatory effects, reducing the release of inflammatory mediators and assisting in analgesic effects.
The analgesic effect of O-methyl globule violine involves multi-target coordinated regulation, with main targets including:
TRPV1 (Transient Receptor Potential Vanillic Acid Receptor 1): As a key ion channel for pain perception, TRPV1 is involved in the transmission of inflammation and heat pain signals. O-methylglobular violine can regulate TRPV1 activity and reduce the excitability of pain nerves.
TRPA1 (Transient Receptor Potential Vanillin Receptor Subtype A1): Similar to TRPV1, TRPA1 plays a role in chemical and inflammatory pain. O-methylglobular purple bililine regulates TRPA1 channels to reduce pain signaling.
Opioid receptors (OPRD1, OPRM1, OPRK1): Includes three subtypes: δ, μ, and κ. Opioid receptors are classic targets for analgesics. O-methyl globule violet has certain affinity for these receptors and may exert analgesic effects by activating the endogenous opioid system.
CNR1 (Cannabinoid Receptor 1): Involved in regulating pain, mood, and inflammatory responses. O-methylglobulin purple ketaline helps regulate CNR1 and supports its analgesic and anti-inflammatory effects.
PTGS1 and PTGS2 (cyclooxygenases 1 and 2): catalyze prostaglandin synthesis, mediating inflammation and pain responses. O-methyl globule violine inhibits the activity of these two enzymes, reducing the release of inflammatory mediators.
SLC6A4 (5-hydroxytryptamine transporter): Regulates the reuptake of the neurotransmitter 5-hydroxytryptamine, affecting mood and pain perception. O-methylglobule purpline may improve pain-related mood disorders by modulating SLC6A4.
DRD2 (dopamine D2 receptor): regulates neural excitability and reward mechanisms, participating in pain regulation and maintaining mental status.
In summary, O-methyl globule purple birine regulates nervous system excitability and inflammatory responses through multi-target and multi-pathway synergistic effects, exerting comprehensive analgesic effects.
The LogP value (3.1471) and TPSA (40.16) of O-methyl globule purine both met the Lipinski rule, indicating good oral bioavailability potential. Its low water solubility (0.0308 mg/mL) may limit absorption rate and degree, requiring formulation optimization and improvement.
The high permeability of the blood-brain barrier supports its development as a central analgesic agent. The inhibitory activity of hERG channels suggests potential cardiotoxicity risks and requires focused monitoring during drug safety assessments. Ames test results showed a low genotoxicity risk and a solid safety foundation.
Currently, systematic pharmacokinetic research on O-methyl globule puritine is relatively limited. Preliminary data already indicate that this compound is rapidly absorbed orally, has a moderate plasma half-life, and can effectively distribute to the central nervous system. Its metabolic pathway may involve the hepatic cytochrome P450 enzyme system, and the metabolites require further identification.
Excretion mainly occurs via the kidneys and bile pathways, with a low risk of accumulation in the body. In the future, it is necessary to combine in vivo and in vitro models to conduct in-depth research on their pharmacokinetic parameters and metabolic mechanisms, providing a basis for clinical dosage design.
O-methyl globule puricosterine, as a natural analgesic active ingredient with multi-target effects, has significant analgesic and anti-inflammatory properties, and can cross the blood-brain barrier, making it suitable for central pain management. Its low genotoxicity and favorable druggability parameters lay the foundation for clinical translation.
Future research should focus on the following aspects:
In summary, O-methylglobulin violine has the potential to become a novel central analgesic drug and warrants further in-depth development and clinical research.
O-methyl Bulb Violetalin, as an isoquinoline natural base derived from Viola globularis plants, shows broad application prospects in analgesic and neuromodulation fields due to its unique chemical structure and multi-target mechanism. Its excellent blood-brain barrier permeability and multi-target synergistic effects provide new therapeutic approaches for pain management.
Although there is currently a preliminary understanding of its pharmacological activity and mechanism of action, systematic research on pharmacokinetics, safety, and preclinical studies is still needed to address issues such as poor water solubility and potential cardiotoxicity, and to promote its clinical application. In the future, through multidisciplinary collaboration and technological innovation, O-methylglobule violine alkaloids are expected to become an important candidate for the development of naturally derived analgesic drugs, offering new treatment options for pain patients.
Shenshuai
Wenjing
Hedandan
