Drug intelligence / Profile preview

bulleyaconitine a

Development stage
Unknown
Lead developer
KPC Pharmaceuticals
Modality
Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Oral, Intramuscular
01

Overview

Bulleyaconitine a is a C-19 diterpene diester alkaloid isolated from various *Aconitum* species, notably *Aconitum bulleyanum*. It is an analgesic and anti-inflammatory small molecule drug that acts primarily as a voltage-gated sodium channel blocker, reducing neuronal excitability and pain transmission. Clinically, it has been used in China since the 1980s for chronic pain associated with musculoskeletal disorders such as rheumatoid arthritis, frozen shoulder, muscle strain, and fracture-induced pain. Unlike opioids such as morphine, bulleyaconitine a is non-addictive. Its mechanism of action includes inhibition of voltage-gated sodium channels in dorsal root ganglion neurons and modulation of the Src/PI3K/Akt signaling pathway to inhibit osteoclast differentiation and bone destruction in conditions like rheumatoid arthritis. It also exhibits anesthetic activity when combined with other agents like lidocaine or epinephrine[1][2][3][4][6].

Other names
BulleyaconitineBULLEYACONITINE ABulleyaconi cine ABULLEYACONITINE A(P)Bulleyaconitine A-RMBULLEYACONITINE A(RG)crassicauline A(bulleyaconitine)Bulleyaconitine A USP/EP/BP
02

Targets

SCN10A (Sodium channel protein type X alpha subunit)SCN9A (Sodium channel protein type 9 subunit alpha)AKT1 (Proto-oncogene serine/threonine-protein kinase Akt1)PIK3CA (Phosphoinositide 3-kinase alpha)SRC (Proto-oncogene tyrosine-protein kinase Src)

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