bulleyaconitine A transdermal matrix patch (XEL 002BP) / Xel Pharma - LARVOL DELTA

Synthesis and Evaluation of a Series of New Bulleyaconitine A Derivatives as Analgesics. (PubMed, ACS Omega) - "Among them, 2w showed the best analgesic activity and the longest duration. Its pain threshold reached 166.35% in 15 min, peaked at 30 min (182.35%), and remained 82.59% even at 60 min."

Journal • Pain

Bulleyaconitine A Inhibits Visceral Nociception and Spinal Synaptic Plasticity through Stimulation of Microglial Release of Dynorphin A. (PubMed, Neural Plast) - "Dynorphin A also inhibited spinal synaptic plasticity in a κ-opioid receptor-dependent manner. These results suggest that BAA produces visceral antinociception by stimulating spinal microglial release of dynorphin A, which activates presynaptic κ-opioid receptors in afferent neurons and inhibits spinal synaptic plasticity, highlighting a novel interaction mode between microglia and neurons."

Journal • Addiction (Opioid and Alcohol) • Gastrointestinal Disorder • Immunology • Pain

Bulleyaconitine A inhibits the lung inflammation and airway remodeling through restoring Th1/Th2 balance in asthmatic model mice. (PubMed, Biosci Biotechnol Biochem) - "In addition, BLA suppressed the secretion of IgE, Th2-type cytokines, and IL-17A, but enhanced secretions of Th1-type cytokines in BALF and serum. The current study discovered that BLA inhibited the lung inflammation and airway remodeling via restoring the Th1/Th2 balance in asthmatic mice."

Journal • Preclinical • Asthma • Immunology • Respiratory Diseases • IL17A

Bulleyaconitine A Exerts Antianxiety and Antivisceral Hypersensitivity Effects. (PubMed, Front Pharmacol) - "In conclusion, our study demonstrated, for the first time, that BAA exerted marked antivisceral pain and antianxiety effects, which expands the analgesic spectrum and clinical application of BAA. Furthermore, it also it provides a better guidance for the clinical use of BAA."

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Bulleyaconitine A inhibits itch and itch sensitization induced by histamine and chloroquine. (PubMed, Neuroscience) - "Both the itch sensitization and synaptic potentiation were substantially attenuated by intragastrical BLA. Together, BLA was effective in inhibiting histamine-dependent and histamine-independent itches, and the mechanisms underlying these effects were involved but not limited to the inhibition of GRP-GRPR signaling in the spinal dorsal horn."

Journal • GRP-10

Bulleyaconitine A prevents Ti particle-induced osteolysis via suppressing NF-κB signal pathway during osteoclastogenesis and osteoblastogenesis. (PubMed, J Cell Physiol) - "Furthermore, BLA showed preventive effect in Ti particle-induced osteolysis model in vivo. Together, all our data demonstrated that BLA suppressed osteoclastogenesis and promoted osteoblastogenesis via suppressing NF-κB signal pathway and could be an alternative therapeutic choice against bone loss."

Journal

Bulleyaconitine A Effectively Relieves Allergic Lung Inflammation in a Murine Asthmatic Model. (PubMed, Med Sci Monit) - "MATERIAL AND METHODS Specific-pathogen-free (SPF) female Balb/c mice were randomly divided into the following 6 groups: (1) Control group (NC), (2) Asthma group (AS), (3) BLA-L group, (4) BLA-M group, (5) BLA-H group, and (6) Dexamethasone group. Moreover, BLA inhibited the expression of NF-κB1 and PKC-d via the NF-κB signaling pathway in the lung. CONCLUSIONS Our data show that BLA activates PKC-δ/NF-κB to reduce airway inflammation in allergic asthma mice."

Journal • Preclinical