ABSTRACT
Neuropathic pain is a debilitating pathological condition that presents significant therapeutic challenges in clinical practice. Unfortunately, current pharmacological treatments for neuropathic pain lack clinical efficacy and often lead to harmful adverse reactions. As G protein-coupled receptors (GPCRs) are widely distributed throughout the body, including the pain transmission pathway and descending inhibition pathway, the development of novel neuropathic pain treatments based on GPCRs allosteric modulation theory is gaining momentum. Extensive research has shown that allosteric modulators targeting GPCRs on the pain pathway can effectively alleviate symptoms of neuropathic pain while reducing or eliminating adverse effects. This review aims to provide a comprehensive summary of the progress made in GPCRs allosteric modulators in the treatment of neuropathic pain, and discuss the potential benefits and adverse factors of this treatment. We will also concentrate on the development of biased agonists of GPCRs, and based on important examples of biased agonist development in recent years, we will describe universal strategies for designing structure-based biased agonists. It is foreseeable that, with the continuous improvement of GPCRs allosteric modulation and biased agonist theory, effective GPCRs allosteric drugs will eventually be available for the treatment of neuropathic pain with acceptable safety.
ABSTRACT
Objective To determine the steam distillation processing of Elsholtzia and to optimize different parts volatile oil of the anti-bacterial activity and anti-oxidation activityfrom Elsholtzia. Methods The volatile oil of different parts from Elsholtzia was extracted by steam distillation. The anti-oxidationactivity was texted by DPPH. The antibacterial activity was detected by disk diffusion test. Results Watering 14 times, soaking 6 hours, extracting 3 hours by steam distillation to extracte different parts of volatile oil. It is effective that volatile oil inhibit Escherichia coli, Staphylococcus aureus, Dysentery bacillus＇s blessing. The sequential of antibacterial activity was that Escherichia coli ＞ Dysentery bacillus＇s blessing ＞ Staphylococcus aureus ＞Pseudomonas aeruginosa. The anti-oxidation activity increased the concentration of volatile oil, and was konwn to be the best when the content of the volatile oil is 10%. The anti-oxidation activity of VC was stonger than volatile oil. Conclusions It is effective that volatile oil inhibit Escherichia coli, Staphylococcus aureus, Dysentery bacillus＇s blessing and the volatile oil from inflorescence have a stronger antibacterial activity than the volatile oil from leaf.