Yaoxue Xuebao

YX-18-11-2024-2130
| Yaoxue Xuebao (ISSN:0513-4870)

Development of analgesic drugs targeting Nav1.7: advances in clinical trials and discovery of selective inhibitors

Chronic pain is a widespread disorder affecting millions of people and is insufficiently addressed by current classes of analgesics due to significant long-term or high dosage side effects. A promising approach that was recently proposed involves the systemic inhibition of the voltage-gated sodium channel Nav1.7, capable of cancelling pain perception completely. Notwithstanding numerous attempts, currently no drugs have been approved for the inhibition of Nav1.7. The task is complicated by the difficulty of creating a selective drug for Nav1.7, and avoiding binding to the many human paralog

YX-18-11-2024-2129
| Yaoxue Xuebao (ISSN:0513-4870)

Exploration of the antioxidant role and mechanism of Astragalus membranaceus based on a glucose-induced Caenorhabditis elegans model

Astragali radix is a traditional medicinal herb with a long history and wide application. It is frequently used in prescriptions with other medicinal materials to replenish Qi. According to the classics of traditional Chinese medicine, Astragali radix is attributed with properties such as Qi replenishing and surface solidifying, sore healing and muscle generating, and inducing diuresis to reduce edema. Modern pharmacological studies have demonstrated that some extracts and active ingredients in Astragali radix function as antioxidants. The polysaccharides, saponins, and flavonoids in Astrag

YX-18-11-2024-2128
| Yaoxue Xuebao (ISSN:0513-4870)

Pharmacokinetics of wogonin-aloperine cocrystal in rats

Bexarotene (BEX), a specific retinoic acid X receptor (RXR) agonist granted by Food and Drug Administration (FDA) approval for the clinical treatment of T cell lymphoma, has now been found to exert pharmacological effects in the nervous system, with low bioavailability and poor cerebral distribution limiting its application in treatment on neurological disorders. Pharmaceutical co-crystal was a helpful method to improve the bioavailability and tissue distribution of active pharmaceutical ingredients (APIs). Here, 2bexarotene-ligustrazine (2BEX-LIG), a novel co-crystal system of BEX and ligu

YX-18-11-2024-2127
| Yaoxue Xuebao (ISSN:0513-4870)

Application progress of radiolabeling strategies in human mass balance studies

Human radiolabeled mass balance studies are an important component of the clinical pharmacology programs supporting the development of new investigational drugs. These studies allow for understanding of the absorption, distribution, metabolism, and excretion of the parent drug and metabolite(s) in the human body. Understanding the drug's disposition as well as metabolite profiling and abundance via mass balance studies can help inform the overall drug development program. A survey of the US Food and Drug Administration (FDA)‐approved new drug applications (NDAs) indicated that about 6

YX-18-11-2024-2126
| Yaoxue Xuebao (ISSN:0513-4870)

Advances of artificial intelligence technology in the discovery and optimization of lead compounds

Artificial intelligence (AI) encompasses a broad spectrum of techniques that have been utilized by pharmaceutical companies for decades, including machine learning, deep learning, and other advanced computational methods. These innovations have unlocked unprecedented opportunities for the acceleration of drug discovery and delivery, the optimization of treatment regimens, and the improvement of patient outcomes. AI is swiftly transforming the pharmaceutical industry, revolutionizing everything from drug development and discovery to personalized medicine, including target identification and

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Yaoxue Xuebao

Development of analgesic drugs targeting Nav1.7: advances in clinical trials and discovery of selective inhibitors

Exploration of the antioxidant role and mechanism of Astragalus membranaceus based on a glucose-induced Caenorhabditis elegans model

Pharmacokinetics of wogonin-aloperine cocrystal in rats

Application progress of radiolabeling strategies in human mass balance studies

Advances of artificial intelligence technology in the discovery and optimization of lead compounds

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