1-methyl-4-[[2-oxo-2-[4-(2-pyridinyl)-1-piperazinyl]ethyl]thio]-2-quinolinone

1-methyl-4-[[2-oxo-2-[4-(2-pyridinyl)-1-piperazinyl]ethyl]thio]-2-quinolinone, also known as **ML-10**, is a **potent and selective antagonist** of the **neurokinin-1 (NK1) receptor**.

**Here's why it's important for research:**

* **NK1 Receptor: ** This receptor plays a critical role in the central nervous system, mediating the actions of substance P, a neuropeptide involved in various physiological processes including pain perception, inflammation, anxiety, and emesis (vomiting).
* **Antagonist Function:** ML-10 blocks the binding of substance P to the NK1 receptor, effectively inhibiting its signaling pathway. This makes ML-10 a valuable tool for studying the role of the NK1 receptor in various conditions.
* **Therapeutic Potential:** ML-10 has shown promising results in preclinical studies for treating conditions like:
* **Migraine:** ML-10 effectively reduces migraine headache frequency and intensity.
* **Nausea and Vomiting:** It exhibits antiemetic properties, particularly in chemotherapy-induced nausea and vomiting.
* **Anxiety and Depression:** ML-10 has demonstrated potential for alleviating anxiety and depressive symptoms.
* **Pain:** Its ability to block substance P signaling suggests a role in pain management.

**Key Research Applications:**

* **Drug Discovery:** ML-10 serves as a lead compound for the development of new NK1 receptor antagonists with improved efficacy and safety profiles.
* **Mechanism of Action Studies:** Researchers use ML-10 to investigate the precise mechanisms underlying the role of the NK1 receptor in various physiological and pathological processes.
* **Preclinical Models:** ML-10 is used in animal models to study the therapeutic potential of NK1 receptor antagonism in different conditions.

**However, it's important to note that:**

* **ML-10 itself is not currently approved for clinical use.** Further research and clinical trials are needed to determine its safety and efficacy in humans.
* **There are other NK1 receptor antagonists currently in clinical use, like aprepitant.**

**In summary, 1-methyl-4-[[2-oxo-2-[4-(2-pyridinyl)-1-piperazinyl]ethyl]thio]-2-quinolinone (ML-10) is a valuable research tool with potential therapeutic implications for treating various conditions related to the NK1 receptor. Its antagonist activity offers insights into the role of substance P signaling and facilitates the development of novel drugs targeting this pathway.**