An adamantane-based ligand as a novel chemical tool for thermosensory TRPM8 channel therapeutic modulation.

ABSTRACT: Transient receptor potential cation channel subfamily M member 8 (TRPM8) is a nonselective thermosensory cation channel expressed in peripheral nociceptor terminals where it transduces cold temperatures and cooling agents such as menthol. TRPM8 dysfunction has been involved in disabling sensory symptoms, such as cold allodynia. In addition, its widespread expression has signaled this channel as a pivotal therapeutic target for a variety of diseases, from peripheral neuropathies to cancer. Thus, the design and therapeutic validation of TRPM8 antagonists is an important endeavor in biomedicine. To address this, we used the multicomponent Passerini and Ugi reactions to design a novel family of TRPM8 modulators using as a scaffold the adamantane ring that exhibits drug-like qualities. These gr

SUBMITTER: Lamberti A 

PROVIDER: S-EPMC12220852 | biostudies-literature | 2025 Jul

REPOSITORIES: biostudies-literature