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Usage

Uses

Used in Pharmaceutical Industry:
CINNOLINE-3-CARBOXYLIC ACID is used as a reagent for the synthesis of TRPM8 antagonists, which are being developed for their potential therapeutic effects on cold-environment related pain. These antagonists may provide relief to individuals suffering from conditions that involve exposure to cold temperatures or are exacerbated by cold stimuli.

Upstream product

• 51073-57-5 cinnoline-3-carboxaldehyde 
• 17372-78-0 3-Methyl-cinnolin 

Downstream Products

• 1398584-10-5 C₂₆H₂₂FN₃O₃ 
• 1398582-88-1 3-({(cinnolin-3-ylcarbonyl)[(1R)-1-(4-fluorophenyl)ethyl]amino}methyl)benzoic acid 

Relevant academic research and scientific papers

Discovery of a selective TRPM8 antagonist with clinical efficacy in cold-related pain

The transient receptor potential (TRP) family of ion channels comprises nonselective cation channels that respond to a wide range of chemical and thermal stimuli. TRPM8, a member of the melastatin subfamily, is activated by cold temperatures (28 °C), and antagonists of this channel have the potential to treat cold induced allodynia and hyperalgesia. However, TRPM8 has also been implicated in mammalian thermoregulation and antagonists have the potential to induce hypothermia in patients. We report herein the identification and optimization of a series of TRPM8 antagonists that ultimately led to the discovery of PF-05105679. The clinical finding with this compound will be discussed, including both efficacy and its ability to affect thermoregulation processes in humans.

NON-PEPTIDYL, POTENT, AND SELECTIVE MU OPIOID RECEPTOR ANTAGONISTS

Selective, non-peptide antagonists of the ma opioid receptor { MOR) and methods of their use are provided. The antagonists may be used, for example, to identify MOR agonists in competitive binding assays, and to treat conditions related to addiction in which MOR is involved, e.g. heroin, prescription drug and alcohol addiction.