1159996-20-9

Usage

Uses

Used in Pharmaceutical Industry:
TC-I 2000 is used as a potent and orally available transient receptor melastatin type 8 (TRPM8) antagonist. TRPM8 is a calcium-permeable ion channel that is activated by cold temperatures and certain chemical stimuli. By blocking the activity of TRPM8, TC-I 2000 can potentially be used to treat a variety of conditions, such as pain, inflammation, and certain types of cancer.
Used in Pain Management:
TC-I 2000 is used as a pain management agent, particularly for neuropathic and inflammatory pain conditions. By inhibiting TRPM8, it can help reduce pain signals and provide relief to patients suffering from chronic pain.
Used in Cancer Treatment:
TC-I 2000 is used as a potential cancer treatment agent. The inhibition of TRPM8 has been shown to have anti-proliferative and pro-apoptotic effects on certain cancer cells. By targeting TRPM8, TC-I 2000 may help to slow down tumor growth and induce cell death in cancerous cells.
Used in Drug Development:
TC-I 2000 is used as a lead compound in drug development for the discovery of new therapeutic agents targeting TRPM8. Its potent antagonistic activity and oral availability make it a promising candidate for further research and development in the pharmaceutical industry.

Upstream product

• 329-15-7 4-trifluoromethyl-phenyl acetyl chloride 
• 64-04-0 phenethylamine 
• 38925-76-7 N-phenethyl-4-(trifluoromethyl)benzamide 
• 757880-98-1 1-(4-(trifluoromethyl)phenyl)-1,2,3,4-tetrahydroisoquinoline 
• 1195-45-5 para-fluorophenyl isocyanate 
• 1159997-91-7 1-(4-(trifluoromethyl)phenyl)-3,4-dihydroisoquinoline 

Downstream Products

• 1159996-43-6 (R)-N-(4-fluorophenyl)-1-(4-(trifluoromethyl)phenyl)-3,4-dihydroisoquinoline-2(1H)-carboxamide 

Relevant academic research and scientific papers

Fused piperidines as a novel class of potent and orally available transient receptor potential melastatin type 8 (TRPM8) antagonists

The transient receptor potential melastatin type 8 (TRPM8) is a nonselective cation channel primarily expressed in a subpopulation of sensory neurons that can be activated by a wide range of stimuli, including menthol, icilin, and cold temperatures (25 °C). Antagonism of TRPM8 is currently under investigation as a new approach for the treatment of pain. As a result of our screening efforts, we identified tetrahydrothienopyridine 4 as an inhibitor of icilin-induced calcium influx in CHO cells expressing recombinant rat TRPM8. Exploration of the structure-activity relationships of 4 led to the identification of a potent and orally bioavailable TRPM8 antagonist, tetrahydroisoquinoline 87. Compound 87 demonstrated target coverage in vivo after oral administration in a rat pharmacodynamic model measuring the prevention of icilin-induced wet-dog shakes (WDS).

TRP-M8 RECEPTOR LIGANDS AND THEIR USE IN TREATMENTS

Tetrahydroisoquinoline compounds of formula (I), and compositions containing them, for the treatment of acute, inflammatory and neurophatic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neurophatic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintened pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, duodenal ulcers, diarrhea, gastric lesions induced by necrotising agents, hair growth, vasomotor or allergic rhinitis, bronchial disorders or bladder disorders.