N-[(1S)-5-tert-butyl-2,3-dihydro-1H-inden-1-yl]-N'-1H-indazol-4-ylurea is a potent TRPV1 antagonist, blocking activation of TRPV1 by capsaicin with the IC50 of 123 nM.

MDR-652 is a highly specific and efficacious agonist of nonpungent transient receptor potential vanilloid 1 (TRPV1) with Ki value of 11.4 nM and 23.8 nM for hTRPV1 and rTRPV1 respectively and EC50s for hTRPV1 and rTRPV1 are 5.05 and 93 nM respectively.

Elismetrep (MT-8554) is an orally available TRPM8 inhibitor with potential analgesic activity for the study of vasomotor symptoms in postmenopausal women.