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Biological Activity:
Potent and selective antagonist of transient receptor potential vanilloid 1 (TRPV1) receptors (IC50 values to be 5-7 nM) under clinical trials; TRPV1 receptor antagonism is a promising approach for pain management.
References:
CS Surowy et al. (R)-(5-tert-Butyl-2,3-dihydro-1H-inden-1-yl)-3-(1H-indazol-4-yl)-urea (ABT-102) Blocks Polymodal Activation of Transient Receptor Potential Vanilloid 1 Receptors in Vitro and Heat-Evoked Firing of Spinal Dorsal Horn Neurons in Vivo. JPET 2008, 326(3), 879-888. [online]
P Honore et al. Repeated dosing of ABT-102, a potent and selective TRPV1 antagonist, enhances TRPV1-mediated analgesic activity in rodents, but attenuates antagonist-induced hyperthermia. Pain. 2009, 142(1-2), 27-35. [online]
Chemical Name: (R)-(5-tert-Butyl-2,3-dihydro-1H-inden-1-yl)-3-(1H-indazol-4-yl)-urea
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