R116031 is a selective Neurokinin-1 (NK-1) receptor antagonist, demonstrating a Ki value of 0.45 nM against the human NK-1 receptor. This compound effectively inhibits Substance P-induced peripheral responses, such as skin reactions and plasma extravasation in guinea pig models, as well as central effects demonstrated in gerbils. Additionally, R116031, when labeled with 3H, shows significant accumulation in brain regions including the striatum, olfactory tubercle, olfactory bulb, and locus coeruleus, making it suitable for use as a PET ligand in imaging studies.
R116031 is a selective Neurokinin-1 (NK-1) receptor antagonist, demonstrating a Ki value of 0.45 nM against the human NK-1 receptor. This compound effectively inhibits Substance P-induced peripheral responses, such as skin reactions and plasma extravasation in guinea pig models, as well as central effects demonstrated in gerbils. Additionally, R116031, when labeled with 3H, shows significant accumulation in brain regions including the striatum, olfactory tubercle, olfactory bulb, and locus coeruleus, making it suitable for use as a PET ligand in imaging studies.
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