L-732,138 is a selective nonpeptide tachykinin NK-1R (NK1) antagonist with 1000 fold more potency towards the NK-1R receptor over NK-2R (NK2) and NK-3R (NK3) receptors with an IC50= 2.3 nM. In addition, this compound shows a 200 fold selectivity towards human NK-1R receptors compared to rat NK-1R receptors. Studies suggest that L-732,138 reduces H3 induced skin vascular permeability. L-732,138 has been shown to competitively inhibit the binding of [125I]L-703,606 to the NK-1R receptor. Furthermore, it is known that if histidine 265 or histidine 197 are replaced with alanine on NK-1R receptors the affinity of L-732,138 is reduced.
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