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.

A selective competitive antagonist of the tachykinin NK1 receptors

98%

Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.

Solid

L-732138

White or pale yellow solid

Soluble in ethanol (100 mM), ethyl acetate (50 mg/ml), water (partly), and DMSO (100 mM).

NK1