Elinzanetant CAS# 929046-33-3

Elinzanetant is a potent, dual antagonist of the neurokinin-1 (NK-1) and neurokinin-3 (NK-3) receptors, with Kᵢ values reported at ~0.37 nM for NK-1 and ~3.0 nM for NK-3. In vitro studies show it binds and functionally blocks NK-1/3 receptor activity and is >100-fold selective against most non-tachykinin targets. In vivo (animal/occupancy) work includes gerbil and guinea-pig models demonstrating brain penetration and sustained receptor occupancy of NK-1 and NK-3 after oral dosing; for example, brain receptor occupancy in vivo was dose- and exposure-dependent.