SDZ NKT 343 is a potent human NK1 tachykinin receptor antagonist.
Highly selective human tachykinin NK 1 receptor antagonist (IC 50 values are 0.62 and 451 nM for human and rat receptors respectively) that displays > 130-fold selectivity over human NK 2 and NK 3 receptors. Potently antagonizes SP-induced Ca 2+ efflux in vitro and inhibits mechanical hyperalgesia in vivo .
SDZ NKT 343 antagonized [Sar9]SP sulphone-evoked bronchoconstriction (70% reduction at 0.4 mg/kg, i.v.) in anaesthetized guinea-pigs[1].
hNK1: 0.62 nM (IC50); hNK2: 0.52 μM (Ki); hNK3: 3.4 μM (Ki)