Nolpitantium (SR140333) is a potent, selective, non-peptide NK1 receptor antagonist with Ki of 0.74 nM, IC50 of 1.6 nM.
Nolpitantium (SR140333) shows no effect in bioassays for NK2 and NK3 receptors.
Nolpitantium (SR140333) blocks substance P-induced release of acetylcholine from rat striatum, exerts highly potent antagonism toward substance P-induced hypotension in vivo.
Nolpitantium (SR140333) also blocks the activation of rat thalamic neurons after nociceptive stimulation.
