L-733,060

L-733,060 is a drug developed by Merck which acts as an orally active, non-peptide, selective antagonist for the NK1 receptor, binding with a Ki of 0.08 nM.

[1] Only one enantiomer is active which has made it the subject of several asymmetric synthesis efforts.

[2][3][4] L-733,060 has antidepressant[5][6] and anxiolytic effects in animal studies,[7] and reduces both the dopamine release and neurotoxicity produced by methamphetamine and cocaine.

[8][9][10][11][12] It shows anti-inflammatory and anti-hepatotoxic effects in animals,[13][14] and counteracts the development of hyperalgesia following nerve injury.

[15][16] It also has anticancer effects in a variety of in vitro models.