L-733,060

L-733,060 is a potent, selective, non-peptide antagonist of the neurokinin 1 (NK1) receptor. Developed by Merck, it is orally bioavailable and brain penetrant. The compound exhibits high affinity for the NK1 receptor (Ki values of 0.08 nM in gerbil and 0.2 nM in human receptors), with much lower affinity in rats[1][3][5]. Only one enantiomer is active. In preclinical studies, L-733,060 has demonstrated anxiolytic-like and antidepressant effects in animal models[3], as well as antitumor activity both in vitro and in vivo by decreasing HER2 activity and tumor growth in breast cancer models[1][2]. It also shows anti-inflammatory effects and can counteract hyperalgesia following nerve injury[3]. Additionally, it has been studied for its ability to reduce neurological damage after traumatic brain injury by inhibiting substance P signaling through NK1R antagonism[7].

Other names

L-733,060 hydrochloride