ML-314

ML-314 is a neurotensin-1 receptor (NTS₁) agonist.^1,2 It is selective for NTS₁ over NTS₂ in a cell-based assay of receptor/β-arrestin complex formation (EC₅₀s = 2 and >80 μM, respectively) but is inactive in an NTS₁ calcium flux assay (EC₅₀ = >80 μM) indicating that, in contrast to other NTS₁ agonists, it does not signal through the traditional G_q-coupled pathway.² ML-314 is also a positive allosteric modulator of NTS₁ that increases binding of radiolabeled neurotensin (Item No. 24717) to NTS₁ in a concentration-dependent manner.¹ It reduces locomotion in dopamine transporter knockout mice and methamphetamine-exposed mice when administered at doses of 20 and 10 to 30 mg/kg, respectively.¹ ML-314 (30 mg/kg) also reduces methamphetamine self-administration in rats.

WARNING This product is not for human or veterinary use.

1. Barak, L.S., Bai, Y., Peterson, S., et al. ML314: A biased neurotensin receptor ligand for methamphetamine abuse. ACS Chem Biol. 11(7), 1880-1890 (2016).

2. Peddibhotla, S., Hedrick, M.P., Hershberger, P.A., et al. Discovery of ML314, a brain penetrant non-peptidic β-arrestin biased agonist of the neurotensin NTR1 receptor. ACS Med. Chem. Lett. 4(9), 846-851 (2013).