Cayman mL-314

mL-314 is a neurotensin-1 receptor (NTS₁) agonist.^, 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. mL-314 is also a positive allosteric modulator of NTS₁ that increases binding of radiolabeled neurotensin (Item No. ) to NTS₁ in a concentration-dependent manner. 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. mL-314 (30 mg/kg) also reduces methamphetamine self-administration in rats.

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