产品描述:
ML-314 is a neurotensin-1 receptor (NTS1) agonist.{43308,43309} 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 Gq-coupled pathway.{43309} 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.{43308} 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.{43308} ML-314 (30 mg/kg) also reduces methamphetamine self-administration in rats.