ML314

ML314 is a potent, BBB-penetrant and β-arrestin biased molecule agonist of NTR1 (EC₅₀ = 1.9 μM). ML314 shows good selectivity against NTR2 and GPR35, but does not stimulate Ca2+ mobilization. ML314 can attenuate amphetamine-like hyperlocomotion in dopamine transporter knockout mice. ML314 attenuates methamphetamine-associated hyperlocomotion and potentiates the psychostimulant inhibitory effects of a ghrelin antagonist in wild type mouse model. ML314 also acts as an allosteric enhancer of endogenous neurotensin. ML314 antagonizes G protein signaling. ML314 can be studied in research for methamphetamine abuse conditions^[1][2]. In Vitro:ML314 (10 μM) induces aggregation of β-arrestin in NTR1β-arrestin2/GFP containing U2OS cells^[2].
ML314 (10 μM, 10 min) antagonizes G protein signaling in HEK293 cells expressing NTR1^[2].
ML314 (2 μM) increases the number of NTR1 binding in U2OS cells^[2]. In Vivo:ML314 (20 mg/kg, i.p., single dose) reduces locomotion in Dopamine Transporter knock-out mice^[2].
ML314 (10-30 mg/kg, i.p., single dose) reduces hyperlocomotion and conditioned place preference in C57BL/6J mice exposed to Methamphetamine^[2].