RTI-118

RTI-118 is a novel small-molecule neuropeptide S receptor (NPSR) antagonist. RTI-118 can relieve drug addiction including selectively decrease cocaine self-administration[1].

Research Areas >> Neurological Disease

Signaling Pathways >> GPCR/G Protein >> Neuropeptide Y Receptor

RTI-118 (109 nM) has a reduction in antagonist potency at the NPS 107I variant[2].

RTI-118 (5-30 mg/kg, intraperitoneal injection; pre-30 minutes) is well tolerated in rats with no significant outward signs of aversion, sedation or toxicity, it also produces a dose-related decrease in cocaine and food self-administration; however these effects are selective for cocaine at lower doses (10 and 20 mg/kg)[1]. Animal Model: Rat[1] Dosage: 5 mg/kg; 10 mg/kg; 20 mg/kg; 30 mg/kg Administration: Intraperitoneal injection; pre-treatment 30 minutes; 5-30 mg/kg Result: The effects on the reinstatement of extinguished cocaine-seeking behavior are restricted to doses of 20 mg/kg or less.

[1]. Schmoutz CD, et al.Antagonism of the neuropeptide S receptor with RTI-118 decreases cocaine self-administration and cocaine-seeking behavior in rats.Pharmacol Biochem Behav. 2012 Dec;103(2):332-7.

[2]. Bonano JS,et al. Effects of the neuropeptide S receptor antagonist RTI-118