SBI-553 is a potent, brain-penetrant and allosteric modulator of NTR1 with EC50 of 0.34 μM.
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Neurotensin receptor 1 (NTSR1) is a G-protein-coupled receptor (GPCR) that engages multiple subtypes of G protein, and is involved in the regulation of blood pressure, body temperature, weight and the response to pain[1].SBI-553 not only acts as a β-arrestin-biased agonist but also extends profound β-arrestin bias to the endogenous ligand by selectively antagonizing G protein signaling. SBI-553 shows efficacy in animal models of psychostimulant abuse, including cocaine self-administration, without the side effects characteristic of balanced NTSR1 agonism. SBI-553 administration (12 mg/kg, i.p.) to attenuate cocaine-induced hyperlocomotion relative to the vehicle control (saline, 5 ml/kg, i.p.) (Fig 5A,B). By contrast, responses to the vehicle and SBI-553 were comparable in non-stimulant exposed animals. This SBI-553 dose also reduced methamphetamine (2 mg/kg) -induced hyperlocomotion and blocked the expression of methamphetamine conditioned place preference.[2]. SBI-553 increases NTS binding affinity and Bmax,, and its binding affinity is reciprocally increased by NTS. These behaviors are characteristic of positive allosteric modulation and are concordant with the Monod-Wyman-Changeux model of allosteric transitions[3].
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