CELL: NTSR1 new regulator selectively reduces addictive behavior
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Last Update: 2020-05-29
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Source: Internet
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Author: User
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Small molecule neurotransmitter receptor 1 (NTSR1) agonist has been used as a potential treatment for mental illness, including drug addiction, for more than 40 yearsHowever, the clinical development of NTSR1 receptor agonists is hampered by its serious side effectsNTSR1 is a G-protein conjugate receptor (GPCR) that mediates different cellular signaling events by activating the classic signaling pathway of the G protein and binding to beta-arrestinshere, researchers have discovered an heterogeneous regulator of NTSR1, SBI-553This small molecule not only acts as a beta-arrestin-specific agonist, but also extends beta-arrestin preference to endogenous ligands through selectivean antagonistic G protein signal transductionSBI-553 showed efficacy in animal models of psychostimulant abuse, including self-administration of cocaine, and did not show the side effects specific to NTSR1's balanced agitationthese results suggest that NTSR1 G protein and beta-arrestin activation have discrete, isolated physiological effects, providing a more targeted strategy for developing safer GPCR targeted therapeutic drugs
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