Formulation: A solid
Formal Name: 2-[[2-(1-fluorocyclopropyl)-4-[4-(2-methoxyphenyl)-1-piperidinyl]-6-quinazolinyl]methylamino]-ethanol
Purity: ≥98%
Formula Markup: C26H31FN4O2
Formula Weight: 450,6
Shelf life (days): 1460
CAS Number: 1849603-72-0
Notes: SBI-553 is a β-arrestin-biased positive allosteric modulator (PAM) of neurotensin receptor 1 (NTSR1).{62828} It binds to NSTR1 and increases neurotensin-1 affinity for NSTR1 in HEK293 cells expressing the human receptor when used at concentrations ranging from 0.01 to 10 µM. SBI-553 (0.03-30 µM) induces β-arrestin recruitment and NTSR1 internalization without stimulating Gq protein activation, 1,4,5-triphosphate (IP3) generation, or calcium mobilization in cell-based assays. In vivo, SBI-553 (12 mg/kg, i.p.) attenuates cocaine- or methamphetamine-induced hyperlocomotion in wild-type but not β-arrestin-2 knockout mice. It also reduces cocaine self-administration in mice.
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