SR 142948 TFA is an orally active, selective non-peptide neurotensin receptor (NT) antagonist, displaying IC50 values of 1.19 nM in h-NTR1-CHO cells, 0.32 nM in HT-29 cells, and 3.96 nM in adult rat brain. In HT-29 cells, it counteracts NT-induced inositol monophosphate formation with an IC50 of 3.9 nM. It blocks NT-induced hypothermia, analgesia, and turning behavior in vivo and can cross the blood-brain barrier, making it useful for research in psychiatric disorders.
Target-Kategorie:
Neurotensin Receptor
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