SR 142948 TFA 

SR 142948 TFA is an orally active and selective non-peptide neurotensin receptor (NT) antagonist with IC₅₀s of 1.19 nM, 0.32 nM, 3.96 nM in h-NTR1-CHO cells, HT-29 cells, and adult rat brain, respectively. SR 142948 TFA antagonizes NT-induced inositol monophosphate formation in HT-29 cells with an IC₅₀ of 3.9 nM. SR 142948 TFA blocks hypothermia, analgesia and steering behavior induced by NT in vivo. SR 142948 TFA shows blood-brain permeability and can be used in study of psychiatric disorders^[1][2].

SR 142948 (1 µM; 90 min) TFA inhibits expression of c-fos and krox24 in CHO-hNT1-R cells^[1].
SR 142948 (0-1 µM; 1 h) TFA exhibits good antagonistic activity by inhibiting [¹²⁵I-Tyr³]NT binds to h-NTR1-CHO and HT 29 cell membranes, with IC₅₀s of 1.19 and 0.32 nM, respectively^[2].
SR 142948 (0-1 µM; 30 min) TFA antagonizes production of IP1 stimulated by NT both in h-NTR1-CHO and HT 29 cells, in a concentration-dependent manner^[2].
SR 142948 (1, 10 nM; 60-80 s) TFA antagonizes intracellular calcium mobilization stimulated by NT in h-NTR1-CHO cells^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

SR 142948 (2 µg/kg; p.o.; single) TFA inhibits the turning behavior induced by NT (10 pg/mouse)^[2].
SR 142948 (0.01, 0.03, 0.3 mg/kg; i.p.; single) TFA prevents the enhancement of ACh release produced by NT (100 nM), in a dose-dependent manner^[2].
SR 142948 (0-10 mg/kg; p.o.; single) TFA partially but significantly blocks NT-induced hypothermia (53% at 2 mg/kg in rats and 54% at 4 mg/kg in mice)^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

799.88

C₄₁H₅₂F₃N₅O₈

O=C(C1=NN(C2=C(C=C(C(N(C)CCCN(C)C)=O)C=C2)C(C)C)C(C3=C(C=CC=C3OC)OC)=C1)NC4([C@H]5C[C@H](C6)C[C@@H]4C[C@H]6C5)C(O)=O.FC(C(O)=O)(F)F

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Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Portier M, et al. Neurotensin type 1 receptor-mediated activation of krox24, c-fos and Elk-1: preventing effect of the neurotensin antagonists SR 48692 and SR 142948. FEBS Lett. 1998 Jul 31;432(1-2):88-93.  [Content Brief]

  [2]. Gully D, et al. Biochemical and pharmacological activities of SR 142948A, a new potent neurotensin receptor antagonist. J Pharmacol Exp Ther. 1997 Feb;280(2):802-12.  [Content Brief]