SR 142948 (TFA)

• Description :

  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].

• UNSPSC :

  12352005

• Target :

  Neurotensin Receptor

• Related Pathways :

  GPCR/G Protein; Neuronal Signaling

• Applications :

  Neuroscience-Neuromodulation

• Field of Research :

  Neurological Disease

• Smiles :

  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

• Molecular Formula :

  C41H52F3N5O8

• Molecular Weight :

  799.88

• References & Citations :

  [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.|[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.

• Shipping Conditions :

  Room temperature

• Scientific Category :

  Reference compound1

• Clinical Information :

  No Development Reported