SR 142948
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SR 142948
Description :
SR 142948 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 antagonizes NT-induced inositol monophosphate formation in HT-29 cells with an IC50 of 3.9 nM. SR 142948 blocks hypothermia, analgesia and steering behavior induced by NT in vivo. SR 142948 shows blood-brain permeability and can be used in study of psychiatric disorders[1][2].UNSPSC :
12352005Target :
Neurotensin ReceptorType :
Reference compoundRelated Pathways :
GPCR/G Protein; Neuronal SignalingApplications :
Neuroscience-NeuromodulationField of Research :
Neurological DiseaseAssay Protocol :
https://www.medchemexpress.com/sr-142948.htmlPurity :
99.16Solubility :
DMSO : 100 mg/mL (ultrasonic)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)=OMolecular Formula :
C39H51N5O6Molecular Weight :
685.85References & 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 TemperatureStorage Conditions :
-20°C, 3 years; 4°C, 2 years (Powder)Scientific Category :
Reference compound1Clinical Information :
No Development ReportedCAS Number :
[184162-64-9]
