SR 142948 (dihydrochloride)

SR 142948 dihydrochloride 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 dihydrochloride antagonizes NT-induced inositol monophosphate formation in HT-29 cells with an IC50 of 3.9 nM. SR 142948 dihydrochloride blocks hypothermia, analgesia and steering behavior induced by NT in vivo. SR 142948 dihydrochloride shows blood-brain permeability and can be used in study of psychiatric disorders[1][2].

Product Specifications

UNSPSC

12352005

Target

Neurotensin Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/sr-142948-dihydrochloride.html

Purity

99.07

Solubility

DMSO : ≥ 100 mg/mL

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.[H]Cl.[H]Cl

Molecular Formula

C39H53Cl2N5O6

Molecular Weight

758.77

References & Citations

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