Formulation: A crystalline solid
Formal Name: 2-[[[5-(2,6-dimethoxyphenyl)-1-[4-[[[3-(dimethylamino)propyl]methylamino]carbonyl]-2-(1-methylethyl)phenyl]-1H-pyrazol-3-yl]carbonyl]amino]-tricyclo[3.3.1.13,7]decane-2-carboxylic acid, dihydrochloride
Purity: ≥98%
Formula Markup: C39H51N5O6 • 2HCl
Formula Weight: 758,8
Shelf life (days): 1460
Notes: SR 142948 is an orally bioavailable non-peptide antagonist of neurotensin receptors (NTS; IC50s = 1.19, 0.32, and 3.96 nM for human recombinant NTS receptors expressed in CHO cells, HT-29 cells, and adult rat brain membranes, respectively).{41672} It inhibits inositol phosphate formation in HT-29 cells (IC50 = 3.9 nM) and intracellular calcium accumulation in CHO cells expressing human NTS receptors. SR 142948 (1 mg/kg, i.v.) inhibits the firing rate of rat ventral pallidum neurons with a longer duration of action than the NTS receptor antagonist SR 48692 (Item No. 20124).{41673} It also inhibits neurotensin-induced behavioral responses, including inhibition of neurotensin-induced turning behavior in mice when administered at doses ranging from 40 to 640 mg/kg and hypothermia and analgesia in rats and mice.{41672}