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SR48692

Chemical Structure : SR48692

CAS No.: 146362-70-1

SR48692 (Meclinertant, SR-48692)

Catalog No.: PC-60947Not For Human Use, Lab Use Only.

SR48692 (Meclinertant) is a potent, selective and orally active nonpeptide antagonist of neurotensin receptor NTSR1 with IC50 of 0.99 nM (guinea pig), without any intrinsic agonist activity.

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Biological Activity

SR48692 (Meclinertant) is a potent, selective and orally active nonpeptide antagonist of neurotensin receptor NTSR1 with IC50 of 0.99 nM (guinea pig), without any intrinsic agonist activity.
SR48692 (Meclinertant) blocks K(+)-evoked release of [3H]dopamine stimulated by neurotensin in guinea pig striatal slices with IC50 of 0.46 nM, competitively antagonizes neurotensin-induced intracellular Ca2+ mobilization with pA2 of 8.13 in H29 cells.
SR48692 (Meclinertant) reverses the turning behavior induced by intrastriatal injection of neurotensin in mice.

Physicochemical Properties

M.Wt 587.073
Formula C32H31ClN4O5
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(1r,3r,5r,7r)-2-(1-(7-chloroquinolin-4-yl)-5-(2,6-dimethoxyphenyl)-1H-pyrazole-3-carboxamido)adamantane-2-carboxylic acid

References

1. Dubuc I, et al. Br J Pharmacol. 1994 Jun;112(2):352-4.

2. Steinberg R, et al. Neuroscience. 1994 Apr;59(4):921-9.

3. Brouard A, et al. Eur J Pharmacol. 1994 Mar 3;253(3):289-91.

4. Gully D, et al. Proc Natl Acad Sci U S A. 1993 Jan 1;90(1):65-9.

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