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SR 48692

Chemical Structure : SR 48692

CAS No.: 146362-70-1

SR 48692 (Meclinertant;SR48692;SR-48692)

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

SR 48692 (Meclinertant) is a potent, selective and orally active nonpeptide antagonist of the neurotensin receptor with IC50 of 0.99 nM (guinea pig), without any intrinsic agonist activity.

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    Biological Activity

    SR 48692 (Meclinertant) is a potent, selective and orally active nonpeptide antagonist of the neurotensin receptor with IC50 of 0.99 nM (guinea pig), without any intrinsic agonist activity.
    SR 48692 (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.
    SR 48692 (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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