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SR142948 hydrochloride

Chemical Structure : SR142948 hydrochloride

CAS No.: 184162-21-8

SR142948 hydrochloride (SR142948A )

Catalog No.: PC-20497Not For Human Use, Lab Use Only.

SR142948 hydrochloride is a potent, selective and orally active neurotensin receptor antagonist with IC50 of 1.19 nM.

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    Biological Activity

    SR142948 hydrochloride (SR142948A ) is a potent, selective and orally active neurotensin receptor antagonist with IC50 of 1.19 nM.
    SR142948 antagonizes neurotensin-induced inositol monophosphate formation in HT 29 cells with IC50 of 3.9 nM.
    SR142948 inhibits the turning behavior induced by neurotensin in mice, completely antagonizes neurotensin-evoked acetylcholine release in the rat striatum at 0.1 mg/kg.
    SR142948 also blocks both hypothermia and analgesia induced by i.c.v. injection of neurotensin injection into the ventral tegmental area.

    Physicochemical Properties

    M.Wt 722.32
    Formula C39H52ClN5O6
    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

    O=C(C1(NC(C2=NN(C3=CC=C(C(N(CCCN(C)C)C)=O)C=C3C(C)C)C(C4=C(OC)C=CC=C4OC)=C2)=O)C(C5)CC6CC5CC1C6)O.[H]Cl

    References

    1. Gully D, et al. J Pharmacol Exp Ther. 1997 Feb;280(2):802-12.

    2. Betancur C, et al. Eur J Pharmacol. 1998 Feb 5;343(1):67-77.

    3. Schaeffer P, et al. J Cardiovasc Pharmacol. 1998 Apr;31(4):545-50.

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