A κ-opioid receptor agonist
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GR89696 (fumarate)

Item No. 40145

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[2-(3,4-dichlorophenyl)acetyl]-3-(1-pyrrolidinylmethyl)-1-piperazinecarboxylic acid, methyl ester, (2E)-2-butenedioate
CAS Number
126766-32-3
Molecular Formula
C19H25Cl2N3O3 • C4H4O4
Formula Weight
530.4
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: SolubleMethanol: Soluble
SMILES
OC(/C=C/C(O)=O)=O.ClC(C=C1CC(N2C(CN(CC2)C(OC)=O)CN3CCCC3)=O)=C(C=C1)Cl
InChi Code
InChI=1S/C19H25Cl2N3O3.C4H4O4/c1-27-19(26)23-8-9-24(15(13-23)12-22-6-2-3-7-22)18(25)11-14-4-5-16(20)17(21)10-14;5-3(6)1-2-4(7)8/h4-5,10,15H,2-3,6-9,11-13H2,1H3;1-2H,(H,5,6)(H,7,8)/b;2-1+
InChi Key
ABTNETSDXZBJTE-WLHGVMLRSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $94

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    10 mg

    $179

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    25 mg

    $422

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    50 mg

    $748

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    Product Description

    GR89696 is a κ-opioid receptor agonist.1 It inhibits twitch responses in isolated mouse vas deferens (IC50 = 0.12 nM), an effect that can be reversed by the κ-opioid receptor antagonist norbinaltorphimine (nor-BNI). In vivo, GR89696 reduces acetylcholine-induced writhing in mice (ED50 = 0.0005 mg/kg). It reduces hippocampal neuronal loss in a gerbil model of cerebral ischemia induced by bilateral carotid artery occlusion when administered at doses of 10 and 30 mg/kg.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Hayes, A.G., Birch, P.J., Hayward, N.J., et al. A series of novel, highly potent and selective agonists for the κ-opioid receptor. Br. J. Pharmacol. 101(4), 944-948 (1990).

    2. Birch, P.J., Rogers, H., Hayes, A.G., et al. Neuroprotective actions of GR89696, a highly potent and selective κ-opioid receptor agonist. Br. J. Pharmacol. 103(3), 1819-1823 (1991).