Catalog Number: 0495
Chemical Name: trans-(±)-3,4-Dichloro-N-methyl-N-[2-(1-pyrrolidinyl)cyclohexyl]benzeneacetamide hydrochloride
Biological Activity
Selective κ-opioid agonist. At higher concentrations blocks Na+ channels.

(-)-enantiomer and (+)-enantiomer also available.

Technical Data
  • M.Wt:
    405.79
  • Formula:
    C19H26Cl2N2O.HCl
  • Solubility:
    Soluble to 25 mM in water
  • Purity:
    >99%
  • Storage:
    Desiccate at RT
  • CAS No:
    67197-96-0
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Additional Information
Other Product-Specific Information:
Background References
  1. U-50,488 blocks the development of morphine tolerance and dependence at a very low dose in guinea pigs.
    Pao-Luh Tao et al.
    Eur.J.Pharmacol., 1994;256:281
  2. Activation of kappa opioid receptors by U-50488H and morphine enhances the release of substance P from rat trigeminal nucleus slices.
    Suarez-Roca and Maixner
    J.Pharmacol.Exp.Ther., 1993;264:648
  3. Cardiovascular actions of the κ-agonist, U-50-488H, in the absence and presence of opioid receptor blockade.
    Pugsley et al.
    Br.J.Pharmacol., 1992;105:521
  4. Blockade of the development of morphine tolerance by U-50,488, an AVP antagonist or MK 801 in the rat hippocampal slice.
    Su et al.
    Br.J.Pharmacol., 1998;123:625
Citations:

The citations listed below are publications that use Tocris products. Selected citations for (±)-U-50488 hydrochloride include:

4 Citations: Showing 1 - 4
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  1. Constitutive activation of kappa opioid receptors at ventral tegmental area inhibitory synapsesfollowing acute stress
    Authors: Polter
    Elife 2017;6:e23785
  2. Development of functionally selective, small molecule agonists at kappa opioid receptors.
    Authors: Zhou Et al.
    J Biol Chem 2013;288:36703
  3. Inhibition of tumor promoting signals by activation of SSTR2 and opioid receptors in human breast cancer cells.
    Authors: Kharmate Et al.
    Cancer Cell Int 2013;13:93
  4. GPR54-dependent stimulation of luteinizing hormone secretion by neurokinin B in prepubertal rats.
    Authors: Grachev Et al.
    Pain 2012;7:e44344
Tocris Small Molecules
Description Application Cat# Citations Images  

(-)-U-50488 hydrochloride

0496  
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