Home / Kappa Opioid Receptor Agonists / (±)-U-50488 hydrochloride

(±)-U-50488 hydrochloride

Catalog #: 0495
9 Citations Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
0495/25
(±)-U-50488 hydrochloride | CAS No. 67197-96-0 | Kappa Opioid Receptor Agonists
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Description: Selective κ agonist

Chemical Name: trans-(±)-3,4-Dichloro-N-methyl-N-[2-(1-pyrrolidinyl)cyclohexyl]benzeneacetamide hydrochloride

Purity: ≥99%

Product Details
Citations (9)
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Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

Biological Activity

(±)-U-50488 hydrochloride is a 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:
Store 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Other Product-Specific Information:

Background References

  1. Inhibition of tumor promoting signals by activation of SSTR2 and opioid receptors in human breast cancer cells.
    Kharmate G, Rajput P, Lin Y, Kumar U
    Cancer Cell Int, 2013;13(1):93.
  2. Development of functionally selective, small molecule agonists at kappa opioid receptors.
    Zhou L, Lovell K, Frankowski K, Slauson S, Phillips A, Streicher J, Stahl E, Schmid C, Hodder P, Madoux F, Cameron M, Prisinzano T, Aube J, Bohn L
    J Biol Chem, 2013;288(51):36703-16.
  3. High-throughput genotoxicity assay identifies antioxidants as inducers of DNA damage response and cell death.
    Fox JT, Sakamuru S, Huang R
    Proc. Natl. Acad. Sci. U.S.A., 2012;109(14):5423-8.
  4. 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
  5. U-50,488 blocks the development of mor. tolerance and dependence at a very low dose in guinea pigs.
    Pao-Luh Tao et al.
    Eur.J.Pharmacol., 1994;256:281
  6. Activation of kappa opioid receptors by U-50488H and mor. enhances the release of substance P from rat trigeminal nucleus slices.
    Suarez-Roca and Maixner
    J.Pharmacol.Exp.Ther., 1993;264:648
  7. Blockade of the development of mor. 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

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Citations for (±)-U-50488 hydrochloride

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

9 Citations: Showing 1 - 9

  1. Kappa-opioid receptor-dependent changes in dopamine and anxiety-like or approach-avoidance behavior occur differentially across the nucleus accumbens shell rostro-caudal axis
    Authors: Pirino Et al.
    Neuropharmacology  2020;181:108341
  2. Kappa opioid receptor agonists improve postoperative cognitive dysfunction in rats via the JAK2/STAT3 signaling pathway.
    Authors: Li Et al.
    Int J Mol Med  2019;
  3. sMu opioid receptor agonist DAMGO produces place conditioning, abstinence-induced withdrawal, and naltrexone-dependent locomotor activation in planarians.
    Authors: Dziedowiec Et al.
    Neuroscience  2018;386:214
  4. In vivo brain GPCR signaling elucidated by phosphoproteomics.
    Authors: Liu
    Science  2018;360(6395):eaao4927
  5. Constitutive activation of kappa opioid receptors at ventral tegmental area inhibitory synapsesfollowing acute stress
    Authors: Polter
    Elife  2017;6:e23785
  6. Development of functionally selective, small molecule agonists at kappa opioid receptors.
    Authors: Zhou Et al.
    J Biol Chem  2013;288:36703
  7. 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
  8. GPR54-dependent stimulation of luteinizing hormone secretion by neurokinin B in prepubertal rats.
    Authors: Grachev Et al.
    Pain  2012;7:e44344
  9. Medial dorsal hypothalamus mediates the inhibition of reward seeking after extinction.
    Authors: Marchant Et al.
    J Neurosci  2010;30:14102

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