2. Academic Validation
  3. [3H]U-69593 a highly selective ligand for the opioid kappa receptor

[3H]U-69593 a highly selective ligand for the opioid kappa receptor

  • Eur J Pharmacol. 1985 Feb 26;109(2):281-4. doi: 10.1016/0014-2999(85)90431-5.
R A Lahti,  M M Mickelson,  J M McCall,  P F Von Voigtlander
PMID: 2986999 DOI: 10.1016/0014-2999(85)90431-5
Abstract

The selective kappa agonist U-50488 was recently discovered and characterized. In this study, the receptor binding properties of [3H]U-69593, an analog of U-50488, were characterized. [3H]U-69593 binds with high affinity (3 nM) to membranes prepared from guinea pig, mouse and rat brain. The number of kappa binding sites comprise only 13%, 9% and 4% of the total opioid sites, respectively. The benzmorphans, dynorphin, and compounds structurally related to U-50488 have high affinity for this kappa site.

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