Characterization of human placental opioid receptors by 3H-ethylketocyclazocine and 3H-naloxone binding

A. Agbas, J. Simon, H. Avni Öktem, E. Varga, A. Borsodi

Research output: Contribution to journalArticle

5 Citations (Scopus)

Abstract

The human placenta contains membrane bound opioid receptors. The binding of the antagonist naloxone and the fairly kappa-selective agonist EKC were studied in the microvillous membrane fraction. In both cases high affinity binding sites were detected with Kd values in the nanomolar range. A series of kappa-selective ligand (PD-117302, EKC, and U-50, 488H) were tested in displacement experiments, and found to be potent inhibitors of agonist and antagonist binding. It was confirmed that large percentage of the binding is associated with the kappa sub-type which is of current interest, in that it shows distictive pharmacology and distribution and is selective for the natural opioid polypeptide, dynorphin.

Original languageEnglish
Pages (from-to)171-176
Number of pages6
JournalNeuropeptides
Volume12
Issue number3
DOIs
Publication statusPublished - 1988

Fingerprint

Ethylketocyclazocine
Opioid Receptors
Naloxone
(trans)-Isomer 3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide
Membranes
Dynorphins
Placenta
Opioid Analgesics
Binding Sites
Pharmacology
Ligands
Peptides
Experiments

ASJC Scopus subject areas

  • Biochemistry
  • Endocrinology
  • Endocrinology, Diabetes and Metabolism
  • Clinical Neurology
  • Neuroscience(all)
  • Cellular and Molecular Neuroscience

Cite this

Characterization of human placental opioid receptors by 3H-ethylketocyclazocine and 3H-naloxone binding. / Agbas, A.; Simon, J.; Öktem, H. Avni; Varga, E.; Borsodi, A.

In: Neuropeptides, Vol. 12, No. 3, 1988, p. 171-176.

Research output: Contribution to journalArticle

Agbas, A. ; Simon, J. ; Öktem, H. Avni ; Varga, E. ; Borsodi, A. / Characterization of human placental opioid receptors by 3H-ethylketocyclazocine and 3H-naloxone binding. In: Neuropeptides. 1988 ; Vol. 12, No. 3. pp. 171-176.
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