Binding properties of C-truncated delta opioid receptors

Zhongguo Yao Li Xue Bao. 1997 Jul;18(4):337-40.

Abstract

Aim: To study the role of C-terminal delta opioid receptor involved in ligand binding affinity and selectivity.

Methods: The 31 amino acid residues of C-terminal truncated delta opioid receptors and the wild-type were expressed stably in Chinese hamster ovary (CHO) cells, respectively. Then the ligand binding properties of the products were studied by receptor binding assay.

Results: A typical mutated receptor clone CHO-T and a wild-type receptor clone CHO-W were obtained. The Kd values of [3H] diprenorphine (Dip) and [3H]leucine-2-alanine enkephalin (DADLE) bound to CHO-T were similar to CHO-W. Both the specific [3H]Dip bindings of CHO-T and CHO-W were strongly inhibited by delta selective agonists with similar Ki, but neither by mu nor kappa selective agonists.

Conclusion: The C-terminal of the delta opioid receptor is not involved in the ligands binding affinity and selectivity.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Binding Sites
  • CHO Cells / metabolism
  • Cricetinae
  • Diprenorphine / metabolism*
  • Enkephalin, Ala(2)-MePhe(4)-Gly(5)-
  • Enkephalin, D-Penicillamine (2,5)-
  • Enkephalin, Leucine / analogs & derivatives
  • Enkephalin, Leucine / pharmacology
  • Enkephalin, Leucine-2-Alanine / metabolism*
  • Enkephalins / pharmacology
  • Peptide Fragments / metabolism
  • Radioligand Assay
  • Receptors, Opioid, delta / agonists
  • Receptors, Opioid, delta / metabolism*
  • Receptors, Opioid, mu / agonists

Substances

  • Enkephalins
  • Peptide Fragments
  • Receptors, Opioid, delta
  • Receptors, Opioid, mu
  • Enkephalin, Ala(2)-MePhe(4)-Gly(5)-
  • Diprenorphine
  • Enkephalin, Leucine
  • Enkephalin, Leucine-2-Alanine
  • enkephalin, Ser(2), Leu(5), Thr(6)-
  • Enkephalin, D-Penicillamine (2,5)-