Affinity labeling of opioid receptors with enkephalin analogues

Borsodi A., ÖKTEM H. A., Benyhe S., Varga E., Moitra J., Takacs J.

The International Narcotics Research Conference, 8 - 13 July 1989, pp.171, (Full Text) identifier

  • Publication Type: Conference Paper / Full Text
  • Page Numbers: pp.171
  • Middle East Technical University Affiliated: Yes

Abstract

Chloromethyl ketone derivatives of enkephalins and Tyr-D-Ala-Gly(Me)Phe-Gly-ol (DAGO) were synthesized in normal and in tritiated form and were shown to react irreversibly at opioid receptors. Affinity of the chloromethyl ketone derivatives toward the μ site is greater than that of the parent compounds. It was shown in several studies (including autoradiography) with these ligands that the μ receptor protein contains only one type of binding subunit whose apparent M(r) is 58000.