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  • Title: [125I]azido-DTLET as a tool for selective covalent labeling of delta-opioid receptors in rat brain sections.
    Author: Pasquini F, Jomary C, Garbay-Jaureguiberry C, Roques BP, Beaudet A.
    Journal: Eur J Pharmacol; 1993 Oct 12; 243(1):39-45. PubMed ID: 8253123.
    Abstract:
    The binding kinetics and pharmacological selectivity of the photoaffinity delta-opioid ligand [125I]azido-DTLET (Tyr-D-Thr-Gly-Phe(pN3)-Leu-Thr) were investigated in serial frozen sections from rat neostriatum prior to ultraviolet irradiation (i.e., in conditions of reversibility). Scatchard analysis of saturation binding experiments indicated that [125I]azido-DTLET binds to both a high (KD = 5.04 nM) and a low (KD = 38 nM) affinity site. Binding to the low-affinity site was no longer detectable in the presence of unlabeled [D-Ala2,N-MePhe4,Gly-Ol5]enkephalin (DAGO), suggesting that this site corresponds to mu-opioid receptors. This interpretation was further supported by the dose-dependent inhibition of the binding of [3H]DAGO by non-radioactive azido-DTLET. Binding to the high-affinity site was totally inhibited, in a dose-dependent fashion, by a variety of opioid drugs among which delta-opioid ligands showed the highest order of potency. It is concluded that, in the nanomolar range, [125I]azido-DTLET constitutes a highly selective tool for covalent labeling of delta-opioid receptors in rat brain sections.
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