Synthesis and binding characteristics of the highly delta-specific new tritiated opioid peptide, [3H] deltorphin II

B. Búzás; G. Tóth; S. Cavagnero; V. J. Hruby; A. Borsodi

doi:10.1016/0024-3205(92)90103-V

Synthesis and binding characteristics of the highly delta-specific new tritiated opioid peptide, [³H] deltorphin II

B. Búzás, G. Tóth, S. Cavagnero, V. J. Hruby, A. Borsodi

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29 Scopus citations

Abstract

A radiolabelled form of deltorphin II was synthesized by catalytic tritiation using [p-IPhe³]-deltorphin II as a precursor. The ligand labels rat brain membranes with a K_d value of 1.9 nM, and the B_max was found to be 92 fmol/mg protein. This new tritiated ligand exhibits high affinity for the delta opioid binding site, whereas its binding to the mu type is weak and extremely low for the kappa type. Mu/delta and kappa/delta selectivity ratios were about 900 and 10000, respectively. The highly delta selective binding properties of this new radioligand suggest that it could serve as an excellent tool for investigating the delta opioid receptors in various species.

Original language	English (US)
Pages (from-to)	PL75-PL78
Journal	Life Sciences
Volume	50
Issue number	14
DOIs	https://doi.org/10.1016/0024-3205(92)90103-V
State	Published - 1992
Externally published	Yes

ASJC Scopus subject areas

General Pharmacology, Toxicology and Pharmaceutics
General Biochemistry, Genetics and Molecular Biology

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10.1016/0024-3205(92)90103-V

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title = "Synthesis and binding characteristics of the highly delta-specific new tritiated opioid peptide, [3H] deltorphin II",

abstract = "A radiolabelled form of deltorphin II was synthesized by catalytic tritiation using [p-IPhe3]-deltorphin II as a precursor. The ligand labels rat brain membranes with a Kd value of 1.9 nM, and the Bmax was found to be 92 fmol/mg protein. This new tritiated ligand exhibits high affinity for the delta opioid binding site, whereas its binding to the mu type is weak and extremely low for the kappa type. Mu/delta and kappa/delta selectivity ratios were about 900 and 10000, respectively. The highly delta selective binding properties of this new radioligand suggest that it could serve as an excellent tool for investigating the delta opioid receptors in various species.",

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year = "1992",

doi = "10.1016/0024-3205(92)90103-V",

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T1 - Synthesis and binding characteristics of the highly delta-specific new tritiated opioid peptide, [3H] deltorphin II

AU - Búzás, B.

AU - Tóth, G.

AU - Cavagnero, S.

AU - Hruby, V. J.

AU - Borsodi, A.

PY - 1992

Y1 - 1992

N2 - A radiolabelled form of deltorphin II was synthesized by catalytic tritiation using [p-IPhe3]-deltorphin II as a precursor. The ligand labels rat brain membranes with a Kd value of 1.9 nM, and the Bmax was found to be 92 fmol/mg protein. This new tritiated ligand exhibits high affinity for the delta opioid binding site, whereas its binding to the mu type is weak and extremely low for the kappa type. Mu/delta and kappa/delta selectivity ratios were about 900 and 10000, respectively. The highly delta selective binding properties of this new radioligand suggest that it could serve as an excellent tool for investigating the delta opioid receptors in various species.

AB - A radiolabelled form of deltorphin II was synthesized by catalytic tritiation using [p-IPhe3]-deltorphin II as a precursor. The ligand labels rat brain membranes with a Kd value of 1.9 nM, and the Bmax was found to be 92 fmol/mg protein. This new tritiated ligand exhibits high affinity for the delta opioid binding site, whereas its binding to the mu type is weak and extremely low for the kappa type. Mu/delta and kappa/delta selectivity ratios were about 900 and 10000, respectively. The highly delta selective binding properties of this new radioligand suggest that it could serve as an excellent tool for investigating the delta opioid receptors in various species.

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Synthesis and binding characteristics of the highly delta-specific new tritiated opioid peptide, [³H] deltorphin II

Abstract

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