Specific tritium labelling of thyroliberin on histidyl and prolyl residues

Levine‐Pinto, H.; Morgat, Jean‐Louis; Fromageot, P.

doi:10.1002/jlcr.2580190203

Labelled Comp Radiopharmac

1982

DOI: 10.1002/jlcr.2580190203

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Specific tritium labelling of thyroliberin on histidyl and prolyl residues

H. Levine‐Pinto¹,

Jean‐Louis Morgat²,

P. Fromageot³

Abstract: SUMMARY T.ritiation of thyroliberin (L-CGlu-L-His-L-Pro-NHZ) 5starting from the L -[ A -Pro']-TRF, on prolyl and histidyl residues is being dealt with below.By catalytic tritiation of the double bond, followed by iodination of histidyl residue and catalytic deshalogenation in presence of tritium gas, TRF was labelled with a specific radioactivity close to the theoretical value. 3H-[ 2 , 5-His2-3 ,4-Pro 1 -TRF retained all biological potencies. 3Keg words : histidyl -prolyl -thyroliberin -tritiationt r i t ium . Show more

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1983

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Cited by 3 publications

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Synthesis of S‐[³H]‐DO‐710, a benzamide ligand of the D₂‐dopamine receptor and of S‐[³H]‐azidosulpride, its photoactivable analog

Rognan¹,

Mann²,

Hamdi³

et al. 1987

Labelled Comp Radiopharmac

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The preparation of the tritium labelled benzamides, S‐[3H]‐DO‐710 and S‐[3H]‐azidosulpride is reported. The synthesis involves enantioselective preparation of the pyrrolidinyl moiety, reductive tritiation of an allylic precursor and conversion of an amino, to an azido function. Both labelled ligands are D2‐dopaminergic antagonists, useful in binding experiments and to achieve covalent bonds after light exposure at the receptor site level.

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Synthesis of S‐[³H]‐DO‐710, a benzamide ligand of the D₂‐dopamine receptor and of S‐[³H]‐azidosulpride, its photoactivable analog

Rognan¹,

Mann²,

Hamdi³

et al. 1987

Labelled Comp Radiopharmac

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Synthesis and analysis of tritiated neuropeptides

Kaspersen¹,

Rooy²,

Wallaart³

et al. 1983

Recl. Trav. Chim. Pays‐Bas

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The synthesis, purification and analysis of three tritiated neuropeptides are described. Org 2766 (an ACTH (4-9) analogue) and Org G K 78 (des-Tyr-y-endorphin) were labelled in the aromatic ring of phenylalanine by catalytic deiodination of the (p-iodopheny1)alanine precursors using 3H,. Org 5878 (des-enkephalin-y-endorphin) was labelled in the lysine residue by reduction of the ~-2,6-diamino-4-hexynoic acid-containing analogue with 3H,. The peptides were purified by preparative HPLC using ammonium acetate buffer systems. The chemical purity was determined by ' H NMR, the radiochemical purity was measured by HPLC and the 3H distribution by 3H NMR. Specific activities (as determined by HPLC) were ca. 900 GBq.mmol-' for Org 2766 and Org G K 78 and 1400 GBq mmol-' for Org 5878. (1981).phosphate (pH 3)/methanol (65/35, v/v) or on LiChrosorb 10 NH, using a gradient of 0.01 M NH,OAc (pH 4.8) containing We are grateful to Dr. J. van Nispen and Drs. H. Greven for stimulating discussions and we wish to thank Mr. J. Thio for helpful technical assistance in the HPLC experiments.

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Multihormonal regulation of the pituitary gland binding and secretory responses to hypothalamic neuropeptides in rat GH pituitary strains in culture

Gourdji

1985

Neurochemistry International

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Specific tritium labelling of thyroliberin on histidyl and prolyl residues

Cited by 3 publications

References 13 publications

Synthesis of S‐[³H]‐DO‐710, a benzamide ligand of the D₂‐dopamine receptor and of S‐[³H]‐azidosulpride, its photoactivable analog

Synthesis of S‐[³H]‐DO‐710, a benzamide ligand of the D₂‐dopamine receptor and of S‐[³H]‐azidosulpride, its photoactivable analog

Synthesis and analysis of tritiated neuropeptides

Multihormonal regulation of the pituitary gland binding and secretory responses to hypothalamic neuropeptides in rat GH pituitary strains in culture

Contact Info

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Resources

About

Specific tritium labelling of thyroliberin on histidyl and prolyl residues

Cited by 3 publications

References 13 publications

Synthesis of S‐[3H]‐DO‐710, a benzamide ligand of the D2‐dopamine receptor and of S‐[3H]‐azidosulpride, its photoactivable analog

Synthesis of S‐[3H]‐DO‐710, a benzamide ligand of the D2‐dopamine receptor and of S‐[3H]‐azidosulpride, its photoactivable analog

Synthesis and analysis of tritiated neuropeptides

Multihormonal regulation of the pituitary gland binding and secretory responses to hypothalamic neuropeptides in rat GH pituitary strains in culture

Contact Info

Product

Resources

About

Synthesis of S‐[³H]‐DO‐710, a benzamide ligand of the D₂‐dopamine receptor and of S‐[³H]‐azidosulpride, its photoactivable analog

Synthesis of S‐[³H]‐DO‐710, a benzamide ligand of the D₂‐dopamine receptor and of S‐[³H]‐azidosulpride, its photoactivable analog