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Synthesis of the diastereomers of β-Me-Tyr and β-Me-Phe and their effect on the biological properties of the delta opioid receptor antagonist TIPP

✍ Scribed by Els Mannekens; Dirk Tourwé; Sylvia Vanderstichele; Trang Nguyen Thi Diem; Géza Tóth; Antal Péter; Nga N. Chung; Peter W. Schiller

Publisher
Springer Netherlands
Year
1995
Tongue
English
Weight
183 KB
Volume
2
Category
Article
ISSN
1573-3149

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✦ Synopsis

In order to influence side-chain conformations and to increase the I.t-agonist properties of the 5-selective opioid receptor 8-antagonist H-Tyr-Tic-Phe-Phe-NH 2, residues Tyr l, Phe 3 and Phe 4 were replaced by their ]3-methylsubstituted stereoisomers. Synthesis of [3-Me-Tyr was carried out in a stereoselective way. Incorporation of the modified amino acids was performed by SPPS. Receptor binding data and GPI and MVD bioassays were obtained for all stereoisomers, in general showing equal or slightly increased potencies. In the [(R,S)[3-Me-Phe3]analogue, the introduction of the ~-methyl substituent restores signal transduction.

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