Deltorphin II analogues with 6-hydroxy-2-aminotetralin-2-carboxylic acid in position 1

Z Darula, KE Kövér, K Monory, A Borsodi…

Index: Darula, Zsuzsanna; Koever, Katalin E.; Monory, Krisztina; Borsodi, Anna; Mako, Eva; Ronai, Andras; Tourwe, Dirk; Peter, Antal; Toth, Geza Journal of Medicinal Chemistry, 2000 , vol. 43, # 7 p. 1359 - 1366

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Citation Number: 15

Abstract

Two approaches to the design of very active and highly selective δ opioid peptides were used to obtain new deltorphin analogues with altered hydrophobic and stereoelectronic properties. Deltorphin II analogues were synthesized with the substitution of Ile instead of Val at positions 5 and 6 in the address domain and 6-hydroxy-2-aminotetralin-2-carboxylic acid (Hat) instead of Tyr 1 in the message domain. In the radioreceptor-binding studies, in ...