Topographical requirements for delta opioid ligands: presence of a carboxyl group in position 4 is not critical for deltorphin high delta receptor affinity and analgesic activity.

Abstract:

:To investigate the role of the carboxyl group in deltorphin molecules, we have synthesized three new analogues in which the acidic amino acid residues in position 4 of the deltorphins were replaced by non-acidic but hydrophilic amino acids residues. The three analogues, [Ser4]-, [Gln4]-, and [Cys4]-deltorphin, all are as potent or more potent than either deltorphin I or II at delta opioid receptors and possess good delta selectivities. The excellent correlation between their in vitro delta receptor potencies and their intrathecal antinociception activity forms a strong argument for involvement of those receptors in spinal nociceptive modulation in the rats.

authors

Misicka A,Lipkowski AW,Fang L,Knapp RJ,Davis P,Kramer T,Burks TF,Yamamura HI,Carr DB,Hruby VJ

doi

10.1016/s0006-291x(05)81335-x

subject

Has Abstract

pub_date

1991-11-14 00:00:00

pages

1290-7

issue

3

eissn

0006-291X

issn

1090-2104

pii

S0006-291X(05)81335-X

journal_volume

180

pub_type

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