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.
journal_name
Biochem Biophys Res Communjournal_title
Biochemical and biophysical research communicationsauthors
Misicka A,Lipkowski AW,Fang L,Knapp RJ,Davis P,Kramer T,Burks TF,Yamamura HI,Carr DB,Hruby VJdoi
10.1016/s0006-291x(05)81335-xsubject
Has Abstractpub_date
1991-11-14 00:00:00pages
1290-7issue
3eissn
0006-291Xissn
1090-2104pii
S0006-291X(05)81335-Xjournal_volume
180pub_type
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