Deletion of Ac-NMePhe(1) from [NMePhe(1) ]arodyn under acidic conditions, part 2: effects of substitutions on pharmacological activity.
Deletion of Ac-NMePhe(1) from [NMePhe(1) ]arodyn under acidic conditions, part 2: effects of substitutions on pharmacological activity.
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DOI：
10.1002/bip.21495
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发表时间：
2011
期刊：
影响因子：
2.9
通讯作者：
Aldrich, Jane V.
中科院分区：
文献类型：
--
作者：
Fang, Wei-Jie;Bennett, Marco A.;Murray, Thomas F.;Aldrich, Jane V.
Arodyn (Ac[Phe1,2,3,Arg4,D-Ala8]Dyn A(1-11)-NH2) is an acetylated dynorphin A (Dyn A) analog that is a potent and selective κ opioid receptor antagonist (Bennett et al. J. Med. Chem. 2002, 45, 5617), and its analog [NMePhe1]arodyn shows even higher affinity and selectivity for κ opioid receptors (Bennett et al., J. Pep. Res. 2005, 65, 322). However, the latter compound is prone to deletion of the Ac-NMePhe moiety from the N-terminus of the peptide during acidic cleavage as described in the accompanying paper. Several stable analogs of [NMePhe1]arodyn and [NMePhe1,Trp3]arodyn where the acetyl group was substituted with a heteroatom-containing group were evaluated for their opioid receptor affinity, selectivity, and efficacy. Methoxycarbonyl derivatives exhibited the highest κ opioid receptor affinity among the analogs. Additional CH3OCO[NMePhe1]arodyn analogs where position 3 was substituted with other aromatic or non-aromatic residues were also evaluated for κ receptor affinity, selectivity, and efficacy. [CH3OCO-NMePhe1]arodyn has similar κ opioid receptor affinity as [NMePhe1]arodyn, retains high κ opioid receptor selectivity, and is a potent κ opioid receptor antagonist.
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DOI：
10.1111/j.1399-3011.2005.00216.x
发表时间：
2005-03-01
期刊：
JOURNAL OF PEPTIDE RESEARCH
影响因子：
--
作者：
Bennett, MA;Murray, TF;Aldrich, JV
通讯作者：
Aldrich, JV
DOI：
10.1073/pnas.78.10.6543
发表时间：
1981-01-01
期刊：
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA-BIOLOGICAL SCIENCES
影响因子：
--
作者：
CHAVKIN, C;GOLDSTEIN, A
通讯作者：
GOLDSTEIN, A
影响因子：
7.3
作者：
Schlechtingen, G;Zhang, L;Goodman, M
通讯作者：
Goodman, M
影响因子：
5
作者：
Carroll, I;Thomas, JB;Harris, LS
通讯作者：
Harris, LS
DOI：
10.1111/j.1476-5381.1947.tb00336.x
发表时间：
1947-01-01
期刊：
BRITISH JOURNAL OF PHARMACOLOGY AND CHEMOTHERAPY
影响因子：
--
作者：
SCHILD, HO
通讯作者：
SCHILD, HO