Abstract

of Work: The pharmacological and physiological activity of recently developed opioid analogues were determined in mice. The bioactivity profile paralled that of the in vitro pharmacological data and reflected the receptor binding affinity (see previous projects for details). Some synthetic analogues which exhibited agonism were weaker than the control substances (deltorphin for delta or morphine for mu receptors); however, some were substantially better (2- to 25-fold) than morphine in generating analgesia using standard testing procedures. In fact, these compounds are under patent application in Japan and disclosure at this time would jepardize that process.

  Funding Agency

Agency
National Institute of Health (NIH)
Institute
National Institute of Environmental Health Sciences (NIEHS)
Type
Intramural Research (Z01)
Project #
1Z01ES100472-01
Application #
6673283
Study Section
(LCBR)
Project Start
Project End
Budget Start
Budget End
Support Year
1
Fiscal Year
2002
Total Cost
Indirect Cost

  Institution

Name
U.S. National Inst of Environ Hlth Scis
Department
Type
DUNS #
City
State
Country
United States
Zip Code

  Publications

Lazarus, Lawrence H; Okada, Yoshio (2012) Engineering endomorphin drugs: state of the art. Expert Opin Ther Pat 22:1-14
Marczak, Ewa D; Jinsmaa, Yunden; Myers, Page H et al. (2009) Orally administered H-Dmt-Tic-Lys-NH-CH2-Ph (MZ-2), a potent mu/delta-opioid receptor antagonist, regulates obese-related factors in mice. Eur J Pharmacol 616:115-21
Balboni, Gianfranco; Trapella, Claudio; Sasaki, Yusuke et al. (2009) Influence of the side chain next to C-terminal benzimidazole in opioid pseudopeptides containing the Dmt-Tic pharmacophore. J Med Chem 52:5556-9
Vergura, Raffaella; Balboni, Gianfranco; Spagnolo, Barbara et al. (2008) Anxiolytic- and antidepressant-like activities of H-Dmt-Tic-NH-CH(CH2-COOH)-Bid (UFP-512), a novel selective delta opioid receptor agonist. Peptides 29:93-103
Jinsmaa, Yunden; Marczak, Ewa D; Balboni, Gianfranco et al. (2008) Inhibition of the development of morphine tolerance by a potent dual mu-delta-opioid antagonist, H-Dmt-Tic-Lys-NH-CH2-Ph. Pharmacol Biochem Behav 90:651-7
Balboni, Gianfranco; Fiorini, Stella; Baldisserotto, Anna et al. (2008) Further studies on lead compounds containing the opioid pharmacophore Dmt-Tic. J Med Chem 51:5109-17
Koda, Yasuko; Del Borgo, Mark; Wessling, Susanne T et al. (2008) Synthesis and in vitro evaluation of a library of modified endomorphin 1 peptides. Bioorg Med Chem 16:6286-96
Salvadori, Severo; Fiorini, Stella; Trapella, Claudio et al. (2008) Role of benzimidazole (Bid) in the delta-opioid agonist pseudopeptide H-Dmt-Tic-NH-CH(2)-Bid (UFP-502). Bioorg Med Chem 16:3032-8
Ryu, Eun Kyoung; Wu, Zhanhong; Chen, Kai et al. (2008) Synthesis of a potent and selective (18)F-labeled delta-opioid receptor antagonist derived from the Dmt-Tic pharmacophore for positron emission tomography imaging. J Med Chem 51:1817-23
Li, Tingyou; Shiotani, Kimitaka; Miyazaki, Anna et al. (2007) Bifunctional [2',6'-dimethyl-L-tyrosine1]endomorphin-2 analogues substituted at position 3 with alkylated phenylalanine derivatives yield potent mixed mu-agonist/delta-antagonist and dual mu-agonist/delta-agonist opioid ligands. J Med Chem 50:2753-66

Showing the most recent 10 out of 38 publications