Abstract

The major goal in this laboratory will be to synthesize gram quantities of biologically active peptides which are needed for biochemical, pharmacological, biological and biophysical studies in this Program Project. Facilities for synthesis, purification and analysis will be available.
The specific aims of The Core Facility are: 1. To prepare 1-2 g quantities of DPDPE and [p-ClPhe4]DPDPE in high purity for a variety of biochemical, pharmacological, and biophysical studies, as well as studies of bioavailability, biodegredation and toxicity. 2. To prepare 1 g of [Cys5, Cys11]Dynorphin A1-11-NH2 for a wide variety of biological studies as in 1. 3. To prepare 1 g of CTAP, a potent and highly eta opioid receptor selective peptide, to assess its antagonist effect as an opioid and to examine its biostability. 4. To prepare whether peptide ligands as needed in the various projects of the Program Project. 5. To prepare quantities of the new compounds which cross the blood brain barrier more effectively for extensive biological and biodistribution studies.

  Funding Agency

Agency
National Institute of Health (NIH)
Institute
National Institute on Drug Abuse (NIDA)
Type
Research Program Projects (P01)
Project #
5P01DA006284-03
Application #
3094714
Study Section
Special Emphasis Panel (SRCD (07))
Project Start
1989-09-30
Project End
1992-09-14
Budget Start
1991-09-01
Budget End
1992-09-14
Support Year
3
Fiscal Year
1991
Total Cost
Indirect Cost

  Institution

Name
University of Arizona
Department
Type
Schools of Arts and Sciences
DUNS #
City
Tucson
State
AZ
Country
United States
Zip Code
85721

  Publications

Remesic, Michael; Macedonio, Giorgia; Mollica, Adriano et al. (2018) Cyclic biphalin analogues with a novel linker lead to potent agonist activities at mu, delta, and kappa opioid receptors. Bioorg Med Chem 26:3664-3667
Mowlazadeh Haghighi, Saghar; Zhou, Yang; Dai, Jixun et al. (2018) Replacement of Arg with Nle and modified D-Phe in the core sequence of MSHs, Ac-His-D-Phe-Arg-Trp-NH2, leads to hMC1R selectivity and pigmentation. Eur J Med Chem 151:815-823
Sandweiss, A J; McIntosh, M I; Moutal, A et al. (2018) Genetic and pharmacological antagonism of NK1 receptor prevents opiate abuse potential. Mol Psychiatry 23:1745-1755
Bannister, Kirsty; Qu, Chaoling; Navratilova, Edita et al. (2017) Multiple sites and actions of gabapentin-induced relief of ongoing experimental neuropathic pain. Pain 158:2386-2395
Vardanyan, Ruben S; Cain, James P; Haghighi, Saghar Mowlazadeh et al. (2017) Synthesis and Investigation of Mixed ?-Opioid and ?-Opioid Agonists as Possible Bivalent Ligands for Treatment of Pain. J Heterocycl Chem 54:1228-1235
Cai, Minying; Marelli, Udaya Kiran; Mertz, Blake et al. (2017) Structural Insights into Selective Ligand-Receptor Interactions Leading to Receptor Inactivation Utilizing Selective Melanocortin 3 Receptor Antagonists. Biochemistry 56:4201-4209
Hall, Sara M; Lee, Yeon Sun; Hruby, Victor J (2016) Dynorphin A analogs for the treatment of chronic neuropathic pain. Future Med Chem 8:165-77
Deekonda, Srinivas; Cole, Jacob; Sunna, Sydney et al. (2016) Enkephalin analogues with N-phenyl-N-(piperidin-2-ylmethyl)propionamide derivatives: Synthesis and biological evaluations. Bioorg Med Chem Lett 26:222-7
Lee, Yeon Sun; Kupp, Robert; Remesic, Michael V et al. (2016) Various modifications of the amphipathic dynorphin A pharmacophore for rat brain bradykinin receptors. Chem Biol Drug Des 88:615-9
Hall, Sara M; LeBaron, Lindsay; Ramos-Colon, Cyf et al. (2016) Discovery of Stable Non-opioid Dynorphin A Analogues Interacting at the Bradykinin Receptors for the Treatment of Neuropathic Pain. ACS Chem Neurosci 7:1746-1752

Showing the most recent 10 out of 268 publications