Abstract

Significant progress was made in the last reporting period, resulting in five publications. One of these papers was a review article published in Pharmacological Reviews, a very high impact journal. The publication of this paper reflects the overall impact of our collaborative work with Dr. Prisinzano on the synthesis and evaluation of compounds related to Salvinorin A. Our collaborative efforts with Dr. Rices group yielded three publications in high impact Medicinal Chemistry journals. Our work with Dr. Prisinzano led to ne publication in the Journal of Natural Products, a leading journal for this type of work. Several manuscripts are in preparation and should be published by the next reporting period.

  Funding Agency

Agency
National Institute of Health (NIH)
Institute
National Institute on Drug Abuse (NIDA)
Type
Investigator-Initiated Intramural Research Projects (ZIA)
Project #
1ZIADA000525-04
Application #
8336474
Study Section
Project Start
Project End
Budget Start
Budget End
Support Year
4
Fiscal Year
2011
Total Cost
$736,945
Indirect Cost

  Institution

Name
National Institute on Drug Abuse
Department
Type
DUNS #
City
State
Country
Zip Code

  Publications

Sally, Elliott J; Xu, Heng; Dersch, Christina M et al. (2010) Identification of a novel ""almost neutral"" micro-opioid receptor antagonist in CHO cells expressing the cloned human mu-opioid receptor. Synapse 64:280-8
Iyer, Malliga R; Lee, Yong Sok; Deschamps, Jeffrey R et al. (2010) Probes for narcotic receptor mediated phenomena. 40. N-substituted cis-4a-ethyl-1,2,3,4,4a,9a-hexahydrobenzofuro[2,3-c]pyridin-8-ols. Bioorg Med Chem 18:91-9
Hsin, Ling-Wei; Chang, Li-Te; Rothman, Richard B et al. (2010) Synthesis and opioid activity of enantiomeric N-substituted 2,3,4,4a,5,6,7,7a-octahydro-1H-benzofuro[3,2-e]isoquinolines. J Med Chem 53:1392-6
Pelotte, Andrea L; Smith, Ryan M; Ayestas, Mario et al. (2009) Design, synthesis, and characterization of 6beta-naltrexol analogs, and their selectivity for in vitro opioid receptor subtypes. Bioorg Med Chem Lett 19:2811-4
Zhang, Yi; Lee, Yong Sok; Rothman, Richard B et al. (2009) Probes for narcotic receptor mediated phenomena. 39. Enantiomeric N-substituted benzofuro[2,3-c]pyridin-6-ols: synthesis and topological relationship to oxide-bridged phenylmorphans. J Med Chem 52:7570-9
Simpson, Denise S; Lovell, Kimberly M; Lozama, Anthony et al. (2009) Synthetic studies of neoclerodane diterpenes from Salvia divinorum: role of the furan in affinity for opioid receptors. Org Biomol Chem 7:3748-56
Kurimura, Muneaki; Liu, Hehua; Sulima, Agnieszka et al. (2008) Probes for narcotic receptor mediated phenomena. 37. Synthesis and opioid binding affinity of the final pair of oxide-bridged phenylmorphans, the ortho- and para-b-isomers and their N-phenethyl analogues, and the synthesis of the N-phenethyl analogues of J Med Chem 51:7866-81
Zezula, Josef; Singer, Lisa; Przybyl, Anna K et al. (2008) Synthesis and pharmacological effects of the enantiomers of the N-phenethyl analogues of the ortho and para e- and f-oxide-bridged phenylmorphans. Org Biomol Chem 6:2868-83