Skip Navigation

Nucleic Acids Symposium Series 2000 44(1):19-20; doi:10.1093/nass/44.1.19
© 2000 by Oxford University Press
This Article
Right arrow FREE Full Text (PDF) Freely available
Right arrow Alert me when this article is cited
Right arrow Alert me if a correction is posted
Services
Right arrow Email this article to a friend
Right arrow Similar articles in this journal
Right arrow Similar articles in PubMed
Right arrow Alert me to new issues of the journal
Right arrow Add to My Personal Archive
Right arrow Download to citation manager
Right arrowRequest Permissions
Google Scholar
Right arrow Articles by Umino, T.
Right arrow Articles by Matsuda, A.
Right arrow Search for Related Content
PubMed
Right arrow PubMed Citation
Right arrow Articles by Umino, T.
Right arrow Articles by Matsuda, A.
Social Bookmarking
Add to CiteULike   Add to Connotea   Add to Del.icio.us  
What's this?

Synthesis and structure-activity relationships of selective ligands for P3purinoceptor-like protein (P3LP)

Takashi Umino1, Kazuaki Yoshioka2, Yoshiko Saitoh2, Noriaki Minakawa1, Hiroyasu Nakata2 and Akira Matsuda1

1 Graduate School of Pharmaceutical Sciences, Hokkaido University, Kita-12, Nishi-6, Kita-ku, Sapporo 060-0812, Japan, 2 Department of Molecular and Cellular Neurobiology, Tokyo Metropolitan Institute for Neuroscience, Musasidai 2-6, Fuchu, Tokyo 183-8526, Japan

We examined the structure-activity relationship of various 5'-N-substituted-carboxamidoadenosine derivatives toward P3 purinoceptor-like protein (P3LP), which has affinity for both adenine nucleosides and nucleotides. We discovered a hydrophobic binding region near the 5'-N-substituted-carboxamide group. From the linear alkyl N-substituted derivatives, 1-(adenin-9-yl)-1-deoxy-N-n-pentyl-ß-D-ribofuranuronamide (6) was found to be the most potent ligand. In the series of the N-cycloalkyl derivatives, 1-(adenin-9-yl)-1-deoxy-N-cyclohexyl-ß-D-ribofuranuronamide (8) was the strongest ligand. We also examined the receptor selectivity for the selected nucleosides 6 and 8 with 1 (HAK2701) and N-ethylcarboxamidoadenosine (NECA) versus P1 purinoceptor subtypes, such as adenosine A1, A2A, A2B, and A3 receptors and found 8 is the most selective ligand for P3LP.


Add to CiteULike CiteULike   Add to Connotea Connotea   Add to Del.icio.us Del.icio.us    What's this?




Disclaimer:
Please note that abstracts for content published before 1996 were created through digital scanning and may therefore not exactly replicate the text of the original print issues. All efforts have been made to ensure accuracy, but the Publisher will not be held responsible for any remaining inaccuracies. If you require any further clarification, please contact our Customer Services Department.