Selective and potent antagonists for the A 2A adenosine receptors have been described recently. The most potent compounds have a triazolo-pyrimidine structure, whereas 8-styryl-xanthines usually possess lower affinity at the A 2A receptor. We have examined the quantitative structure activity relatio
โฆ LIBER โฆ
Structural Predictions of Adenosine 2B Antagonist Affinity Using Molecular Field Analysis
โ Scribed by Song, Yuqing ;Coupar, Ian M. ;Iskander, Magdy N.
- Publisher
- John Wiley and Sons
- Year
- 2001
- Tongue
- English
- Weight
- 515 KB
- Volume
- 20
- Category
- Article
- ISSN
- 1611-020X
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The tetrapeptide Boc-Trp-Phg-Asp-( l-Nal)-NH2 is a potent CCK-B agonist. Interestingly, bis-methylation of the C-terminal carboxamide group of this compound leads to Boc-Trp-Phg-Asp-( 1 -Nal)-N(Me)2 which behaves as a CCK-B antagonist in electrophysiological studies on hippocampal neurones (Comnger