- A3 ADENOSINE RECEPTOR ALLOSTERIC MODULATORS
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The present invention relates to allosteric modulation of A3 adenosine receptor (A3AR) and provides for the use of an A3 adenosine receptor modulator (A3RM),for the preparation of pharmaceutical compositions for
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Page/Page column 25-26
(2008/06/13)
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- Structure-activity relationships of new 1H-imidazo[4,5-c]quinolin-4-amine derivatives as allosteric enhancers of the A3 adenosine receptor
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1H-Imidazo[4,5-c]quinolin-4-amine derivatives have been synthesized as allosteric modulators of the human A3 adenosine receptor (AR). Structural modifications were made at the 4-amino and 2 positions. The compounds were tested in both binding and functional assays, and many were found to be allosteric enhancers of the action of A3AR agonists by several different criteria. First, a potentiation of the maximum efficacy of the agonist C1-IB-MECA was observed for numerous derivatives. Also, a number of these compounds decreased the rate of dissociation of the agonist [ 125I]I-AB-MECA from the A3AR. Most prominently, compound 43 (LUF6000) was found to enhance agonist efficacy in a functional assay by 45% and decrease dissociation rate similarly without influencing agonist potency. The structural requirements for allosteric enhancement at the A3AR were distinct from the requirements to inhibit equilibrium binding. Thus, we have prepared allosteric enhancers of the human A3AR that have an improved allosteric effect in comparison to the inhibition of equilibrium binding at the orthosteric site.
- G?bly?s, Anikó,Gao, Zhan-Guo,Brussee, Johannes,Connestari, Roberto,Santiago, Sabrina Neves,Ye, Kai,Ijzerman, Adriaan P.,Jacobson, Kenneth A.
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p. 3354 - 3361
(2007/10/03)
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- 1H-imidazo?4,5-c!quinolin-4-amines
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Novel 1H-imidazo?4,5-c!quinolin-4-amines are disclosed. The compounds function as antiviral agents and they are potential synthetic intermediates in the preparation of known antiviral agents and labeled known antiviral agents. Processes for the preparation of the compounds, methods for their antiviral use, and methods of inducing interferon biosynthesis, are also described.
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- Olefinic 1H-imidazo[4,5-c]quinolin-4-amines
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Novel 1-substituted 1H-imidazo-[4,5-c]quinolin-4-amines are disclosed. These compounds function as antiviral agents, and they are potential synthetic intermediates in the preparation of known antiviral agents and labeled known antiviral agents. This inven
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- 1H-Imidazoquinolin-4-amines: Novel Non-Xanthine Adenosine Antagonists
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On the basis of a model we recently developed for the antagonist binding site of the adenosine A1 receptor (J.Med.Chem. 1990, 33, 1708-1713), it was predicted that 1H-imidazoquinolin-4-amines would be antagonists of the A1 rec
- Galen, Philip J. M. van,Nissen, Peter,Wijngaarden, Ineke van,IJzerman, Adriaan P.,Soudijn, Willem
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p. 1202 - 1206
(2007/10/02)
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