Chemistry:LUF6000
From HandWiki
LUF6000 is an experimental drug which acts as a positive allosteric modulator of the adenosine A3 receptor. It has no effect on A3-mediated signalling by itself, but significantly enhances the effect of A3-selective agonists or partial agonists, and can even cause some adenosine A3 antagonists to produce agonist-like signalling. It has antiinflammatory effects in animal studies.[1][2][3][4][5][6]
References
- ↑ "Structure-activity relationships of new 1H-imidazo[4,5-cquinolin-4-amine derivatives as allosteric enhancers of the A3 adenosine receptor"]. Journal of Medicinal Chemistry 49 (11): 3354–3361. June 2006. doi:10.1021/jm060086s. PMID 16722654.
- ↑ "Flexible modulation of agonist efficacy at the human A3 adenosine receptor by the imidazoquinoline allosteric enhancer LUF6000". BMC Pharmacology 8: 20. December 2008. doi:10.1186/1471-2210-8-20. PMID 19077268.
- ↑ "A series of 2,4-disubstituted quinolines as a new class of allosteric enhancers of the adenosine A3 receptor". Journal of Medicinal Chemistry 52 (4): 926–931. February 2009. doi:10.1021/jm8014052. PMID 19161279.
- ↑ "Functionally biased modulation of A(3) adenosine receptor agonist efficacy and potency by imidazoquinolinamine allosteric enhancers". Biochemical Pharmacology 82 (6): 658–668. September 2011. doi:10.1016/j.bcp.2011.06.017. PMID 21718691.
- ↑ "A₃ adenosine receptor allosteric modulator induces an anti-inflammatory effect: in vivo studies and molecular mechanism of action". Mediators of Inflammation 2014. 2014. doi:10.1155/2014/708746. PMID 25374446.
- ↑ "Genetic and functional modulation by agonist MRS5698 and allosteric enhancer LUF6000 at the native A3 adenosine receptor in HL-60 cells". Purinergic Signalling 20 (5): 559–570. October 2024. doi:10.1007/s11302-024-09992-z. PMID 38416332.
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