IBMX, 3-isobutyl-1-methylxanthine, like other methylated xanthine derivatives, is both a
- competitive nonselective phosphodiesterase inhibitor [1] which raises intracellular cAMP, activates PKA, inhibits TNF-alpha [2] [3] and leukotriene [4] synthesis, and reduces inflammation and innate immunity [4] and
- nonselective adenosine receptor antagonist [5].
As a phosphodiesterase inhibitor, IBMX has IC50 = 2-50 μM [6] and does not inhibit PDE8 or PDE9 [7].
[edit] References
- ^ Essayan DM. (2001). "Cyclic nucleotide phosphodiesterases.". J Allergy Clin Immunol. 108 (5): 671-80. doi:10.1067/mai.2001.119555. PMID 11692087.
- ^ Deree J, Martins JO, Melbostad H, Loomis WH, Coimbra R. (2008). "Insights into the regulation of TNF-alpha production in human mononuclear cells: the effects of non-specific phosphodiesterase inhibition.". Clinics (Sao Paulo). 63 (3): 321-8. doi:10.1590/S1807-59322008000300006. PMID 18568240.
- ^ Marques LJ, Zheng L, Poulakis N, Guzman J, Costabel U (February 1999). "Pentoxifylline inhibits TNF-alpha production from human alveolar macrophages". Am. J. Respir. Crit. Care Med. 159 (2): 508–11. PMID 9927365. http://ajrccm.atsjournals.org/cgi/pmidlookup?view=long&pmid=9927365.
- ^ a b Peters-Golden M, Canetti C, Mancuso P, Coffey MJ. (2005). "Leukotrienes: underappreciated mediators of innate immune responses.". J Immunol. 174 (2): 589-94. PMID 15634873. http://www.jimmunol.org/cgi/content/full/174/2/589.
- ^ Daly JW, Jacobson KA, Ukena D. (1987). "Adenosine receptors: development of selective agonists and antagonists.". Prog Clin Biol Res. 230 (1): :41-63. PMID 3588607.
- ^ J.A.Beavo et al. Mol. Pharmacol. 1970 6 597
- ^ Soderling and Beavo Current Opinion in Cell Biol. 2000 12 174