Theaffinities (Ki) of the drug for the humanadenosine receptors are 5.9nM for the adenosine A2A receptor, 410nM for the adenosineA1 receptor (69-fold lower than for the A2A receptor), 260nM for the adenosineA2B receptor (44-fold lower than for the A2A receptor), and >10,000nM for the adenosineA3 receptor (>1,695-fold lower than for the A2A receptor).[2]
^abcdMüller, Christa E. (2015). "Adenosine A2A Receptor Antagonists in Drug Development".The Adenosinergic System. Current Topics in Neurotoxicity. Vol. 10. Cham: Springer International Publishing. pp. 39–56.doi:10.1007/978-3-319-20273-0_3.ISBN978-3-319-20272-3.
^Al-Attraqchi OH, Attimarad M, Venugopala KN, Nair A, Al-Attraqchi NH (2019). "Adenosine A2A Receptor as a Potential Drug Target - Current Status and Future Perspectives".Curr Pharm Des.25 (25):2716–2740.doi:10.2174/1381612825666190716113444.PMID31333093.
^Zheng J, Zhang X, Zhen X (February 2019). "Development of Adenosine A2A Receptor Antagonists for the Treatment of Parkinson's Disease: A Recent Update and Challenge".ACS Chem Neurosci.10 (2):783–791.doi:10.1021/acschemneuro.8b00313.PMID30199223.
^abMikkelsen GK, Langgård M, Schrøder TJ, Kreilgaard M, Jørgensen EB, Brandt G, Griffon Y, Boffey R, Bang-Andersen B (March 2015). "Synthesis and SAR studies of analogues of 4-(3,3-dimethyl-butyrylamino)-3,5-difluoro-N-thiazol-2-yl-benzamide (Lu AA41063) as adenosine A2A receptor ligands with improved aqueous solubility".Bioorg Med Chem Lett.25 (6):1212–1216.doi:10.1016/j.bmcl.2015.01.062.PMID25701253.
^Sams AG, Mikkelsen GK, Larsen M, Langgård M, Howells ME, Schrøder TJ, et al. (February 2011). "Discovery of phosphoric acid mono-{2-[(E/Z)-4-(3,3-dimethyl-butyrylamino)-3,5-difluoro-benzoylimino]-thiazol-3-ylmethyl} ester (Lu AA47070): a phosphonooxymethylene prodrug of a potent and selective hA(2A) receptor antagonist".Journal of Medicinal Chemistry.54 (3):751–764.doi:10.1021/jm1008659.PMID21210664.
^"LU AA 47070".AdisInsight. Springer Nature Switzerland AG. 18 May 2009. Retrieved22 September 2024.
^Sachdeva S, Gupta M (July 2013)."Adenosine and its receptors as therapeutic targets: An overview".Saudi Pharmaceutical Journal.21 (3):245–253.doi:10.1016/j.jsps.2012.05.011.PMC3744929.PMID23960840.Antagonists of the A2A subtype of adenosine receptor have emerged as a leading candidate class of nondopaminergic antiparkinsonian agents (Feigin, 2003). The ability of Lu AA47070, adenosine A2A antagonist to reverse the effects of D2 receptor blockade suggests that this compound could have potential utility as a treatment for parkinsonism, and for some of the motivational symptoms of depression. In the adult male Sprague Dawley rats the tremulous jaw movements induced by subchronic administration of the DA D2 antagonist pimozide were reversed by Lu AA47070. Lu AA47070 was also able to reverse the catalepsy induced by subchronic administration of the D2 antagonist pimozide and it also reverse the locomotor suppression induced by subchronic administration of the D2 antagonist pimozide (Collins et al., 2012).
^Collins LE, Sager TN, Sams AG, Pennarola A, Port RG, Shahriari M, Salamone JD (January 2012). "The novel adenosine A2A antagonist Lu AA47070 reverses the motor and motivational effects produced by dopamine D2 receptor blockade".Pharmacology, Biochemistry, and Behavior.100 (3):498–505.doi:10.1016/j.pbb.2011.10.015.PMID22037410.
