Chemistry:Lu AA47070
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Short description: Adenosine A2A receptor antagonist for Parkinson's disease
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| Other names | Lu-AA47070; LU AA 47070; LU-AA-47070 |
| Drug class | Adenosine A2A receptor antagonist |
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| Formula | C17H20F2N3O6PS |
| Molar mass | 463.39 g·mol−1 |
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Lu AA47070 is a selective adenosine A2A receptor antagonist that was under development for the treatment of Parkinson's disease but was never marketed.[1][2][3] It has been found to reverse some of the effects of dopamine D2 receptor antagonists like pimozide and haloperidol, for instance tremulous jaw movements, catalepsy, locomotor suppression, and other anti-motivational effects, in animals.[2][4][5] The drug is a prodrug of Lu AA41063.[6][7][3] It was discontinued in phase 1 clinical trials because it lacked the intended pharmacological properties in humans.[7][1] Lu AA47070 was first described by 2008.[8]
References
- ↑ 1.0 1.1 "LU AA 47070". AdisInsight. Springer Nature Switzerland AG. 18 May 2009. https://adisinsight.springer.com/drugs/800027391.
- ↑ 2.0 2.1 "Adenosine and its receptors as therapeutic targets: An overview". Saudi Pharmaceutical Journal 21 (3): 245–253. July 2013. doi:10.1016/j.jsps.2012.05.011. PMID 23960840. "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).".
- ↑ 3.0 3.1 "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. February 2011. doi:10.1021/jm1008659. PMID 21210664.
- ↑ "The Psychopharmacology of Effort-Related Decision Making: Dopamine, Adenosine, and Insights into the Neurochemistry of Motivation". Pharmacological Reviews 70 (4): 747–762. October 2018. doi:10.1124/pr.117.015107. PMID 30209181.
- ↑ "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. January 2012. doi:10.1016/j.pbb.2011.10.015. PMID 22037410.
- ↑ "International Union of Basic and Clinical Pharmacology. CXII: Adenosine Receptors: A Further Update". Pharmacological Reviews 74 (2): 340–372. April 2022. doi:10.1124/pharmrev.121.000445. PMID 35302044.
- ↑ 7.0 7.1 "Towards next generation adenosine A(2A) receptor antagonists". Current Medicinal Chemistry 21 (34): 3918–3935. 2014. doi:10.2174/0929867321666140826115123. PMID 25174927.
- ↑ "What's in the pipeline for the treatment of Parkinson's disease?". Expert Review of Neurotherapeutics 8 (12): 1829–1839. December 2008. doi:10.1586/14737175.8.12.1829. PMID 19086879.
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