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Lu-aa47070

Names

[ CAS No. ]:
913842-25-8

[ Name ]:
Lu-aa47070

[Synonym ]:
phosphoric acid mono{2-[(E/Z)-4-(3,3-dimethylbutyrylamino)-3,5-difluorobenzoylimino]thiazol-3-ylmethyl} ester
phosphoric acid mono-{2-[(E/Z)-4-(3,3-dimethyl-butyrylamino)-3,5-difluoro-benzoylimino]-thiazol-3-ylmethyl} ester
LU-AA47070

Biological Activity

[Description]:

Lu AA47070 is a phosphonooxymethylene prodrug of a potent and selective Adenosine A2A receptor antagonist. Lu AA47070 reverses the motor and motivational effects produced by dopamine D2 receptor blockade[1][2].

[Related Catalog]:

Research Areas >> Neurological Disease
Signaling Pathways >> GPCR/G Protein >> Adenosine Receptor

[In Vivo]

Lu AA47070 (3.75、7.5、15、30 mg/kg；腹腔注射) 逆转由亚慢性给药 D2 拮抗剂匹莫齐特（1.0 mg/kg；腹腔注射）引起的下颌颤动、僵直和运动抑制[2]< /sup>。 Animal Model: Male Sprague Dawley rats[2] Dosage: 3.75, 7.5, 15, 30 mg/kg Administration: I.p. Result: Reversed the tremulous jaw movements, catalepsy, and locomotor suppression induced by subchronic administration of the D2 antagonist pimozide (1.0 mg/kg IP).

[References]

[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 hA2A Receptor AntagonistJ. Med. Chem., Article ASAPDOI: 10.1021/jm1008659Publication Date (Web): January 6, 2011

[2]. Collins LE, et al. The novel adenosine A2A antagonist Lu AA47070 reverses the motor and motivational effects produced by dopamine D2 receptor blockade. Pharmacol Biochem Behav. 2012 Jan;100(3):498-505.  

Chemical & Physical Properties

[ Molecular Formula ]:
C17H20F2N3O6PS

[ Molecular Weight ]:
463.39

[ Exact Mass ]:
463.07800

[ PSA ]:
168.27000

[ LogP ]:
3.08340

Related Compounds