Lu AA47070

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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.

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Lu AA47070 Chemical Structure

CAS No. : 913842-25-8

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Description

In Vivo

Lu AA47070 (3.75, 7.5, 15, 30 mg/kg; i.p.) reverseS the tremulous jaw movements, catalepsy, and locomotor suppression induced by subchronic administration of the D2 antagonist pimozide (1.0 mg/kg IP)^[2].
Pharmacokinetic Parameters of Lu AA47070 in Sprague-Dawley rats^[1].

Compd	dose （mg/kg）	AUC(ng*h/L)	T_max (h)	C_max (ng/mL)	F (%)
32	1.5	2.9±0.7	0.5±0.1	869±68	55±13
32	15	35±3.0	0.4±0.2	6413±281	66±6

Sprague-Dawley rats, 1.5, 15 mg/kg po^[1]

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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).

Molecular Weight

463.39

Formula

C₁₇H₂₀F₂N₃O₆PS

CAS No.

913842-25-8

SMILES

O=P(O)(O)OCN1C=CS/C1=N\C(C2=CC(F)=C(NC(CC(C)(C)C)=O)C(F)=C2)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

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 Antagonist J. Med. Chem., Article ASAP DOI: 10.1021/jm1008659 Publication 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. [Content Brief]

Lu AA47070 Related Classifications

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Lu AA47070913842-25-8Lu AA 47070Lu AA-47070Adenosine ReceptorP1 receptorInhibitorinhibitorinhibit

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