ST3932-Adenosine-Receptor-Antagonist-MedChemExpress

ST3932Cat. No.:

HY-112840CAS No.:

1246018-21-2分?式:

C??H??N?O 分?量:

288.31作?靶点:

Adenosine Receptor 作?通路:

GPCR/G Protein 储存?式:Please store the product under the recommended conditions in the COA.BIOLOGICAL ACTIVITY

?物活性

ST3932 是 ST1535 的代谢物，为 adenosine A 2A 受体拮抗剂，对 A 2A 和 A 1 受体的 K i 值分别为 8 nM 和 33 nM 。IC?? & Target

Ki: 8 nM (A 2A receptor), 33 nM (A 1 receptor)[1]体外研究ST3932 is a metabolite of ST1535, acts as an antagonist of adenosine A 2A receptor, with K i s of 8 nM and 33 nM for A

2A and A 1 receptors, respectively. ST3932 inhibits agonist-induced cAMP accumulation with an IC 50 value of 450 nM

[1].

体内研究ST3932 (10, 20, 40 mg/kg, p.o.) antagonizes haloperidol-induced catalepsy, and increases motor activity in mice.

ST3932 (20, 40 mg/kg, i.p.) significantly increases the number of contralateral turns induced by l-DOPA in rats [1].

PROTOCOL

Mice [1] Catalepsy is induced by haloperidol (2 mg/kg) injected intraperitoneally (i.p.) 2.5 h before oral administration of 10,

20, and 40 mg/kg ST1535, ST3932, ST4206 or vehicle. An additional group without haloperidol (control group) with

only vehicle is administered. At time 0 min, successful induction of catalepsy in all animals is checked before

compounds administration, then, catalepsy is scored every 60 min for 3 h. Each mouse is gently placed by its

forepaws on a wire at a height of 4.5 cm. The catalepsy is measured as the time necessary for the animal to step

down with at least one forepaw with a cut off time for each animal of 60 s; after this time the mouse is gently

removed from the wire. Catalepsy is recorded using a video-camera and by an observer who is unaware of the

treatment [1].

Rats [1]

Two weeks after the unilateral 6-OHDA-lesion, rats are screened on the basis of their contralateral rotation in

response to l-DOPA (50 mg/kg i.p.)+benserazide (30 mg/kg i.p.). Rats not showing at least 200 contralateral rotations

during 3 h testing period are eliminated from the study. One week later, rats are administered with the threshold

dose of l-DOPA (3 mg/kg i.p.)+benserazide (6 mg/kg i.p.) in combination with vehicle (10% sucrose and 0.3% Tween

80 in sterile water i.p.) or with ST1535, ST3932 and ST4206 respectively (10, 20 and 40 mg/kg i.p.). l-DOPA is

administered 5 min after vehicle or molecules in study, whereas benserazide is administered 30 min before l-DOPA

injection. Contralateral rotations are measured every 10 min for 2 h by Rotameter system [1].

Animal

Administration [1]Product Data Sheet

Inhibitors ?Agonists ?Screening Libraries

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

REFERENCES

[1]. ST3932, et al. Animal models of Parkinson s disease: Effects of two adenosine A2A receptor antagonists ST4206 and ST3932, metabolites of 2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine (ST1535). Eur J Pharmacol. 2015 Aug 15;761:353-61.

McePdfHeight

Caution: Product has not been fully validated for medical applications. For research use only.

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