1. GPCR/G Protein
  2. Adenosine Receptor
  3. ST4206

ST4206 

Cat. No.: HY-U00341
Handling Instructions

ST4206 is a potent and orally active adenosine A2A receptor antagonist, with Kis of 12 nM and 197 nM for adenosine A2A receptor and adenosine A1 receptor, respectively. ST4206 has the potential for Parkinson׳s disease research.

For research use only. We do not sell to patients.

ST4206 Chemical Structure

ST4206 Chemical Structure

CAS No. : 1246018-36-9

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Description

ST4206 is a potent and orally active adenosine A2A receptor antagonist, with Kis of 12 nM and 197 nM for adenosine A2A receptor and adenosine A1 receptor, respectively. ST4206 has the potential for Parkinson׳s disease research[1].

IC50 & Target

Ki: 12 nM (adenosine A2A receptor), 197 nM (adenosine A1 receptor)[1]

In Vitro

ST4206 inhibits agonist-induced cAMP accumulation with an IC50 of 990 nM[1].

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

In Vivo

ST4206 (10, 20, and 40 mg/kg, p.o.) antagonizes haloperidol-induced catalepsy, and increases motor activity in a dose dependent manner in mice.
ST4206 (20 and 40 mg/kg) significantly increases the number of contralateral turns induced by l-DOPA in rats[1].
ST4206 is orally active at concentrations of 10, 20, and 40 mg/kg in haloperidol-induced catalepsy in mice[2].

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

Molecular Weight

286.29

Formula

C₁₂H₁₄N₈O

CAS No.

1246018-36-9

SMILES

CC(CCC1=NC(N)=C2N=C(N3N=CC=N3)N(C)C2=N1)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

References
Animal Administration
[1]

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.
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.

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

References
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Keywords:

ST4206ST 4206ST-4206Adenosine ReceptorP1 receptorAdenosine A2AParkinson?s diseasePD cAMP accumulationInhibitorinhibitorinhibit

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