1. GPCR/G Protein
  2. Adenosine Receptor
  3. ST3932

ST3932 是 ST1535 的代谢物,为 adenosine A2A 受体拮抗剂,对 A2A 和 A1 受体的 Ki 值分别为 8 nM 和 33 nM。

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ST3932 Chemical Structure

ST3932 Chemical Structure

CAS No. : 1246018-21-2

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Top Publications Citing Use of Products
  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

ST3932 is a metabolite of ST1535, acts as an antagonist of adenosine A2A receptor, with Kis of 8 nM and 33 nM for A2A and A1 receptors, respectively.

IC50 & Target

Ki: 8 nM (A2A receptor), 33 nM (A1 receptor)[1]

体外研究
(In Vitro)

ST3932 is a metabolite of ST1535, acts as an antagonist of adenosine A2A receptor, with Kis of 8 nM and 33 nM for A2A and A1 receptors, respectively. ST3932 inhibits agonist-induced cAMP accumulation with an IC50 value of 450 nM[1].

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

体内研究
(In Vivo)

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].

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

分子量

288.31

Formula

C12H16N8O

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

纯度 & 产品资料
参考文献
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[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].

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

参考文献

ST3932 相关分类

  • 摩尔计算器

  • 稀释计算器

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HY-112840
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