2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor
  4. AL-38022A

AL-38022A 是一种强效和具有选择性的 5-HT2 受体激动剂 (Ki ≤2.2 nM)，但对其他 5-HT 受体的亲和力显著降低 (降低 100 倍以上)。AL-38022A 能有效刺激 5-HT2 受体亚型的功能反应，包括胞内 [Ca2+]i 动员和组织收缩，且效力和内在活性相似。AL-38022A 在药物区分实验中可完全泛化 DL-二甲氧基甲基苯异丙胺 (DOM) 刺激。AL-38022A 可用于青光眼的研究。

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AL-38022A

AL-38022A Chemical Structure

CAS No. : 478132-11-5

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AL-38022A 相关抗体

Top Publications Citing Use of Products

查看 5-HT Receptor 亚型特异性产品:

查看所有亚型
5-HT Receptor 5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

AL-38022A is a potent and selective 5-HT2 receptor agonist (Ki ≤2.2 nM), but a significantly lower (>100-fold less) affinity for other 5-HT receptors. AL-38022A potently stimulates functional responses via 5-HT2 receptor subtypes including [Ca2+]i mobilization and tissue contractions with apparently similar potencies and intrinsic activities. AL-38022A fully generalizes to the (±)-1-(2,5-dimethoxy 4-methylphenyl)-2-aminopropane hydrochloride (DOM) stimulus in drug discrimination paradigms. AL-38022A can be used for the glaucoma research[1].

IC50 & Target[1]

Human 5-HT2A Receptor

2.2 nM (Ki)

human 5-HT2B Receptor

2.0 nM (Ki)

Human 5-HT2C Receptor

0.51 nM (Ki)

Human 5-HT2A Receptor

1.68 nM (EC50)

human 5-HT2B Receptor

3.98 nM (EC50)

Human 5-HT2C Receptor

0.3 nM (EC50)

Rat 5-HT2A

0.13 nM (Ki)

Rat 5-HT2A

22.5 nM (EC50)

体外研究
(In Vitro)

AL-38022A 对大鼠 5-HT2A/C、人 5-HT2A、人 5-HT2B 和人 5-HT2C 受体的 Ki 值分别为 0.13 nM、2.2 nM、2.0 nM 和 0.51 nM[1]。
AL-38022A 对大鼠 5-HT2A、大鼠 5-HT2B、大鼠 5-HT2C、人 5-HT2A、人 5-HT2B 和人 5-HT2C 受体的 EC50 值分别为 22.5 nM、1.9 nM、15.7 nM、1.68 nM、3.98 nM 和 0.3 nM。[1]。
AL-38022A 对其他 5-HT 受体的亲和力极低 (>1 µM)，但对 5-HT1A 受体的亲和力适中 (Ki = 294 nM)[1]。

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

AL-38022A 相关抗体:
体内研究
(In Vivo)

AL-38022A (0.03-0.3 mg/kg) 可剂量依赖性地替代 DOM 刺激物，其在雄性 Sprague-Dawley 大鼠体内的 ED50 为 0.05 mg/kg，在恒河猴体内的 ED50 为 0.04 mg/kg[1]。
AL-38022A (0.03-0.3 mg/kg) 在成年恒河猴 (5-8 kg) 中可诱导反应率降低效应，而 MDL 100907 (HY-14940) (0.00032-0.032 mg/kg) 可剂量依赖性地逆转这种效应[1]。

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

Animal Model: Male Sprague-Dawley rats were trained under a variable interval 15-s schedule of reinforcement to build a drug discrimination model[1].
Dosage: 0.032 mg/kg; 0.3 mg/kg
Administration: i.p.; 15 min pre-session
Result: Produced a maximum of 99% DOM-appropriate responding (at 0.3 mg/kg).
Did not produce response rates substantially different from those observed following administration of DOM or saline at doses that engendered ≥80% DOM-appropriate responding.
Animal Model: Two males and two females adult rhesus monkeys were trained under a stimulus-shock termination schedule to build a drug discrimination model[1].
Dosage: 0.01 mg/kg; 0.1 mg/kg; 0.1 mg/kg plus MDL 100907 (0.00032-0.032 mg/kg)
Administration: s.c.; 1 min prior to testing
Result: Occasioned responding on the DOM-associated lever up to a maximum of 100% at a dose of 0.1 mg/kg.
Induced response rate-decreasing effects that were dose-dependently reversed by MDL 100907.
分子量

231.29

Formula

C13H17N3O
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

AL-38022A 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

AL-38022A478132-11-55-HT ReceptorSerotonin Receptor5-hydroxytryptamine Receptor5-HT2 receptor agonist[Ca2+]i mobilizationtissue contractionsglaucomaInhibitorinhibitorinhibit

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产品名称：
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目录号：
HY-182472
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