1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. GABA Receptor
  3. Lesogaberan

Lesogaberan  (Synonyms: AZD-3355)

目录号: HY-10061
产品使用指南

Lesogaberan (AZD-3355) 是一种有效的选择性 GABAB 受体激动剂,对人重组 GABAB 受体的 EC50 为 8.6 nM。通过脑膜中 [3H]GABA 结合位移测量,Lesogaberan 对大鼠 GABAB 和 GABAA 受体的亲和力 (Kis):分别为 5.1 nM 和 1.4 μM。Lesogaberan 通过外周作用模式抑制短暂的食管下括约肌松弛。

该游离形式化合物不稳定,推荐具有相同生物学活性的稳定盐形式 Lesogaberan hydrochloride

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Lesogaberan Chemical Structure

Lesogaberan Chemical Structure

CAS No. : 344413-67-8

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  • 生物活性

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  • 参考文献

生物活性

Lesogaberan (AZD-3355) is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptors. The affinity (Kis) of Lesogaberan for rat GABAB and GABAA receptors, as measured by displacement of [3H]GABA binding in brain membranes: 5.1 nM and 1.4 μM, respectively. Lesogaberan inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action[1].

IC50 & Target

Ki: 5.1±1.2 nM (rat GABAB), 1.4±0.3 μM (rat GABAA)[1]
EC50: 8.6±0.77 nM (human GABAB receptor)[1]

体外研究
(In Vitro)

Lesogaberan (3-30 nM) enhances human islet cell proliferation in vitro[2].

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

Cell Proliferation Assay[2]

Cell Line: Human islet cells
Concentration: 3, 10, and 30 nM
Incubation Time: 4 days
Result: Had a small but nonsignificant promitotic effect at 3 nM, while treatment at higher dosages (10 and 30 nM) led to a 2-3-fold increase in proliferation relative to that of islets cultured in medium alone.
体内研究
(In Vivo)

Lesogaberan (AZD3355) potently stimulates recombinant human GABAB receptors and inhibits transient lower esophageal sphincter relaxation (TLESR) in dogs, with a biphasic dose-response curve[1].
Oral Lesogaberan (0.08 mg/mL; 48 hours) protects human islet β-cells from apoptosis in islet grafts in mice[2].
Lesogaberan (7 μmol/kg) shows high oral availability (88% in the dog and 100% in the rat) and relatively low systemic clearance in female SpragueDawley rats[1].

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

Animal Model: Diabetic NOD/scid mice were implanted with human islets[2]
Dosage: 0.08 mg/mL
Administration: Oral feeding; 48 hours
Result: Significantly reduced the percentages of apoptotic islet cells and increased the frequency of insulin+ β-cells in human islet grafts.
Animal Model: Female Sprague Dawley rats[1]
Dosage: 7 μmol/kg (Pharmacokinetic Analysis)
Administration: Oral
Result: High oral availability (88% in the dog and 100% in the rat) and relatively low systemic clearance. Plasma protein binding was 1% in rat and human plasma.
Clinical Trial
分子量

141.08

Formula

C3H9FNO2P

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
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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.

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