Lesogaberan napadisylate
- CAS No.
- 477956-38-0
- Chemical Name:
- Lesogaberan napadisylate
- Synonyms
- AZD-3355 napadisylate;Lesogaberan napadisylate
- CBNumber:
- CB29624214
- Molecular Formula:
- C13H17FNO5PS
- Molecular Weight:
- 349.31
- MDL Number:
- MFCD34469975
- MOL File:
- 477956-38-0.mol
Lesogaberan napadisylate Chemical Properties,Uses,Production
Uses
Lesogaberan (AZD-3355) napadisylate 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 napadisylate 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 napadisylate inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action[1].
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].
| 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. |
References
[1] Lehmann A, et al. (R)-(3-amino-2-fluoropropyl) phosphinic acid (AZD3355), a novel GABAB receptor agonist, inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action. J Pharmacol Exp Ther. 2009 Nov;331(2):504-12. DOI:10.1124/jpet.109.153593
[2] Tian J, et al. Repurposing Lesogaberan to Promote Human Islet Cell Survival and β-Cell Replication. J Diabetes Res. 2017;2017:6403539. DOI:10.1155/2017/6403539
Lesogaberan napadisylate Preparation Products And Raw materials
Raw materials
Preparation Products
Lesogaberan napadisylate Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Beijing Jin Ming Biotechnology Co., Ltd. | 010-60605840 15801484223; | psaitong@jm-bio.com | China | 29770 | 58 |
| TargetMol Chemicals Inc. | 15002134094 | marketing@targetmol.cn | China | 21630 | 58 |
| Supplier | Advantage |
|---|---|
| Beijing Jin Ming Biotechnology Co., Ltd. | 58 |
| TargetMol Chemicals Inc. | 58 |