344413-67-8
344413-67-8 structure
- Name: Lesogaberan
- Chemical Name: [(2R)-3-amino-2-fluoropropyl]phosphinic acid
- CAS Number: 344413-67-8
- Molecular Formula: C3H9FNO2P
- Molecular Weight: 141.08100
- Catalog: Signaling Pathways Membrane Transporter/Ion Channel GABA Receptor
- Create Date: 2017-10-29 03:14:46
- Modify Date: 2024-01-11 13:33:38
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Lesogaberan (AZD-3355) is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptors. Binding affinity (Kis) of 5.1 nM and 1.4 μM for rat brain GABAB and GABAA receptors, respectively[1].
| Name | [(2R)-3-amino-2-fluoropropyl]phosphinic acid |
|---|---|
| Synonyms |
Lesogaberan [INN]
(2R)-3-Amino-2-fluoropropylphosphinic acid UNII-4D6Q6HGC7Z |
| Description | Lesogaberan (AZD-3355) is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptors. Binding affinity (Kis) of 5.1 nM and 1.4 μM for rat brain GABAB and GABAA receptors, respectively[1]. |
|---|---|
| Related Catalog | |
| 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] |
| In Vitro | Lesogaberan (3-30 nM) enhances human islet cell proliferation in vitro[2]. Cell Proliferation Assay[2] Cell Line: Human islet cells Concentration: 3, 10, and 30 nM Incubation Time: 4 days Result: 3 nM had a small but nonsignificant promitotic effect, 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. |
| 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 |
| Molecular Formula | C3H9FNO2P |
|---|---|
| Molecular Weight | 141.08100 |
| Exact Mass | 141.03500 |
| PSA | 86.79000 |
| LogP | 0.45050 |