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

Lesogaberan (Synonyms: AZD-3355)

Cat. No.: HY-10061
Handling Instructions

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.

For research use only. We do not sell to patients.

Lesogaberan Chemical Structure

Lesogaberan Chemical Structure

CAS No. : 344413-67-8

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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].

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]

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.
Molecular Weight

141.08

Formula

C₃H₉FNO₂P

CAS No.

344413-67-8

SMILES

O=P(C[[email protected]](F)CN)O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

References
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Keywords:

LesogaberanAZD-3355AZD3355AZD 3355GABA ReceptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid ReceptorIsletCellSurvivalGastroesophagealrefluxdiseaseGERDdiabeteGABABInhibitorinhibitorinhibit

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