Lesogaberan (Synonyms: AZD-3355)

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Lesogaberan (AZD-3355) is a potent and selective GABA_B receptor agonist with an EC₅₀ of 8.6 nM for human recombinant GABA_B receptors. The affinity (K_is) of Lesogaberan for rat GABA_B and GABA_A 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.

The free form of the compound is prone to instability, it is advisable to consider the stable salt form (Lesogaberan hydrochloride) that retains the same biological activity.

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

Lesogaberan Chemical Structure

CAS No. : 344413-67-8

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Other Forms of Lesogaberan:

Lesogaberan napadisylate Get quote
Lesogaberan hydrochloride Get quote

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Description

IC₅₀ & Target

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

Cellular Effect

Cell Line	Type	Value	Description	References
CHO-K1	EC₅₀	8.64 nM Compound: (R)-7	Agonist activity at human recombinant GABABreceptor expressed in CHO-K1 cells assessed as inhibition of intracellular calcium release by FLIPR Agonist activity at human recombinant GABABreceptor expressed in CHO-K1 cells assessed as inhibition of intracellular calcium release by FLIPR	[PMID: 18578471]

In Vitro

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

MedChemExpress (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.

In Vivo

Lesogaberan (AZD3355) potently stimulates recombinant human GABA_B 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].

MedChemExpress (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

Molecular Weight

141.08

Formula

C₃H₉FNO₂P

CAS No.

344413-67-8

SMILES

O=P(O)C[C@H](F)CN

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

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. [Content Brief]

[2]. Tian J, et al. Repurposing Lesogaberan to Promote Human Islet Cell Survival and β-Cell Replication. J Diabetes Res. 2017;2017:6403539. [Content Brief]

Lesogaberan Related Classifications

Metabolic Disease

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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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