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Losigamone

Catalog No. T27845   CAS 112856-44-7
Synonyms: ADD-137022, AO33, AO 33, ADD 137022, AO-33, ADD137022;Losigamone

Losigamone (AO-33) is an agonist of GABA receptor and can be used in studies about the treatment of partial seizures.

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Losigamone Chemical Structure
Losigamone, CAS 112856-44-7
Pack Size Availability Price/USD Quantity
1 mg In stock $ 75.00
5 mg In stock $ 179.00
10 mg In stock $ 270.00
25 mg In stock $ 506.00
50 mg In stock $ 680.00
100 mg In stock $ 990.00
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Purity: 100%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Losigamone (AO-33) is an agonist of GABA receptor and can be used in studies about the treatment of partial seizures.
In vivo Losigamone (AO-33) was tested in 52 healthy male volunteers in 4 placebo-controlled phase I studies. In the study 1 single dose of 100, 200, 300, 500, 700, and 1,000 mg losigamone was given as a fast-releasing capsule to 12 subjects. The pharmacokinetics of losigamone measured after administration of 100, 300, and 700 mg was linear. Clearance and t1/2 were about 350 ml/min and 4 h, respectively, the Cmax values of 0.7, 1.7, and 4.4 micrograms/ml were reached after 2.5 h. In study, 2,500 mg losigamone was given as a fast-release capsule for 6 days (t.i.d.) to 12 subjects. There was a small but statistically significant decrease for the AUC but no change in t1/2, Cmax, or tmax comparing single dose kinetics on days 1 and 8. There appeared to be no change in caffeine clearance on days 1 and 9. Study 2 was repeated in 20 volunteers with a film-coated tablet. Pharmacokinetic parameters appeared to be unaffected by this change in galenical formulation. In the study 4 daily doses of 400, 1,200, and 1,800 mg losigamone were given 28 days to 24 subjects. The kinetics of caffeine and antipyrine were compared on days 1 and 29. With the exception of t1/2 for antipyrine in the 400 mg group there was no statistically significant change in pharmacokinetic parameters. Generally, losigamone was well tolerated and no serious adverse side effects occurred. In some subjects, a reversible increase in transaminases was observed.[1]
Synonyms ADD-137022, AO33, AO 33, ADD 137022, AO-33, ADD137022;Losigamone
Molecular Weight 254.67
Formula C12H11ClO4
CAS No. 112856-44-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences and Literature

1. Biber A, et al. Pharmacokinetics of losigamone, a new antiepileptic drug, in healthy male volunteers. Int J Clin Pharmacol Ther. 1996;34(1):6-11. 2. Xiao Y, et al. Losigamone add-on therapy for partial epilepsy. Cochrane Database Syst Rev. 2012;(6):CD009324. 3. Dimpfel W, et al. Effects of the anticonvulsant losigamone and its isomers on the GABAA receptor system. Epilepsia. 1995;36(10):983-989. 4. Gebhardt C, et al. The antiepileptic drug losigamone decreases the persistent Na+ current in rat hippocampal neurons. Brain Res. 2001;920(1-2):27-31. 5. Xiao Y, et al. Losigamone add-on therapy for partial epilepsy. Cochrane Database Syst Rev. 2015;(12):CD009324.

Related compound libraries

This product is contained In the following compound libraries:
Membrane Protein-targeted Compound Library Neurotransmitter Receptor Compound Library

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Keywords

Losigamone 112856-44-7 Membrane transporter/Ion channel Neuroscience GABA Receptor ADD-137022 ADD137022 AO33 AO 33 ADD 137022 AO-33 ADD137022;Losigamone inhibitor inhibit

 

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