GABA Modulators

Applications Brivaracetam, is a 4-n-propyl analog of levetiracetam (L331500), and a racetam derivative with anticonvulsant properties.
References Rosenstiel, P., et al.:Neurotherapeutics, 4 (1), 84 (2007); Malawska, B., et al.:, Curr. Opin. Investig. Drugs, 6(7), 740 (2005);

Applications N-Desmethyl Clozapine is a metabolite of Clozapine (C587500). N-Desmethyl Clozapine is a potent, allosteric agonist at human M1 receptors and is able to potentiate hippocampal NMDA receptor currents through M1 receptor activation.
References Sur, C., et al.: Proc. Nat. Acad. Sci. U. S. A., 100, 13674 (2003); Kuoppamaki, M. et al.: Eur. J. Pharm. Mol. Pharm. Sect., 245, 179 (1993); Olessen, O.V., et al.: J. Chromatog., 622, 39 (1993); Pirmohamed, M., et al.: J. Pharmacol. Exp. Ther., 272, 984 (1995)

Applications A deuterated CYP2C19 metabolite of Mephenytoin.
References Karlaganis, G., et al.: Drug Metab. Dispos., 8, 173 (1980)

Applications Antiepileptic, structurally similar to meprobamate.
References Swinyard, E.A., et al.: Epilepsia, 27, 27 (1986), Remmel, R.P., et al.: Ther. Drug Monit., 12, 90 (1990), Sofia, R.D., et al.: Epilepsy Res. Suppl., 3, 103 (1991),

Applications Flumazenil-D5 is a labelled analogue of Flumazenil (F500450), a benzodiazepine antagonist that can prevent or abolish (at the receptor level) the effects of a benzodiazepine.
References Brogden, R. & Goa, K.: Drugs, 35, 448 (1988); Klotz, U. & Kanto, J.: Clin. Pharmacokinet., 14, 1 (1988)

Applications A metabolic intermediate in nucleic acid metabolism.
References Yoon, K., et al.: Nat. Prod. Sci., 14, 254 (2008), Ramazzina, I., et al.: J. Biol. Chem., 283, 23295 (2008), Kim, K., et al.: J. Mol. Biol., 387, 1067 (2009),

Impurity Valproic Acid USP Related Compound A
Applications Diallylacetic Acid (Valproic Acid USP Related Compound A), is a metabolite of Valproic Acid (V094750) as anticonvulsant agents. It can also be used for the synthesis of Velbanamine.
References Liu, H., et al.: Beilstein J. Org. Chem., 9, 983 (2013); Loscher, W., Prog. Neurobiol., 58, 31 (1999); Netzeva, T., et al.: Pharmac. Res., 17, 727 (2000);

Applications A metabolite of Carbamazepine (C175840).Representative lots contained 1-2% carbamazepine by HPLC.
References Bellucci, G., et al.: J. Med. Chem., 30, 768 (1987), Johannessen, S., et al.: Ther. Drug. Monit., 27, 710 (2005), Bialer, M., et al.: Expert Opin. Invest. Drugs, 15, 637 (2006), Williams, J., et al.: J. Clin. Pharmacol., 46, 258 (2006),

Applications An analogue of Carbamazepine (C175840). The toxicity of Cyheptamide in mice and rats is very low, and anticonvulsant activity is marked. Carbamazepine and Cyheptamide have certain stereochemical features in common with Phenytoin.
References Platt, D.S., et al.: Biochem. Pharmacol., 18, 429 (1969), Kraml, M., et al.: Biochem. Pharmacology, 20, 2327 (1971),

Stability Hygroscopic
Applications α/β Mixture of 1-Deoxy-1-[(4R)-4-(2-methylpropyl)-2-oxo-1-pyrrolidinyl]-D-fructopyranose is a glucose conjugate degradation product of pregabalin (P704800), a GABA analogue used as an anticonvulsant.
References Lovdahl, M.J., et al.: J. Pharma. Biomed. Anal., 28, 917 (2002);

Stability Very Hygroscopic
Applications α/β Mixture of 1-Deoxy-1-[(4R)-4-(2-methylpropyl)-2-oxo-1-pyrrolidinyl]-D-tagatopyranose is a galactose conjugate degradation product of pregabalin (P704800), a GABA analogue used as an anticonvulsant.
References Lovdahl, M.J., et al.: J. Pharma. Biomed. Anal., 28, 917 (2002);

Applications A labelled metabolite of Primidone.
References Holler, M., et al.: Biochem. Pharmacol., 33, 1753 (1984), Lafont, O., et al.: Eur. J. Med. Chem., 25, 61 (1990), Fisher, J., et al.: Pharmacol. Res., 26, 207 (1992), Florence, A., et al.: Pharmacol. Res., 14, 259 (1997), El-Masri, H., et al.: Drug Metab. Dispos., 26, 585 (1998),

Applications Flutazolam can be used as analyte in analytical study of development and application of a multi-component LC-MS/MS method for determination of designer benzodiazepines in urine. A benzodiazepine derivative that has sedative, muscle relaxant, anticonvulsant, and anxiolytic effects.
References Pettersson B., et al.: J Chromatgr B, 1035, 104 (2016)

Stability Hygroscopic
Applications Gabapentin is an Amino acid structurally related to γ-Aminobutyric Acid (GABA), designed to cross the blood brain barrier. Used as an anticonvulsant.
References Vollmer, K.-O. et al.: Arzneimittel-Forshc., 36, 830 (1986), Saletu, B., et al.: Int. J. Clin. Pharmacol. Ther. Toxicol., 24, 362 (1986)

Stability Hygroscopic
Applications Gentiopicroside is an anticonvulsant agent present in plant extracts.
References Mahendran, G. et al.: Biomed. Res. Int., 2015, 542385 (2014);