Anticonvulsant activity of some 2-aminoethanesulphonic acid (taurine) derivatives

Oja, Simo S.; Kontro, P.; Lindén, Inge‐Britt; Gothóni, G.

doi:10.1016/0014-2999(83)90329-1

Cited by 31 publications

(17 citation statements)

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“…Both taltrimide and the main metabolite phthalimidoethanesulphonamide penetrate well into the brain (Niemi et al, 1982). Taltrimide has a definitive antiepileptic action in many experimental animal models of epilepsy Oja et al, 1983).…”

Section: Discussionmentioning

confidence: 99%

“…La taltrimida oral tiene efectos anticonvulsivos claros en modelos de ataques experimentales agudos (p.ej. ataques al maximo electroshock, ataques secundarios al pentilentetrazol) siendo la ED,, del orden de 10s 100-300 mg/kg en el raton Oja et al, 1983). En esta comunicacion se presentan 10s resultados de un ensayo clinico abierto con la taltrimida en el que se ha estudiado su efecto antiepiICptico, asi como 10s efectos sobre el EEG y su tolerancia en pacientes con epilepsia severa resistente a medicaciones convencionales.…”

Section: Resume Nunclassified

“…maximale Elektroschockkrampfe, Pentylentetrazol-Krampfschwelle). Die ED,, liegt fur Mause in der Groknordnung von 100 bis 300 mg/kg Oja et al, 1983). Diese Mitteilung zeigt Ergebnisse einer offenen klinischen Taltrimid-Studie, in der seine antiepileptische Wirkung, seine Wirkung auf das EEG und die Toleranz bei Patienten mit schwerer gegeniiber konventionellen Medikamenten resistenter Epilepsie untersucht wird.…”

Section: Resume Nunclassified

“…Tdtrimide (phthalimidoethanesulphon-N-isopropylamide) is a lipophilic taurine derivative which penetrates well into the brain . Oral taltrimide has a clear anticonvulsive effect in acute experimental seizure models (e.g., maximal electroshock seizure, pentylentetrazol seizure threshold), with ED,, values on the order of 100-300 mg/kg in mice Oja et al, 1983). This report presents the results of an open clinical trial in which we studied taltrimide's antiepileptic effect, effects on electroencephalogram (EEG), and tolerability, in patients with severe epilepsy resistant to conventional drugs.…”

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Clinical Trial with an Experimental Taurine Derivative, Taltrimide, in Epileptic Patients

et al. 1986

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The antiepileptic effect, effects on EEG, and tolerability of taltrimide, a new taurine derivative, were studied in this open clinical trial in 27 patients with severe epilepsy resistant to conventional drugs. After the 2-week control phase, taltrimide was given in gradually increasing doses up to 4.0 g/day--this dose used for 12 days. Taltrimide was given over 4 weeks and it was gradually withdrawn over 2 weeks. The frequency of seizures increased statistically significantly during the trial with increasing dose of taltrimide and decreased again in the withdrawal phase of the trial. Of six dropouts, one had status epilepticus, and in two patients increased number or severity of seizures necessitated withdrawal of taltrimide. There were no changes in EEG recordings or in laboratory data for safety evaluation. Taltrimide penetrated well through the blood-brain barrier, with the concentration of its main metabolite, phthalimidoethanesulphonamide, in cerebrospinal fluid, about half that in serum. The concentration of phenytoin increased statistically significantly, and there was a significant decrease in serum carbamazepine concentration during the taltrimide treatment. The anticonvulsive effect of taltrimide observed in animal experiments could not be confirmed in this study; in contrast, the seizures increased statistically significantly during taltrimide treatment. The reason for this remains obscure. The doses used, the significant drug interactions, or the patient material seemingly do not explain totally the noticed increase in seizure frequency. One explanation may be that taltrimide has proconvulsive properties in humans.

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confidence: 99%

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Clinical Trial with an Experimental Taurine Derivative, Taltrimide, in Epileptic Patients

et al. 1986

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“…The anti-convulsant activity was evaluated in the subcutaneous pentylentetrazole seizure threshold (PST) test. Phthalimidoethane sulfonamides derivatives of taurine [54] were also prepared and studied ( Table 1). These compounds are of special interest as their sulfone-methylamide, dimethylamide, ethylamide and isopropylamide have almost equal activity.…”

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Taurine Analogues; A New Class of Therapeutics: Retrospect and Prospects

Gupta

Win

Bittner

2005

CMC

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Taurine was discovered more than two hundred years ago from animal sources. It is distributed in both mammals and non-mammals and its content is high in several tissues. For more than a century-and-a-half, taurine was regarded just as an end product of sulfur metabolism. Recently, taurine has been rediscovered and its beneficial effects in processes like epilepsy, hypertension, congestive heart failure and diabetes have been well-documented. It was patented and found some clinical utility, but being an amino acid, therapeutic use confronts limitations like restricted permeability and more. This necessitates the development of pro-drugs (analogues) mainly derivatives of taurine. A large number of taurine derivatives have been reported in the literature with partial to marked activity. Taurine derivatives like taltrimide, acamprosate and tauromustine, are already in the market as anti-convulsant, anti-alcoholic and anti-cancer agents. Many other analogues are effective in experimental models. The in depth analysis of these analogues and their biological actions can provide certain clues for further consideration. In the present review, attempts have been made to provide synopsis, synthesis and symbiosis of chemical and biological actions, which may provide future guidance and facilitate further research in this area. The successful journey of these analogues to clinical utility is a healthy and happy sign and an index of bright future, and we hope that this review will provide enough input to ignite the minds.

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Synthesis and anticonvulsant activity ofN,N-phthaloyl derivatives of central nervous system inhibitory amino acids

Usifoh¹,

Lambert²,

Wouters³

et al. 2001

Arch. Pharm. Pharm. Med. Chem.

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In order to study the influence of the length of the amino acid chain of N,N‐phthaloylamino acid amides as analogues of the former anticonvulsant taltrimide on the seizureantagonizing activity glycine, β‐alanine and γ‐aminobutyric acid (GABA) derivatives were synthesized. The corresponding taurine derivatives were also included. Generally, the glycine‐derived amides showed a higher activity than the β‐alanine and GABA derivatives in the maximal electroshock seizure (MES) test in mice upon intraperitoneal administration. The activity was comparable to the respective taurine derivatives. The N,N‐phthaloyl‐glycine amides were also active in the MES test upon oral administration to rats. No significant activity was noted in the seizure threshold test with subcutaneous pentylenetetrazole. The ED50 of N,N‐phthaloyl‐glycine ethyl amide (4b) in the MES test upon intraperitoneal administration to mice was 19.1 mg/kg. On a molar basis this activity is comparable to the activity of phenytoin with little toxicity in the rotorod test. In conclusion, N,N‐phthaloyl‐glycine amides might represent promising antiepileptic drugs.

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Anticonvulsant activity of some 2-aminoethanesulphonic acid (taurine) derivatives

Cited by 31 publications

References 16 publications

Clinical Trial with an Experimental Taurine Derivative, Taltrimide, in Epileptic Patients

Clinical Trial with an Experimental Taurine Derivative, Taltrimide, in Epileptic Patients

Taurine Analogues; A New Class of Therapeutics: Retrospect and Prospects

Synthesis and anticonvulsant activity ofN,N-phthaloyl derivatives of central nervous system inhibitory amino acids

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