The
taurine derivatives, 2-phthalimidoethanesulfon-N-isopropylamide (
taltrimide) and
2-phthalimidoethanesulfonamide (MY-103), were tested intraperitoneally against genetic and experimentally produced
seizures. In the genetically seizure-susceptible rat,
taltrimide raised the threshold for audiogenic
seizures and decreased seizure severity.
MY-103 decreased seizure intensity in maximally-responding animals, but was otherwise without effect on sound-induced
seizures.
Taltrimide had a greater potency against maximal as compared to minimal
seizures, and, at 150 mg/kg, it completely suppressed clonic and
myoclonic seizures induced by intracerebroventricular
injections of
guanidinoethane sulfonate (9.2 ?mol) in rats.
MY-103, at doses up to 300 mg/kg, was ineffective against
guanidinoethane sulfonate-induced
seizures. In pentylene
tetrazole-induced
seizures in the rat,
taltrimide (300 mg/kg) raised the threshold for
seizures from 80 mg/kg pentylene
tetrazole to 115 mg/kg.
Taltrimide also raised the threshold for lead-exacerbated pentylene
tetrazole-induced
seizures.
Taurine, being more lipophobic than
taltrimide, was ineffective on intraperitoneal administration against pentylene
tetrazole-induced
seizures. The more lipophilic
beta-alanine (8 mmol/kg) raised pentylene
tetrazole-seizure threshold on intraperitoneal administration. Thus, lipophilic phthalimido analogs of
taurine are effective on peripheral administration against both genetic and experimentally-induced
seizures.