N-(3-aminopropyl)-cyclohexylamine blocks facilitation by spermidine of N-methyl-DL-aspartate-induced seizure in mice in vivo.

The facilitating or antagonizing effects of polyamine analogues on N-methyl-DL-aspartate (NMDLA)-induced seizures were investigated using mice. Intracerebroventricular injection of spermidine and spermine, but not putrescine, shortened the latency to appearance of clonic convulsion induced by subcutaneous administration of NMDLA. Injection of N-(3-aminopropyl)cyclohexylamine (APCHA) alone did not affect the NMDLA-induced seizure. However, APCHA, when administered together with spermidine, clearly antagonized the facilitating effect of spermidine on the NMDLA-induced seizure. Another cyclohexylamine derivative, trans-4-methylcyclohexylamine, did not block the effect of spermidine. APCHA also antagonized the facilitation by D-serine of NMDLA-induced seizure, although the blocking effect for D-serine was weaker than that for spermidine. APCHA should be useful as a new tool for pharmacological studies on the neuromodulatory action of polyamines.