Segontin - Prenylamine

Some inhibitors of the vesicle uptake process are listed in Table IS. The most potent inhibitors are reserpine and related substances. Kinetic studies indicate that reserpine has an affinity for the vesicle uptake sites some 10,000 times higher than that of the catecholamines. Another compound with very high affinity is prenylamine (segontin), which is about 10 times less potent than reserpine. Imi-pramine and chlorpromazine are both active as inhibitors, but are very much less potent on the vesicle system than on the neuronal membrane uptake. Other inhibitors include substances, such as N-ethylmaleimide, which block free sulphydryl groups. The action of such compounds appears to be related to an inhibition of the storage vesicle ATP-ase (Para. 5.2.4). 

---