RESUMO
Organophosphate (OP) pesticides, monocrotophos (MCP), dichlorvos (DDVP) and phosphamidon significantly inhibit both MAO-A and MAO-B activities in rat brain mitochondria. The inhibition of MAO-A by MCP is reversible whereas the inhibition by DDVP and phosphamidon is irreversible. MAO-B is inhibited irreversibly by all these organophosphates suggesting that the mechanism of action of OP pesticides is through phosphorylation of serine residue present in active centre of MAO.
Assuntos
Animais , Benzilaminas/metabolismo , Encéfalo/enzimologia , Inseticidas/metabolismo , Masculino , Mitocôndrias/enzimologia , Monoaminoxidase/metabolismo , Compostos Organofosforados , Oxirredução , Ratos , Ratos Wistar , Serotonina/metabolismoRESUMO
Chlorpromazine, imipramine and amphetamine at a concentration of 0.66, 1.33 and 13.3 x 10(4) M in vitro inhibited acetyl cholinesterase activity by 16, 23 and 31% respectively in rat brain mitochondria. No change in enzyme activity was induced by these drugs in vivo. There is little cholinergic facilitation through acetylcholinesterase inhibition in the presence of psychoactive drugs.
Assuntos
Acetilcolinesterase/metabolismo , Anfetamina/farmacologia , Animais , Encéfalo/enzimologia , Clorpromazina/farmacologia , Inibidores da Colinesterase/farmacologia , Imipramina/farmacologia , Cloreto de Lítio/farmacologia , Masculino , Mitocôndrias/efeitos dos fármacos , Parassimpatolíticos/farmacologia , Psicotrópicos/farmacologia , Ratos , Ratos EndogâmicosRESUMO
The psychoactive drugs imipramine, chlorpromazine and lithium chloride inhibit tryptamine tetrazolium reductase activity in vitro by 68, 60 and 33% respectively at a concentration of 1 x 10(-3) M while amphetamine negligibly inhibits the enzyme activity. No change in enzyme activity is observed in vivo.
Assuntos
Animais , Encéfalo/efeitos dos fármacos , Cloretos/farmacologia , Clorpromazina/farmacologia , Dextroanfetamina/farmacologia , Imipramina/farmacologia , Lítio/farmacologia , Cloreto de Lítio , Masculino , Oxirredutases atuantes sobre Doadores de Grupo CH-NH/antagonistas & inibidores , Psicotrópicos/farmacologia , RatosRESUMO
Of the organophosphate pesticides studied, dichlorvos inhibited significantly both, phosphate-activated glutaminase and alpha-keto acid-activated glutaminase, while monocorotophos inhibited moderately alpha-keto acid activated glutaminase in rat brain. Phosphamidon inhibited glutamine synthetase activity negligibly.