Structure-activity relationships among desmethyl derivatives of neuroleptics and antidepressants for substrate specificty to indolethylamine N-methyltransferase from rabbit lung

Psychopharmacol Commun. 1976;2(1):27-38.

Abstract

Desmethylperazine (norperazine) and desmethylprochlorperazine (norprochlorperazine), like nor1- and nor2chlorpromazine, are excellent substrates for indolethylamine N-methyltransferase (NMT) and also inhibit the formation of dimethyltryptamine (DMT) from N-methyl-tryptamine (NMT). Nortriptyline and protriptyline, antidepressant compounds which like NMT contain a secondary amino group, also serve as substrates for INMT but lack in inhibitory effect on DMT formation.

MeSH terms

  • Animals
  • Antipsychotic Agents / pharmacology*
  • Dibenzocycloheptenes / pharmacology*
  • Lung / enzymology*
  • Methyltransferases / metabolism*
  • Nortriptyline / pharmacology*
  • Perazine / analogs & derivatives
  • Prochlorperazine / analogs & derivatives
  • Protriptyline / pharmacology*
  • Rabbits
  • Structure-Activity Relationship

Substances

  • Antipsychotic Agents
  • Dibenzocycloheptenes
  • Protriptyline
  • Perazine
  • Nortriptyline
  • Methyltransferases
  • Prochlorperazine