Structure-activity relationships among desmethyl derivatives of neuroleptics and antidepressants for substrate specificty to indolethylamine N-methyltransferase from rabbit lung.
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.
D000818:Animals; D014150:Antipsychotic Agents / Q000494:pharmacology*; D003986:Dibenzocycloheptenes / Q000494:pharmacology*; D008168:Lung / Q000201:enzymology*; D008780:Methyltransferases / Q000378:metabolism*; D009661:Nortriptyline / Q000494:pharmacology*; D010464:Perazine / Q000031:analogs & derivatives; D011346:Prochlorperazine / Q000031:analogs & derivatives; D011530:Protriptyline / Q000494:pharmacology*; D011817:Rabbits; D013329:Structure-Activity Relationship
D014150:Antipsychotic Agents; D003986:Dibenzocycloheptenes; D011530:Protriptyline; D010464:Perazine; D009661:Nortriptyline; D008780:Methyltransferases; D011346:Prochlorperazine