Synthesis of isomeric thienobenzothiazines and their effect on dopamine metabolism in rat brain.
The synthesis of the thieno[2,3-b]-, thieno[3,4-b]- and thieno[3,2-b]benzothiazines with a hydroxyethylpiperazinylpropyl side chain and various 2 substituents is described. The influence of these neuroleptic compounds on dopamine metabolism in vivo is quantitated by determining the rise in homovanillic acid concentrations in rat corpus striatum. Notable differences in activity were found among the isomers, which were useful for structure--activity correlations in the phenothiazine neuroleptics.
D000818:Animals; D014150:Antipsychotic Agents / Q000138:chemical synthesis*; D001921:Brain / Q000187:drug effects* / Q000378:metabolism; D004298:Dopamine / Q000378:metabolism*; D006719:Homovanillic Acid / Q000378:metabolism; D007536:Isomerism; D007700:Kinetics; D008297:Male; D051381:Rats; D013843:Thiazines / Q000138:chemical synthesis* / Q000494:pharmacology
D014150:Antipsychotic Agents; D013843:Thiazines; D004298:Dopamine; D006719:Homovanillic Acid