STRUCTURE-ACTIVITY STUDIES OF SOME PUTATIVE OCTOPAMINERGIC AGONISTS IN VENTRAL NERVE CORD OF PERIPLANETA-AMERICANA L

The effect of 2-(arylimino)thiazolidines (AITs), arylethanolamines (AEAs), 2-(aralkylamino)-2-thiazolines (AATs), 2-(arylimino)oxazolidines (AIOs), and related compounds was examined on the adenylate cyclase prepared from ventral nerve cords of the American cockroach Periplaneta americana L. No AEAs had a higher V-max (the maximal response) than OA. However, Various AEAs had higher potency than OA. Greater enzyme activation appeared to be favored by alkyl chain of medium length rather than halogen substitutions in the 2,6-positions of the aromatic ring of AITs. Although the difference of substituents at the phenyl of AAT compounds in V-max was not significant, their potency was of wide difference. AIT and AIO with the 2-Me-4-Cl group had similar V-max, and AIT with the 2,6-Et(2) group had a higher V-max than its AIO analog. The AIOs had higher potency than the AITs, whereas 3,4-dichlorobenzyl AAT was more active than its oxazoline derivative in both V-max and potency. (C) 1994 Academic Press, Inc.