Benzo[<i>b</i>]thiophene derivatives. XX. The sulfur isostere of 5,6‐Dihydroxytryptamine

Abstract

Abstract 3β‐Aminoethyl‐5,6‐dihydroxybenzo[ b ]thiophene, the sulfur bioisostere of 5,6‐dihydroxytryptamine, a selective neurotoxin, has been synthesized and shown to have significant effect on biogenic amine levels both centrally and peripherally. A derivative, 3β‐aminoethyl‐5,6‐isopropylidenedioxybenzo[ b ]thiophene, showed significant but opposite activity. The syntheses and preliminary pharmacology are reported.