5-O-Carboxymethyl piperazide derivatives of serotonin: a new class of potent and selective 5-HT1D receptor agonists

New 5-O-carboxymethyl piperazide derivatives of tryptamine ( a-d) have been prepared in 4 steps from serotonin as 5-HT1D receptors agonists. Binding studies with cloned human 5-HT1Dα and 5-HT1Dβ receptors demonstrate that these derivatives are high affinity ligands at both receptor subtypes and inhibition of forskolin mediated cyclase studies with human 5-HT1Dβ and 5-HT1A receptors show that these compounds are very efficient and selective 5-HT1Dβ agonists.