ChemInform Abstract: 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 (6a-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.