Synthesis, pharmacology and therapeutic potential of 10-methoxypyrazinoindoles, partial agonists at the 5HT2C receptor

Article abstract of DOI:10.1016/S0223-5234(97)83976-1

A series of new 10-methoxypyrazino<1,2-a>indoles has been prepared and shown to be 5HT_2C receptor ligands.The studied compounds 10a-j were found to act as partial agonists at the 5HT_2C receptor, binding with high affinity and moderate selectivity versus 5HT_1A and 5HT_2A receptors, but inducing only a submaximal increase in phosphonoinositol formation.Compound 10j was demonstrated to be active in animal models of obsessive-compulsive disorder, depression and panic anxiety. - Keywords: pyrazinoindole; serotonin; 5HT_2C receptor; partial agonist; psychiatric disorder.