SYNTHESIS, PHARMACOLOGY AND THERAPEUTIC POTENTIAL OF 10-METHOXYPYRAZINO[1,2-A]INDOLES, PARTIAL AGONISTS AT THE 5HT(2C) RECEPTOR

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 wer e found to act as partial agonists at the 5HT(2C) receptor, binding wi th high affinity and moderate selectivity versus 5HT(1A) and 5HT(2A) r eceptors, but inducing only a submaximal increase in phosphoinositol f ormation. Compound 10j was demonstrated to be active in animal models of obsessive-compulsive disorder, depression and panic anxiety.