Introduction: The 5-HT(1A) receptors are implicated in mood disorders (anxiety, depression), in cognition, and in modulation of pain. Nearly 30 years of research in this field, there is still interest in developing new chemical entities capable of 5-HT(1A) receptor activation or blockade.
Areas covered: This review article will highlight and review the research advances published in the patent literature between January 2007 and December 2011, giving emphasis to the medicinal chemist's standpoint. Literature search methodology included search in Scifinder and PubMed Databases and browsing clinicaltrials.gov website.
Expert opinion: Almost no new therapeutic applications have been proposed for molecules targeting the 5-HT(1A) receptor, during the years covered by the present review. The discovery that stimulation of 5-HT(1A) receptor can promote neurogenesis will likely renew the interest for selective 5-HT(1A) receptor agonists as therapeutics to replace neural populations damaged by disease or injury.