5-HT1A RECEPTOR LIGANDS AS POTENTIAL ANTIDEPRESSANTS

Affective diseases belong to the group of mental disorders and are characterized by a complex pathogenesis and etiology. Some of the major biological factors that cause depression include disorders of catecholamine neurotransmission in the brain. Compounds that affect serotonin levels offer a very promising direction in the search for new antidepressants. This paper focuses on a review and structure modification analysis of serotonin 5-HT1A receptor ligands. The 5-HT1A receptor can function both as a presynaptic receptor (autoreceptor) and as a postsynaptic receptor. Its stimulation, depending on the localization, may result in the inhibition of endogenous serotonin secretion into the synaptic cleft or in an increased level of transmission in serotoninergic neurons. 5-HT1AR is recognized as a crucial factor in the pathogenesis and treatment of depression. The main ligands of this receptor are derivatives of arylpiperazines, tetralin and indolylalkylamines. In this review, particular attention has been given to structural modifications that increase affinity and selectivity of the above-mentioned molecules for 5-HT1AR.