Synthesis and Pharmacological Properties of 1-Aryl-4-[4-(naphthalimidoalkyl)]piperazines

The anxiolytic effects of buspirone (I) and its analogs (giperone, ipsapirone, campirone) are related mostly to the ability of these compounds to interact with serotonin (5-HT1A) receptors in the central nervous system [1]. As is known, the serotoninergic system is also involved in the regulation of appetite [2]. For example, 8-OH-DPAT (a selective agonist of 5-HT1A receptors) increases the amount of consumed food in rats [3]. It was suggested that the increase in food intake caused by small doses of 5-HT1A receptor agonists is related to the activation of serotonin autoreceptors in the dorsal raphe nucleus [2, 4]. In particular, cyproheptadine (II) increases appetite, probably by acting upon serotonin receptors in the hypothalamus, while the anorexigenic effect of fenfluramine (III) is explained by inhibition serotonin reuptake and the resulting activation of serotonin metabolism in the brain tissues [5].