Targeting 5-HT receptors for the treatment of obesity

Are the Hydantoin-1,3,5-triazine 5-HT6R Ligands a Hope to a Find New Procognitive and Anti-Obesity Drug? Considerations Based on Primary In Vivo Assays and ADME-Tox Profile In Vitro

“…The 5-HT 6 receptor blockade has been implicated in the reduction of food intake, body weight, visceral adiposity, and insulin resistance [30]. 5-HT 6 receptor antagonists block the serotonin-dependent activation of γ-aminobutyric acid (GABA) neurons, which results in a reduction of inhibitory effects of GABA on proopiomelanocortin neurons in the arcuate nucleus, with the subsequent inhibition of hunger signal induction [31]. Our previous results indicated that an administration of KMP-10 to rats in the overeating model caused a significantly lower increase of body mass when compared to that of the control group [19].…”

Ondansetron attenuates co-morbid depression and anxiety associated with obesity by inhibiting the biochemical alterations and improving serotonergic neurotransmission

“…Reduced level of serotonin is majorly associated with depression (Owens and Nemeroff, 1994). Serotonin also plays a crucial role in obesity as it controls appetite (Lam et al, 2010;Sargent and Henderson, 2011). An important finding of serotonin remains the regulation of insulin secretion by beta-pancreatic cells (Paulmann et al, 2009).…”

Prenatal exposure to selective serotonin reuptake inhibitors and childhood overweight at 7 years of age

“…Long-term effects of prenatal SSRI exposure is an important area of concern given the key role serotonin (5-HT) plays as a neurotransmitter within the central nervous system, affecting neurogenesis, migration and differentiation of neurons in the fetal brain [3][4][5]. The importance of the serotonergic system in regulating food intake and body weight places particular interest in the potential long-term effects of prenatal SSRI exposure on child growth [6][7][8].…”

“…The lack of inclusion of data on postnatal factors such as the child's diet, energy intake and physical activity may constitute a study limitation. However, these factors lie in the predicted pathway between prenatal SSRI exposure and childhood overweight, given the involvement of the serotonergic system in the regulation of appetite (influencing energy intake [6][7][8]) as well as motor control (influencing physical activity in later life [49]).…”