5-HT2C Receptor Agonist Anorectic Efficacy Potentiated by 5-HT1B Receptor Agonist Coapplication: An Effect Mediated via Increased Proportion of Pro-Opiomelanocortin Neurons Activated
pmid: 23739976
pmc: PMC3717514
5-HT2C Receptor Agonist Anorectic Efficacy Potentiated by 5-HT1B Receptor Agonist Coapplication: An Effect Mediated via Increased Proportion of Pro-Opiomelanocortin Neurons Activated
An essential component of the neural network regulating ingestive behavior is the brain 5-hydroxytryptamine2C receptor (5-HT2CR), agonists of which suppress food intake and were recently approved for obesity treatment by the US Food and Drug Administration. 5-HT2CR-regulated appetite is mediated primarily through activation of hypothalamic arcuate nucleus (ARC) pro-opiomelanocortin (POMC) neurons, which are also disinhibited through a 5-HT1BR-mediated suppression of local inhibitory inputs. Here we investigated whether 5-HT2CR agonist anorectic potency could be significantly enhanced by coadministration of a 5-HT1BR agonist and whether this was associated with augmented POMC neuron activation on the population and/or single-cell level. The combined administration of subanorectic concentrations of 5-HT2CR and 5-HT1BR agonists produced a 45% reduction in food intake and significantly greater in vivo ARC neuron activation in mice. The chemical phenotype of activated ARC neurons was assessed by monitoring agonist-induced cellular activity via calcium imaging in mouse POMC-EGFP brain slices, which revealed that combined agonists activated significantly more POMC neurons (46%) compared with either drug alone (∼25% each). Single-cell electrophysiological analysis demonstrated that 5-HT2CR/5-HT1BR agonist coadministration did not significantly potentiate the firing frequency of individual ARC POMC-EGFP cells compared with agonists alone. These data indicate a functional heterogeneity of ARC POMC neurons by revealing distinct subpopulations of POMC cells activated by 5-HT2CRs and disinhibited by 5-HT1BRs. Therefore, coadministration of a 5-HT1BR agonist potentiates the anorectic efficacy of 5-HT2CR compounds by increasing the number, but not the magnitude, of activated ARC POMC neurons and is of therapeutic relevance to obesity treatment.
- Australian National University Australia
- University of Cambridge United Kingdom
- University of Aberdeen United Kingdom
- University of Edinburgh United Kingdom
proopiomelanocortin, drug antagonism, orga, Male, Pro-Opiomelanocortin, drug combination, feeding behavior, Mice, Transgenic, Eating, Mice, Organ Culture Techniques, male, serotonin 2 agonist, Appetite Depressants, Animals, animal, mouse, Neurons, drug potentiation, C57BL mouse, drug effect, article, Drug Synergism, Feeding Behavior, serotonin 1 agonist, Serotonin 5-HT1 Receptor Agonists, eating, Keywords: anorexigenic agent, Mice, Inbred C57BL, female, Treatment Outcome, Drug Therapy, Combination, Female, nerve cell, metabolism, Serotonin 5-HT2 Receptor Agonists
proopiomelanocortin, drug antagonism, orga, Male, Pro-Opiomelanocortin, drug combination, feeding behavior, Mice, Transgenic, Eating, Mice, Organ Culture Techniques, male, serotonin 2 agonist, Appetite Depressants, Animals, animal, mouse, Neurons, drug potentiation, C57BL mouse, drug effect, article, Drug Synergism, Feeding Behavior, serotonin 1 agonist, Serotonin 5-HT1 Receptor Agonists, eating, Keywords: anorexigenic agent, Mice, Inbred C57BL, female, Treatment Outcome, Drug Therapy, Combination, Female, nerve cell, metabolism, Serotonin 5-HT2 Receptor Agonists
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