Recent studies demonstrated that 5-HT-1a or 4a receptor agonists (8-OH-DPAT, BIMU8 respectively) can reverse µ-opioid receptor (µ-OR) evoked respiratory depression. Here, we assessed if 8-OH-DPAT could rescue the severe disturbances in the cardiovascular system caused by intravenous in...
F11440 (4-methyl-2-[4-(4-(pyrimidin-2-yl)-piperazino)-butyl]-2H, 4H-1,2,4-triazin-3,5-dione) was the outcome of a research effort guided by the hypothesis that the magnitude of the intrinsic activity of agonists at 5-HT1A receptors determines the magnitude of their antidepressant and...
During recent years a multiplicity of 5-HT receptor subtypes has been characterized by pharmacological studies as well as by molecular cloning of the receptors. Serotonin (5-HT) is a neurotransmitter detectable in most organisms, ranging from highly specialized humans to species with a primitive CNS...
Serotonin 5-HT1A receptor biased agonists display differential anxiolytic activity in a rat social interaction model. ACS Chem. Neurosci. 10, 3101–3107 (2019). 54. Banasr, M., Hery, M., Printemps, R. & Daszuta, A. Serotonin-induced increases in adult cell proliferation and neurogenesis ...
We have inactivated the gene encoding the 5-HT1A receptor in mice and found that receptor-deficient animals have an increased tendency to avoid a novel and fearful environment and to escape a stressful situation, behaviors consistent with an increased anxiety and stress response. Based on the role...
The novel 5-HT1A receptor agonist, NLX-112, fits the criteria for a potentially superior anti-LID therapy. Unlike previous 5-HT1A receptor agonists, NLX-112 (a.k.a. befiradol or F13640) is a potent (nanomolar affinity), 5-HT1A receptor ‘full’ agonist and highly selective (>1000-fold...
Together, our results confirm previous observations that 5-HT1Areceptors play a pivotal role in alcohol drinking behavior and the associated emotional and neurogenic impairments, and suggest that 5-HT1Apartial agonists represent a promising treatment strategy for alcohol abuse....
The hypothesis that antianxiety or antidepressant agents (e.g., 5-HT1A agonists, 5-HT uptake blockers) exert their clinical actions via enhancement of serotonergic neurotransmission due to desensitization of 5-HT1A autoreceptors predicts that regulation of this receptor plays a crucial role in the ...
The aim of this study was to investigate the cardiovascular effects of the 5-HT 1A receptor agonists, 8-OH-DPAT (8-hydroxy-2-(di-n-propylamino)tetralin), flesinoxan and 5-carboxamidotryptamine (5-CT) following injection into the dorsal raphe nucleus of conscious rats. 8-OH-DPAT (0.5–...
In non-human animals, decreasing serotonin levels via 5-HT1A receptor agonists diminishes female sexual receptivity and induces aggression towards male mates6,8. The G allele of the C-1019G (rs6295) polymorphism, which leads to higher expression of 5-HT1A gene, is related to decreased comfort ...