Neuron
Article5-HT3 receptors mediate rapid responses in cultured hippocampus and a clonal cell line
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2020, Handbook of Behavioral NeuroscienceCitation Excerpt :Interestingly, Nash & Brodkin, 1991 reported a lack of effect of ketanserin on striatal dopamine release stimulated by intrastriatal infusions of MDMA. Distinct from the other 5-HT receptors, the 5-HT3 receptor gates a cation permeable ion channel (Derkach, Surprenant, & North, 1989; Yakel & Jackson, 1988). The highest expression of these receptors has been reported in the brainstem (Gehlert, Gackenheimer, Wong, & Robertson, 1991; Parker, Barnes, Ge, Barber, & Barnes, 1996).
The antidepressant bupropion is a negative allosteric modulator of serotonin type 3A receptors
2017, NeuropharmacologyCitation Excerpt :The assembly of five 5-HT3 subunits constitutes a central ion-channel which is permeable to the monovalent cations, Na+ and K+ (Yang, 1990), and the divalent cation Ca++ (Hargreaves et al., 1994). The 5-HT3R activation-induced influx of cations via its intrinsic ion channel results in a rapid depolarization of the neuronal cell membrane (Yakel and Jackson, 1988). 5-HT3R mediated depolarization of the presynaptic nerve terminal modulates the release of a spectrum of neurotransmitters, including dopamine (DA), GABA, acetylcholine (ACh), glutamate and substance P (Fink and Gothert, 2007; Giovannini et al., 1998; Koyama et al., 2000; Wang et al., 1998), whereas postsynaptically, it evokes excitatory fast synaptic neurotransmission (Sugita et al., 1992).