5-HT3 receptor
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The 5-HT3 receptor is a member of the superfamily of ligand-gated ion channels, a family that also includes the neuronal nicotinic acetylcholine receptors (nAChRs), and the inhibitory neurotransmitter receptors for GABA (both GABAA and GABAC receptors) and glycine.[1][2] The 5-HT3 receptor is expressed throughout the central and peripheral nervous systems and mediates a variety of physiological functions.[2] On a cellular level, it has been shown that postsynaptic 5-HT3 receptors mediate fast excitatory synaptic transmission in rat neocortical interneurons and amygdala, and in ferret visual cortex.[3][4][5] 5-HT3 receptors are also present on presynaptic nerve terminals, where they are thought to mediate or modulate neurotransmitter release.[6][7][8]
Identification of the 5-HT3 receptor did not take place until 1986 because of a lack of selective pharmacological too.[2] However, with the discovery that the 5-HT3 receptor plays a prominent role in chemotherapy- and radiotherapy-induced vomiting, and the concomitant development of selective 5-HT3 receptor antagonists to suppress these side effects, the identification of 5-HT3 receptors in cell lines and native tissues followed naturally.[2] At present, research on 5-HT3 receptor function tends to be hampered by another source. For most of the members of the superfamily of ligand-gated ion channels, a variety of different subunits have been cloned, which has provided insight into the molecular determinants of receptor expression and function. However, the molecular diversity of the 5-HT3 receptor is limited and the molecular makeup of this receptor in the CNS is still unknown. The cloning of a second receptor subunit in 1998[9][10][11] initially seemed to provide some answers regarding the molecular determinants of the functional properties of 5-HT3 receptors in the CNS. In this article, the recent developments in this field are summarized.
[edit] References
- ^ Maricq AV et al. (1991) "Primary structure and functional expression of the 5HT3 receptor, a serotonin-gated ion channel". Science 254: 432–437.
- ^ a b c d Yakel JL (2000). The 5-HT3 receptor channel: function, activation and regulation. In: Endo, M (ed.) Pharmacology of Ionic Channel Function: Activators and Inhibitors, pp. 541–560. Berlin: Springer-Verlag. ISBN 3540661271.
- ^ Férézou I et al. (2002) "5-HT3 receptors mediate serotonergic fast synaptic excitation of neocortical vasoactive intestinal peptide/cholecystokinin interneurons". J Neurosci 22: 7389–7397.
- ^ Sugita S et al. (1992) "5-Hydroxytryptamine is a fast excitatory transmitter at 5-HT3 receptors in rat amygdala". Neuron 8: 199–203.
- ^ Roerig B et al. (1997) "Fast synaptic signaling by nicotinic acetylcholine and serotonin 5-HT3 receptors in developing visual cortex". J Neurosci 17: 8353–8362.
- ^ Rondé P, Nichols RA (1998). "High calcium permeability of serotonin 5-HT3 receptors on presynaptic nerve terminals from rat striatum". J Neurochem 70: 1094–1103.
- ^ Rondé P, Nichols RA (1997). "5-HT3 receptors induce rises in cytosolic and nuclear calcium in NG108-15 cells via calcium-induced calcium release". Cell Calcium 22: 357–365.
- ^ van Hooft JA, Vijverberg HM (2000). "5-HT3 receptors and neurotransmitter release in the CNS: a nerve ending story?" Trends Neurosci 23: 605–610.
- ^ Davies PA et al. (1999). "The 5-HT3B subunit is a major determinant of serotonin-receptor function". Nature 397: 359–363.
- ^ Dubin AE et al. (1999). "The pharmacological and functional characteristics of the serotonin 5-HT(3A) receptor are specifically modified by a 5-HT(3B) receptor subunit". J Biol Chem 274: 30799–30810.
- ^ Monk SA et al. (2001). "Generation of a selective 5-HT3B subunit-recognising polyclonal antibody; identification of immunoreactive cells in rat hippocampus". Neuropharmacology 41: 1013–1016.
