5-HT receptors subtypes

Deakin, JFW, Graeff, FG and Guimaraes, FS (1992) 5-HT receptor subtypes and the modulation of aversion. In Central Serotonin Receptors and Psychotropic Drugs (Eds Marsden, CA and Heal, DJ), Blackwell Scientific Publications, Oxford, pp. 147-174. 

Three families of serotonin receptor, the 5-HT family, the 5-HT2 family and the family that includes the 5-HT4, 5-ht6 and 5-HT7 receptors represent the three major classes of 5-HT receptor that are G-protein-coupled receptors (Ch. 19). The 5-HT3 receptor is a ligand-gated ion channel and is a separate family. Although each serotonin receptor can be potently activated by 5-HT, differences insignal transduction mechanisms,neuroanatomical distribution and affinities for synthetic chemicals create opportunities for drug discovery and make each 5-HT receptor subtype a potential therapeutic target. 

The selectivity for 5-HT4 vs. other 5-HT receptor subtypes was examined in a set of radioligand binding assays available at the time (5-HT1A, 5-HT1D, 5-HT2A., 5-HT2c and 5-HT3) for some of the new compounds. While most derivatives exhibited a high selectivity for 5-HT4 vs. 5-HT3 receptors, structural adjustments of 5 led to profound effects on selectivity vs. other 5-HT receptors. 

Appel JB, Callahan PM. (1989). Involvement of 5-HT receptor subtypes in the discriminative stimulus properties of mescaline. Eur J Pharmacol. 159(1) 41-46. 

Table 6.1. Distribution and selectivity of drugs for 5-HT receptor subtypes 5-HTj receptors...

Figure 6.2. Diagrammatic representation of the 5-HT3 receptor. The 5-HT3 receptor is distinct from the other 5-HT receptor subtypes, in that it is a ligand gated ion channel that is permeable to sodium and potassium. The 5-HT3 receptor is structurally similar to the nicotinic acetylcholine receptor and is composed of five sub-units. Two sub-units have been cloned, 5-HT3A and 5-HT35, and homomeric (5-HT3A) and heteromeric (5-HT3a/5-HT3b) forms of the receptor have both been...

Nevertheless, despite these cautions, there is a growing body of information which implicates different 5-HT receptor subtypes in a variety of physiological and pharmacological responses and these will be briefly reviewed (see Table 6.2). 

The molecular characterization of different 5-HT receptor subtypes has simplified fhe elucidation of gene transcription, mRNA processing, and translation as well as intracellular trafficking and posttranslational modification relevant to synaptic and postreceptor signaling. Transcriptional control regions... 

Cowen PJ Neuroendocrine measures of 5-HT receptor subtype function in depression, in Serotonin, CNS Receptors and Brain Function [Advances in the Biosciences, Vol 85). Edited by Bradley PB, Handley SL, Cooper SJ, et al. Oxford, England, Pergamon, 1992, pp 287-296... 

Mitsushima D, Hei DL, Terasawa E GABA is an inhibitory neurotransmitter restricting the release of luteinizing hormone-releasing hormone before the onset of puberty. Proc Natl Acad Sci USA 91 395-399, 1994 Miura N, Nakata N, Tanaka Y, et al Improving effects of FG-7080 a serotonin reuptake inhibitor on scopolamine-induced performance deficits of memory tasks in rats. Jpn J Pharmacol 62 203-206, 1993 Mizuta T, Segawa T Chronic effects of imipramine and lithium on 5-HT receptor subtypes in rat frontal cortex, hippocampus and choroid plexus quantitative receptor autoradiographic analysis. Jpn J Pharmacol 50 315-326, 1989... 

Banasr, M., , M., Printemps, R., Daszuta, A. (2004). Serotonin-induced increases in adult cell proliferation and neurogenesis are mediated through different and common 5-HT receptor subtypes in the dentate gyrus and the subventricular zone. Neuropsychopharmacology, 29, 450-60. 

Courade, J. P., Chassaing, C., Bardin, L., Alloui, A., Eschalier, A. 5-HT receptor subtypes involved in the spinal antinociceptive effect of acetaminophen in rats, Eur. J. Pharmacol. 2001, 432, 1-7. 

Monteau R, Pasquale ED, Hilaire G (1994) Further evidence that various 5-HT receptor subtypes modulate central respiratory activity in vitro studies with SR 46349B. Eur J Pharm 259 71-74... 

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