Trends in Pharmacological Sciences
CommentA proposed new nomenclature for 5-HT receptors
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Cited by (556)
“Selective” serotonin 5-HT<inf>2A</inf> receptor antagonists
2022, Biochemical PharmacologyCentral 5-HT receptors and their function; present and future
2020, NeuropharmacologyCitation Excerpt :Thirteen of the 14 5-HT receptor subtypes are classical metabotropic G-protein coupled receptors which couple to canonical signalling pathways, that elicit the expected second messenger cascades (Table 1). The 5-HT1 receptor family, comprises 5-HT1A, 5-HT1B, 5-HT1D, 5-ht1e, and 5-HT1F subtypes (5-HT1C subsequently being re-designated 5-HT2C; Humphrey et al., 1993), and these are Gi-coupled and inhibit adenylate cyclase and decrease cAMP formation (Masson et al., 2012). These receptors also indirectly open G-protein-gated inwardly rectifying potassium channels (GIRKs) to hyperpolarise neurons, and inhibit the opening of voltage-gated calcium channels (e.g. Montalbano et al., 2015).
Distribution of 5-HT receptors in the central nervous system: an update
2020, Handbook of Behavioral NeuroscienceCitation Excerpt :Since this receptor was also labeled by [3H]-5-HT, but not [3H]-spiperone, they were initially identified as being similar to other 5-HT1 receptors and thus called 5-HT1C (Hoyer et al.1985b; Pazos et al., 1987, 1984; Pazos & Palacios, 1985); see Palacios et al. (2017) for a historical overview. When the receptor was cloned several years later, the 5-HT1C was recognized to belong structurally to the 5-HT2 class (Hoyer, 1988) and was thus renamed 5-HT2C (Hoyer et al., 1994; Humphrey et al., 1993). Incidentally, the 5-HT2A receptor was cloned by homology to 5-HT2C (Pritchett et al., 1988).
Serotonin receptors nomenclature
2019, The Serotonin System: History, Neuropharmacology, and PathologyNew therapeutic opportunities for 5-HT<inf>2C</inf> receptor ligands in neuropsychiatric disorders
2016, Pharmacology and TherapeuticsCitation Excerpt :The 5-HT2Rs form a closely-related subgroup of G-protein coupled receptors (GPCR) and depict the typical heptahelical structure of an integral membrane protein. The 5-HT2Rs are currently classified as 5-HT2A, 5-HT2B and 5-HT2C subtypes (Humphrey et al., 1993; Hoyer et al., 1994). The amino acid sequences of the 5-HT2Rs share a high degree (>70%) of identity within the transmembrane segments (Hannon & Hoyer, 2008).
Identification of Spiro[chromene-2,4′-piperidine]s as Potent, Selective, and G<inf>q</inf>-Biased 5-HT<inf>2C</inf> Receptor Partial Agonists
2024, ACS Medicinal Chemistry Letters