Trends in Pharmacological Sciences
Tips reviewsMolecular pharmacology and biology of 5-HT1C receptors
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Cited by (225)
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 PathologyAtorvastatin evokes a serotonergic system-dependent antidepressant-like effect in mice
2014, Pharmacology Biochemistry and BehaviorCitation Excerpt :It can be highlighted by studies that showed a reduced cerebrospinal fluid concentration of 5-HT and its main metabolite 5-hydroxyindoleacetic acid (5-HIAA) in postmortem brain tissue of depressed or suicidal patients (Asberg et al., 1976; Roy et al., 1989). 5-HT can interact with multiple receptors, and to date seven families have been characterized (5HT1R–5HT7R), and with exception to 5HT3R that is a ligand-gated ion channel, they are all G-protein-coupled receptors (Barnes and Sharp, 1999; Hoyer, 1988; Kriegebaum et al., 2010). The 5-HT1A receptor subtype is the best studied (Glennon and Dukat, 1991; Pessoa-Mahana et al., 2003), and it is generally accepted to be involved in psychiatric disorders such as anxiety and depression (Blier and Abbott, 2001).
Multiple receptors contribute to the behavioral effects of indoleamine hallucinogens
2011, NeuropharmacologyCitation Excerpt :This hypothesis was proposed prior to the discovery of 5-HT2C sites, and was partially based on evidence demonstrating that ketanserin and pirenperone block the behavioral effects of hallucinogens in several animal paradigms. However, ketanserin and pirenperone exhibit less than a 100-fold difference in affinity for 5-HT2A receptors versus 5-HT2C receptors, and therefore display only moderate selectivity for the 5-HT2A receptor (Newton et al., 1996; Hoyer, 1988a,b). It was also reported that there is a significant correlation (r = 0.78) between the affinities of various phenylalkylamine hallucinogens for 5-HT2C receptors and their psychoactive potency in humans (Titeler et al., 1988).
Molecular biology of 5-HT receptors
2008, Behavioural Brain Research