Biochemical and Biophysical Research Communications
Cloning of the human serotonin 5-HT2 and 5-HT1C receptor subtypes
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Cited by (172)
New therapeutic opportunities for 5-HT<inf>2</inf> receptor ligands
2017, Pharmacology and TherapeuticsCitation Excerpt :Although the work by Julius et al. (1988) was the first to report the cloning of a full-length functional serotonin receptor from rat (the 5-HT1c receptor), this publication was shortly followed by considerable efforts from several groups that cloned other unidentified 5-HT receptors. The classical 5-HT2 receptor described by Peroutka et al. (1981) was cloned from rats slightly later in 1988 (Pritchett et al., 1988) followed by human analogue (Branchek et al., 1990; Saltzman et al., 1991) and was renamed 5-HT2A. The 5-HT1c receptor was renamed 5-HT2C because of its structural similarity to the other 5-HT2 receptor, identical second messenger pathways, and similar pharmacological properties.
New therapeutic opportunities for 5-HT<inf>2C</inf> receptor ligands in neuropsychiatric disorders
2016, Pharmacology and TherapeuticsCitation Excerpt :The 5-HT2CR gene is unique among the members of the 5-HTRs family by virtue of its genomic organization and that fact that it was one of the first 5-HTR genes that was cloned. The partial cloning of the mouse 5-HT2CR (Lubbert et al., 1987) was followed by the sequencing of the full length clone in the rat (Julius et al., 1988), human (Saltzman et al., 1991), mouse (Foguet et al., 1992) and zebrafish (Schneider et al., 2012). Comparison of the cDNA-deduced amino acid sequences from the rat, mouse, and human revealed strong sequence homology.
Drug discovery targeting human 5-HT <inf>2C</inf> receptors: Residues S3.36 and Y7.43 impact ligand-Binding pocket structure via hydrogen bond formation
2011, European Journal of PharmacologyCitation Excerpt :Some of the diverse neurophysiological functions of serotonin (5-hydroxytryptamine, 5-HT) are mediated by the 5-HT2 G protein-coupled receptors, 5-HT2A, 5-HT2B, and 5-HT2C. The human 5-HT2C receptor (Saltzman et al., 1991), expressed with apparent exclusivity in the central nervous system, regulates ingestive behavior and is proposed to be involved in the pathophysiology of schizophrenia, psychostimulant abuse, and other neuropsychiatric disorders (Bubar and Cunningham, 2008; Jensen et al., 2010; Millan, 2005; Tecott et al., 1995). Recently, (1R, 3S)-(−)-trans-1-phenyl-3-N,N-dimethylamino-1,2,3,4-tetrahydronaphthalene (N(CH3)2-PAT) was reported as the first 5-HT2C receptor agonist with 5-HT2A and 5-HT2B receptor inverse agonist activity (Booth et al., 2009), and suggests a class of ligands suitable for pharmacotherapeutic development.
Differential regulation of 5-HT <inf>2A</inf> receptor mRNA expression following withdrawal from a chronic escalating dose regimen of D-amphetamine
2011, Brain ResearchCitation Excerpt :Slides were air-dried and stored at − 20 °C. For the detection of 5-HT2A receptor mRNA, a 48-base oligonucleotide probe (GeneDetect, Bradenton, FL, USA) was used that was complementary to bases 572–619 of the 5-HT2A receptor mRNA (Saltzman et al., 1991) and end-labeled with [35S]-dATP (Perkin Elmer NEN, Wellesley, MA, USA), as previously described (Horner et al., 2005; Horner and Keefe, 2006; Horner et al., 2009; Horner et al., 2010). Briefly, the probe was diluted in hybridization buffer (0.6 M sodium chloride, 80 mM Tris, 4 mM EDTA, 0.1% w/v sodium pyrophosphate, 10% w/v dextran, 0.2% w/v lauryl sulfate, 0.5 mg/ml heparin, 50% formamide) and 90 μl of the probe in hybridization buffer was applied to each slide and covered with glass coverslips.
Genetic Organization of the Serotonergic System
2010, Handbook of Behavioral NeuroscienceCitation Excerpt :They couple preferentially to Gq/11 to increase the hydrolysis of inositol phosphates and elevate intracellular calcium (Barnes and Sharp, 1999; Hoyer et al., 2002). The 5-HT2A receptor gene was cloned in rat (Prichett et al., 1988; Julius et al., 1990), hamster (Chambard et al., 1990), mouse (Yang et al., 1992) and human (Saltzman et al., 1991; Stam et al., 1992), and encodes a protein of 471 amino acids. The human 5-HT2A gene is located on chromosome 13q14-q21 (Sparkes et al., 1991), spans over 20 kb and consists of three exons separated by two introns (Chen et al., 1992); it is 87 percent homologous with its rat counterpart.