Genomes and Genes
Gene Symbol: Htr2a
Description: 5-hydroxytryptamine (serotonin) receptor 2A
Alias: 5-HT-2, 5-HT-2A, E030013E04, Htr-2, Htr2, 5-hydroxytryptamine receptor 2A, 5-HT2A receptor, 5-hydroxytryptamine 2 receptor
- Weisstaub N, Zhou M, Lira A, Lambe E, Gonzalez Maeso J, Hornung J, et al. Cortical 5-HT2A receptor signaling modulates anxiety-like behaviors in mice. Science. 2006;313:536-40 pubmed..These findings indicate a specific role for cortical 5HT2AR function in the modulation of conflict anxiety, consistent with models of cortical, "top-down" influences on risk assessment. ..
- Fribourg M, Moreno J, Holloway T, Provasi D, Baki L, Mahajan R, et al. Decoding the signaling of a GPCR heteromeric complex reveals a unifying mechanism of action of antipsychotic drugs. Cell. 2011;147:1011-23 pubmed publisher..These observations provide mechanistic insight into antipsychotic action that may advance therapeutic strategies for disorders including schizophrenia and dementia. ..
- Kurrasch Orbaugh D, Parrish J, Watts V, Nichols D. A complex signaling cascade links the serotonin2A receptor to phospholipase A2 activation: the involvement of MAP kinases. J Neurochem. 2003;86:980-91 pubmed
- Pavone L, Spina A, Rea S, Santoro D, Mastellone V, Lombardi P, et al. Serotonin transporter gene deficiency is associated with sudden death of newborn mice through activation of TGF-beta1 signalling. J Mol Cell Cardiol. 2009;47:691-7 pubmed publisher..Overall, our findings provide i) new insights into the role of SERT gene in SIDS, and ii) the first in vivo validation of the molecular mechanism involving the activation of TGF-beta1 signalling in the cardiac fibrosis...
- Kinoshita M, Ono K, Horie T, Nagao K, Nishi H, Kuwabara Y, et al. Regulation of adipocyte differentiation by activation of serotonin (5-HT) receptors 5-HT2AR and 5-HT2CR and involvement of microRNA-448-mediated repression of KLF5. Mol Endocrinol. 2010;24:1978-87 pubmed publisher..In this study, we identified the regulation of adipocyte differentiation by 5-HT, 5-HT(2A)R, and 5-HT(2C)R. miR-448-mediated repression of KLF5 was identified as a negative regulator for adipocyte differentiation. ..
- Isosaka T, Matsuo T, Yamaguchi T, Funabiki K, Nakanishi S, Kobayakawa R, et al. Htr2a-Expressing Cells in the Central Amygdala Control the Hierarchy between Innate and Learned Fear. Cell. 2015;163:1153-1164 pubmed publisher..Whole-brain mapping and pharmacological screening indicated that serotonin-2A receptor (Htr2a)-expressing cells in the central amygdala (CeA) control both innate and learned freezing, but in opposing ..
- Nau F, Miller J, Saravia J, Ahlert T, Yu B, Happel K, et al. Serotonin 5-HTâ‚‚ receptor activation prevents allergic asthma in a mouse model. Am J Physiol Lung Cell Mol Physiol. 2015;308:L191-8 pubmed..Our results highlight a likely role of the 5-HT2 receptors in allergic airways disease and suggest that 5-HT2 receptor agonists may represent an effective and novel small molecule-based therapy for asthma. ..
- Ago Y, Nakamura S, Arikawa S, Yata M, Matsuda T. [Involvement of prefrontal serotonergic neurons in methamphetamine-induced behavioral sensitization]. Nihon Shinkei Seishin Yakurigaku Zasshi. 2008;28:85-91 pubmed..Here, we provide an overview of the roles of serotonergic neurons in the psychostimulant-induced behavioral sensitization. ..
- McOmish C, Lira A, Hanks J, Gingrich J. Clozapine-induced locomotor suppression is mediated by 5-HT2A receptors in the forebrain. Neuropsychopharmacology. 2012;37:2747-55 pubmed publisher..Moreover, we show that it is the cortical population of 5-HT(2A) that mediate the locomotor-suppressing effects of clozapine. ..
- Bonhaus D, Bach C, Desouza A, Salazar F, Matsuoka B, Zuppan P, et al. The pharmacology and distribution of human 5-hydroxytryptamine2B (5-HT2B) receptor gene products: comparison with 5-HT2A and 5-HT2C receptors. Br J Pharmacol. 1995;115:622-8 pubmed..Finally, the finding of two distinct bands on the Northern blots of liver and kidney raises the possibility of splice variants or subtypes of 5-HT2B receptors, within these tissues. ..
- Kurita M, Moreno J, Holloway T, Kozlenkov A, Mocci G, García Bea A, et al. Repressive epigenetic changes at the mGlu2 promoter in frontal cortex of 5-HT2A knockout mice. Mol Pharmacol. 2013;83:1166-75 pubmed publisher..Together, these observations suggest that 5-HT(2A) receptor-dependent signaling epigenetically affects mGlu2 transcription in mouse frontal cortex. ..
- Duerschmied D, Canault M, Lievens D, Brill A, Cifuni S, Bader M, et al. Serotonin stimulates platelet receptor shedding by tumor necrosis factor-alpha-converting enzyme (ADAM17). J Thromb Haemost. 2009;7:1163-71 pubmed publisher..Stimulation of 5-HT2AR on platelets induces TACE-mediated shedding of GPIbalpha, the key adhesion molecule under high shear conditions. Our observations demonstrate a new pathway through which 5-HT could modulate cardiovascular disease. ..
- Weber E, Andrade R. Htr2a Gene and 5-HT(2A) Receptor Expression in the Cerebral Cortex Studied Using Genetically Modified Mice. Front Neurosci. 2010;4: pubmed publisher..and electrophysiological approaches in genetically modified mice to address the expression of the Htr2a gene and 5-HT(2A) receptors in cortex...
- Varela M, Lage S, Caruncho H, Cadavid M, Loza M, Brea J. Reelin influences the expression and function of dopamine D2 and serotonin 5-HT2A receptors: a comparative study. Neuroscience. 2015;290:165-74 pubmed publisher..These changes are similar to changes described in schizophrenic patients and provide further support for the suitability of using HRM as a model for studying this disease and the effects of antipsychotic drugs. ..
- Moreno J, Holloway T, Albizu L, Sealfon S, Gonzalez Maeso J. Metabotropic glutamate mGlu2 receptor is necessary for the pharmacological and behavioral effects induced by hallucinogenic 5-HT2A receptor agonists. Neurosci Lett. 2011;493:76-9 pubmed publisher..However, the induction of egr-2 by DOI was eliminated in mGlu2-KO mice. These findings suggest that the 5-HT2AR-mGluR2 complex is necessary for the neuropsychological responses induced by hallucinogens. ..
- Kvajo M, McKellar H, Gogos J. Avoiding mouse traps in schizophrenia genetics: lessons and promises from current and emerging mouse models. Neuroscience. 2012;211:136-64 pubmed publisher..Finally, we discuss emerging mouse models, such as second-generation pathophysiology models based on innovative approaches that are facilitated by the information gathered from the current genetic mouse models. ..
- Huttunen H, GUENETTE S, Peach C, Greco C, Xia W, Kim D, et al. HtrA2 regulates beta-amyloid precursor protein (APP) metabolism through endoplasmic reticulum-associated degradation. J Biol Chem. 2007;282:28285-95 pubmed..Based on these results we suggest a novel function for HtrA2 as a regulator of APP metabolism through ER-associated degradation. ..
- Moreno J, Muguruza C, Umali A, Mortillo S, Holloway T, Pilar Cuéllar F, et al. Identification of three residues essential for 5-hydroxytryptamine 2A-metabotropic glutamate 2 (5-HT2A·mGlu2) receptor heteromerization and its psychoactive behavioral function. J Biol Chem. 2012;287:44301-19 pubmed publisher..Together, these findings provide structural evidence for the unique behavioral function of a GPCR heteromer. ..
- Nitsch R, Deng M, Growdon J, Wurtman R. Serotonin 5-HT2a and 5-HT2c receptors stimulate amyloid precursor protein ectodomain secretion. J Biol Chem. 1996;271:4188-94 pubmed..Inasmuch as generation of APPs precludes the formation of amyloidogenic derivatives, serotonin receptors provide a novel pharmacological target to reduce these derivatives in Alzheimer's disease...
- Hsieh C, Bowcock A, Farrer L, Hebert J, Huang K, Cavalli Sforza L, et al. The serotonin receptor subtype 2 locus HTR2 is on human chromosome 13 near genes for esterase D and retinoblastoma-1 and on mouse chromosome 14. Somat Cell Mol Genet. 1990;16:567-74 pubmed..The serotonin receptor subtype 2 (gene symbol HTR2) is a G-protein-coupled receptor, expressed primarily in the cerebral cortex, where upon stimulation it stimulates ..
- Yadav V, Ryu J, Suda N, Tanaka K, Gingrich J, Schutz G, et al. Lrp5 controls bone formation by inhibiting serotonin synthesis in the duodenum. Cell. 2008;135:825-37 pubmed publisher..By identifying duodenum-derived serotonin as a hormone inhibiting bone formation in an Lrp5-dependent manner, this study broadens our understanding of bone remodeling and suggests potential therapies to increase bone mass. ..
- Zhang G, Asgeirsdóttir H, Cohen S, Munchow A, Barrera M, Stackman R. Stimulation of serotonin 2A receptors facilitates consolidation and extinction of fear memory in C57BL/6J mice. Neuropharmacology. 2013;64:403-13 pubmed publisher..Taken together these results suggest that the 5HT2AR may be a potential therapeutic target for enhancing hippocampal and amygdala-dependent memory. This article is part of a Special Issue entitled 'Cognitive Enhancers'. ..
- Xu Z, Yang Q, Ma L, Liu S, Chen G, Wu Y, et al. Deficits in LTP induction by 5-HT2A receptor antagonist in a mouse model for fragile X syndrome. PLoS ONE. 2012;7:e48741 pubmed publisher..These findings suggested that FMRP was involved in serotonin receptor signaling and contributed in GluR1 surface expression induced by 5-HT2AR inactivation. ..
- Mouillet Richard S, Pietri M, Schneider B, Vidal C, Mutel V, Launay J, et al. Modulation of serotonergic receptor signaling and cross-talk by prion protein. J Biol Chem. 2005;280:4592-601 pubmed..They provide a foundation for uncovering the impact of prion infection on serotonergic functions. ..
- Voronova I, Khramova G, Kulikova E, Petrovskii D, Bazovkina D, Kulikov A. 5-HT2A receptors control body temperature in mice during LPS-induced inflammation via regulation of NO production. Pharmacol Res. 2016;103:123-31 pubmed publisher..Moreover, adverse side effects of 5-HT2A receptor antagonists in patients with inflammation may be expected. ..
- Fiorica Howells E, Hen R, Gingrich J, Li Z, Gershon M. 5-HT(2A) receptors: location and functional analysis in intestines of wild-type and 5-HT(2A) knockout mice. Am J Physiol Gastrointest Liver Physiol. 2002;282:G877-93 pubmed
- Hirai T, Kaneshige K, Kurosaki T, Nishio H. Functional expression of 5-HT2A receptor in osteoblastic MC3T3-E1 cells. Biochem Biophys Res Commun. 2010;396:278-82 pubmed publisher..Notably, 5-HT(2A) receptor may be functionally expressed to regulate mechanisms underlying osteoblast cell proliferation, at least in part, through activation of ERK/MAPK pathways in MC3T3-E1 cells. ..
- Mori T, Komiya S, Ohya J, Uzawa N, Sugiyama K, Saitoh Y, et al. Involvement of 5-HT2 receptors in the expression of withdrawal diarrhea in morphine-dependent mice. Eur J Pharmacol. 2014;740:160-7 pubmed publisher..These results suggest that peripheral 5-HT2-receptor function could be altered in morphine-dependent mice, and the blockade of 5-HT2 receptor or free radical scavengers may be useful for the treatment of opioid-withdrawal diarrhea. ..
- Kayser V, Elfassi I, Aubel B, Melfort M, Julius D, Gingrich J, et al. Mechanical, thermal and formalin-induced nociception is differentially altered in 5-HT1A-/-, 5-HT1B-/-, 5-HT2A-/-, 5-HT3A-/- and 5-HTT-/- knock-out male mice. Pain. 2007;130:235-48 pubmed..These results support the conclusion that the complex control of pain mechanisms by 5-HT, acting at multiple receptors, is physiologically relevant in mice. ..
- Walsh R, Shen E, Bagot R, Anselmo A, Jiang Y, Javidfar B, et al. Phf8 loss confers resistance to depression-like and anxiety-like behaviors in mice. Nat Commun. 2017;8:15142 pubmed publisher..signalling within the prefrontal cortex of Phf8 deficient mice and identify the serotonin receptors Htr1a and Htr2a as direct targets of PHF8...
- Van Steenwinckel J, Brisorgueil M, Fischer J, Vergé D, Gingrich J, Bourgoin S, et al. Role of spinal serotonin 5-HT2A receptor in 2',3'-dideoxycytidine-induced neuropathic pain in the rat and the mouse. Pain. 2008;137:66-80 pubmed
- Fiorica Howells E, Maroteaux L, Gershon M. Serotonin and the 5-HT(2B) receptor in the development of enteric neurons. J Neurosci. 2000;20:294-305 pubmed..It is possible that by stimulating 5-HT(2B) receptors, 5-HT affects the fate of the large subset of enteric neurons that arises after the development of endogenous sources of 5-HT. ..
- Bombardi C. Neuronal localization of 5-HT2A receptor immunoreactivity in the rat hippocampal region. Brain Res Bull. 2012;87:259-73 pubmed publisher..The results of the present study suggest that the 5-HT2Ar could participate in the hippocampal neurotransmission by acting on different neuronal populations. ..
- Popa D, Léna C, Fabre V, Prenat C, Gingrich J, Escourrou P, et al. Contribution of 5-HT2 receptor subtypes to sleep-wakefulness and respiratory control, and functional adaptations in knock-out mice lacking 5-HT2A receptors. J Neurosci. 2005;25:11231-8 pubmed..Moreover, 5-HT(2A) gene knock-out leads to functional compensations yielding adaptive changes opposite to those caused by pharmacological blockade of 5-HT(2A) receptors in 5-HT(2A)+/+ mice. ..
- Hernandez L, Gregerson K, Horseman N. Mammary gland serotonin regulates parathyroid hormone-related protein and other bone-related signals. Am J Physiol Endocrinol Metab. 2012;302:E1009-15 pubmed publisher..These results connect 5-HT synthesis to the induction of bone-regulating factors in the normal mammary gland and in breast cancer cells. ..
- Foguet M, Nguyen H, Le H, Lubbert H. Structure of the mouse 5-HT1C, 5-HT2 and stomach fundus serotonin receptor genes. Neuroreport. 1992;3:345-8 pubmed..This intron distribution is unique and distinguishes these receptors from other members of the family of receptors coupled to G-proteins. ..
- Brennan T, Seeley W, Kilgard M, Schreiner C, Tecott L. Sound-induced seizures in serotonin 5-HT2c receptor mutant mice. Nat Genet. 1997;16:387-90 pubmed..This AGS syndrome is the first produced by a known genetic defect; it provides a robust model for the examination of serotoninergic mechanisms in epilepsy. ..
- Pena F, Ramirez J. Endogenous activation of serotonin-2A receptors is required for respiratory rhythm generation in vitro. J Neurosci. 2002;22:11055-64 pubmed..We conclude that endogenously activated 5-HT(2A) receptors are required for maintaining fictive respiratory activity in the brainstem slice by modulating sodium conductances via a PKC pathway. ..
- Popova N, Amstislavskaya T. 5-HT2A and 5-HT2C serotonin receptors differentially modulate mouse sexual arousal and the hypothalamo-pituitary-testicular response to the presence of a female. Neuroendocrinology. 2002;76:28-34 pubmed..05). The present findings suggest that 5-HT2A/5-HT2C receptors may be involved in the neural control of male sexual motivation and arousal, presumably by exerting reciprocal facilitative (5-HT2A) or suppressive (5-HT2C) influences. ..
- Gould G, Hensler J, Burke T, Benno R, Onaivi E, Daws L. Density and function of central serotonin (5-HT) transporters, 5-HT1A and 5-HT2A receptors, and effects of their targeting on BTBR T+tf/J mouse social behavior. J Neurochem. 2011;116:291-303 pubmed publisher..1 mg/kg) reduced marble burying, but failed to improve sociability. Overall, altered SERT and/or 5-HT(1A) functionality in hippocampus could contribute to the relatively low sociability of BTBR mice. ..
- Fox M, Stein A, French H, Murphy D. Functional interactions between 5-HT2A and presynaptic 5-HT1A receptor-based responses in mice genetically deficient in the serotonin 5-HT transporter (SERT). Br J Pharmacol. 2010;159:879-87 pubmed publisher..Our findings strongly support the correlation of WAY 100635 induced head twitches with increased 5-HT availability, induced genetically or pharmacologically. ..
- ForcÃ©n R, Latorre E, Pardo J, Alcalde A, Murillo M, Grasa L. Toll-like receptors 2 and 4 modulate the contractile response induced by serotonin in mouse ileum: analysis of the serotonin receptors involved. Neurogastroenterol Motil. 2015;27:1258-66 pubmed publisher..TLR2 and TLR4 signaling may modulate the spontaneous contractions and the serotonin contractile response by acting on 5-HT2, 5-HT3, 5-HT4, and 5-HT7 receptors. ..
- Petit A, Quesseveur G, Gressier F, Colle R, David D, Gardier A, et al. Converging translational evidence for the involvement of the serotonin 2A receptor gene in major depressive disorder. Prog Neuropsychopharmacol Biol Psychiatry. 2014;54:76-82 pubmed publisherAn association between serotonin 2A receptor (5-HT2AR), encoded by HTR2A gene, and major depressive disorder (MDD) has been suggested...
- Moreno J, Miranda Azpiazu P, GarcÃa Bea A, Younkin J, Cui M, Kozlenkov A, et al. Allosteric signaling through an mGlu2 and 5-HT2A heteromeric receptor complex and its potential contribution to schizophrenia. Sci Signal. 2016;9:ra5 pubmed publisher..These findings offer structural insights into this important target in molecular psychiatry. ..
- Rasmussen E, Cipp L, Hitzemann R. Identification of quantitative trait loci for haloperidol-induced catalepsy on mouse chromosome 14. J Pharmacol Exp Ther. 1999;290:1337-46 pubmed..4) on chromosome 14 near the piebald (Ednrb) and 5-hydroxytryptamine(2A) (Htr2a) loci...
- Naumenko V, Bazovkina D, Kondaurova E. [On the Functional Cross-Talk between Brain 5-HT1A and 5-HT2A Receptors]. Zh Vyssh Nerv Deiat Im I P Pavlova. 2015;65:240-7 pubmed..The obtained data indicate that 5-HTA and 5-HT2A receptors are able to modulate each other functional activity by means of bilateral functional cross-talk. ..
- Kanamaru M, Homma I. Compensatory airway dilation and additive ventilatory augmentation mediated by dorsomedial medullary 5-hydroxytryptamine 2 receptor activity and hypercapnia. Am J Physiol Regul Integr Comp Physiol. 2007;293:R854-60 pubmed..Interaction between 5-HT2 receptor activity in the DMM and CO(2) drive may elicit a cycle of hyperventilation with airway dilation and hypoventilation with airway narrowing...
- Bras H, Gaytan S, Portalier P, Zanella S, Pasaro R, Coulon P, et al. Prenatal activation of 5-HT2A receptor induces expression of 5-HT1B receptor in phrenic motoneurons and alters the organization of their premotor network in newborn mice. Eur J Neurosci. 2008;28:1097-107 pubmed publisher..These results show that a prenatal 5-HT excess affects, via the overactivation of 5-HT(2A)-R, the expression of 5-HT(1B)-R in PhMns and the organization of their premotor network. ..
- Schiller L, Jahkel M, Kretzschmar M, Brust P, Oehler J. Autoradiographic analyses of 5-HT1A and 5-HT2A receptors after social isolation in mice. Brain Res. 2003;980:169-78 pubmed..Besides metabolism-related adaptation processes also neurotransmitter and hormonal (e.g., glucocorticoid) interactions especially in limbic regions have to be considered. ..
- Orejarena M, Lanfumey L, Maldonado R, Robledo P. Involvement of 5-HT2A receptors in MDMA reinforcement and cue-induced reinstatement of MDMA-seeking behaviour. Int J Neuropsychopharmacol. 2011;14:927-40 pubmed publisher..25 mg/kg. Our results indicate that 5-HT2ARs are crucial for MDMA-induced reinforcement and cue-induced reinstatement of MDMA-seeking behaviour. These effects are probably due to the modulation of mesolimbic dopaminergic activity. ..
- Rasul A, Johansson B, Lonne Rahm S, Nordlind K, Theodorsson E, El Nour H. Chronic mild stress modulates 5-HT1A and 5-HT2A receptor expression in the cerebellar cortex of NC/Nga atopic-like mice. Arch Dermatol Res. 2013;305:407-13 pubmed publisher..In addition, the signal intensity was highest in the SE group, with a difference compared to the other groups. In conclusion, chronic mild stress modulates serotonergic receptor expressions in the cerebellar cortex of atopic-like mice. ..
- Salomon L, Lanteri C, Glowinski J, Tassin J. Behavioral sensitization to amphetamine results from an uncoupling between noradrenergic and serotonergic neurons. Proc Natl Acad Sci U S A. 2006;103:7476-81 pubmed..Uncoupling between noradrenergic and serotonergic neurons may occur not only in addiction but also during chronic stressful situations, thus facilitating the onset of mental illness. ..
- Cario E, Gerken G, Podolsky D. Toll-like receptor 2 controls mucosal inflammation by regulating epithelial barrier function. Gastroenterology. 2007;132:1359-74 pubmed..TLR2 may provide a target to pharmacologically modulate mucosal injury and intestinal inflammation. ..
- Saucier C, Albert P. Identification of an endogenous 5-hydroxytryptamine2A receptor in NIH-3T3 cells: agonist-induced down-regulation involves decreases in receptor RNA and number. J Neurochem. 1997;68:1998-2011 pubmed..The NIH-3T3 cells provide a novel system for understanding 5-HT2A receptor regulation. ..
- Kurita M, Holloway T, García Bea A, Kozlenkov A, Friedman A, Moreno J, et al. HDAC2 regulates atypical antipsychotic responses through the modulation of mGlu2 promoter activity. Nat Neurosci. 2012;15:1245-54 pubmed publisher..These observations support the view of HDAC2 as a promising new target for schizophrenia treatment...
- Becamel C, Gavarini S, Chanrion B, Alonso G, Galeotti N, Dumuis A, et al. The serotonin 5-HT2A and 5-HT2C receptors interact with specific sets of PDZ proteins. J Biol Chem. 2004;279:20257-66 pubmed..The interaction of the 5-HT(2A) and the 5-HT(2C) receptor with specific sets of PDZ proteins may contribute to their different signal transduction properties. ..
- Sibille E, Sarnyai Z, Benjamin D, Gal J, Baker H, Toth M. Antisense inhibition of 5-hydroxytryptamine2a receptor induces an antidepressant-like effect in mice. Mol Pharmacol. 1997;52:1056-63 pubmed
- Kato M, Ikawa Y, Hayashizaki Y, Shibata H. Paternal imprinting of mouse serotonin receptor 2A gene Htr2 in embryonic eye: a conserved imprinting regulation on the RB/Rb locus. Genomics. 1998;47:146-8 pubmed
- Zhang G, Cinalli D, Cohen S, Knapp K, Rios L, MartÃnez HernÃ¡ndez J, et al. Examination of the hippocampal contribution to serotonin 5-HT2A receptor-mediated facilitation of object memory in C57BL/6J mice. Neuropharmacology. 2016;109:332-340 pubmed publisher..The 5-HT2AR-mediated facilitation of hippocampal memory may be associated with an increase in hippocampal neuronal firing and glutamate efflux during a post-training time window in which recently encoded memories undergo consolidation. ..
- Naumenko V, Bazovkina D, Kondaurova E, Zubkov E, Kulikov A. The role of 5-HT2A receptor and 5-HT2A/5-HT1A receptor interaction in the suppression of catalepsy. Genes Brain Behav. 2010;9:519-24 pubmed publisher..Thus, 5-HT(2A)/5-HT(1A) receptor interaction in the mechanism of catalepsy suppression in mice was shown. ..
- Coelho W, Costa K, Sola Penna M. Serotonin stimulates mouse skeletal muscle 6-phosphofructo-1-kinase through tyrosine-phosphorylation of the enzyme altering its intracellular localization. Mol Genet Metab. 2007;92:364-70 pubmed
- Abrantes E, Pires E, Carvalho A, Costa F, Savino W, Reis L. Identification, structural characterization, and tissue distribution of Tsg-5: a new TNF-stimulated gene. Genes Immun. 2003;4:298-311 pubmed..Our data suggest that Tsg-5 encodes a new, rare transcript, with a very tight regulation of expression and differential splicing. ..
- Haberzettl R, Fink H, Bert B. Role of 5-HT(1A)- and 5-HT(2A) receptors for the murine model of the serotonin syndrome. J Pharmacol Toxicol Methods. 2014;70:129-33 pubmed publisher..In summary, the murine model of the SS is a valid tool for preclinical studies to screen drugs and drug combinations for the risk to cause an SS in man. ..
- Rajkumar R, Pandey D, Mahesh R, Radha R. 1-(m-Chlorophenyl)piperazine induces depressogenic-like behaviour in rodents by stimulating the neuronal 5-HT(2A) receptors: proposal of a modified rodent antidepressant assay. Eur J Pharmacol. 2009;608:32-41 pubmed publisher..Finally, the mCPP induced depression-like behaviour in rodents is envisaged as a modified antidepressant assay to identify novel serotonergic antidepressants. ..
- Amodeo D, Jones J, Sweeney J, Ragozzino M. Risperidone and the 5-HT2A receptor antagonist M100907 improve probabilistic reversal learning in BTBR T + tf/J mice. Autism Res. 2014;7:555-67 pubmed publisher..Because risperidone can lead to unwanted side effects, treatment with a specific 5HT2A receptor antagonist may improve cognitive flexibility in individuals with ASD while also minimizing unwanted side effects. ..
- Quesseveur G, Reperant C, David D, Gardier A, Sanchez C, Guiard B. 5-HT?A receptor inactivation potentiates the acute antidepressant-like activity of escitalopram: involvement of the noradrenergic system. Exp Brain Res. 2013;226:285-95 pubmed publisher..Indeed, among the genetic factors known to influence the individual response to antidepressants, the HTR2A gene has been associated with SSRIs response in depressed patients...
- Nonogaki K, Nozue K, Oka Y. Increased hypothalamic 5-HT2A receptor gene expression and effects of pharmacologic 5-HT2A receptor inactivation in obese Ay mice. Biochem Biophys Res Commun. 2006;351:1078-82 pubmed..These results suggest that obesity increases hypothalamic 5-HT2A receptor gene expression, and pharmacologic inactivation of 5-HT2A receptors inhibits overfeeding and obesity in A(y) mice, but did not increase plasma adiponectin levels. ..
- Medrihan L, Sagi Y, Inde Z, Krupa O, Daniels C, Peyrache A, et al. Initiation of Behavioral Response to Antidepressants by Cholecystokinin Neurons of the Dentate Gyrus. Neuron. 2017;95:564-576.e4 pubmed publisher..Finally, inhibition of CCK neurons mimics the antidepressant behavioral effects of SSRIs, suggesting that these cells may represent a novel cellular target for the development of fast-acting antidepressant drugs. ..
- Huang M, Dai J, Meltzer H. 5-HT(2A) and 5-HT(2C) receptor stimulation are differentially involved in the cortical dopamine efflux-Studied in 5-HT(2A) and 5-HT(2C) genetic mutant mice. Eur J Pharmacol. 2011;652:40-5 pubmed publisher..These findings suggest that 5-HT(2C) receptor agonists may be useful as antipsychotics, consistent with previous suggestions. ..
- Trajkovska V, Santini M, Marcussen A, Thomsen M, Hansen H, Mikkelsen J, et al. BDNF downregulates 5-HT(2A) receptor protein levels in hippocampal cultures. Neurochem Int. 2009;55:697-702 pubmed publisher..This interaction may be an important mechanism in the role of BDNF in affective disorders emphasizing the need for further elucidating the specificity and the mechanism behind this regulation. ..
- Lauder J, Wilkie M, Wu C, Singh S. Expression of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors in the mouse embryo. Int J Dev Neurosci. 2000;18:653-62 pubmed
- Choi D, Ward S, Messaddeq N, Launay J, Maroteaux L. 5-HT2B receptor-mediated serotonin morphogenetic functions in mouse cranial neural crest and myocardiac cells. Development. 1997;124:1745-55 pubmed
- Halberstadt A, Powell S, Geyer M. Role of the 5-HT?A receptor in the locomotor hyperactivity produced by phenylalkylamine hallucinogens in mice. Neuropharmacology. 2013;70:218-27 pubmed publisher..These studies provide additional support for the link between 5-HT?A activation and hallucinogenesis. ..
- Bulley S, Liu Y, Ripps H, Shen W. Taurine activates delayed rectifier Kv channels via a metabotropic pathway in retinal neurons. J Physiol. 2013;591:123-32 pubmed publisher..In sum, this study provides new evidence that taurine activates a serotonin system, apparently via 5-HT(2A) receptors and related intracellular pathways. ..
- Niebert M, Vogelgesang S, Koch U, Bischoff A, Kron M, Bock N, et al. Expression and function of serotonin 2A and 2B receptors in the mammalian respiratory network. PLoS ONE. 2011;6:e21395 pubmed publisher..Taken together, the results of this study suggest a significant role of both receptors in respiratory network modulation. ..
- Farisse J, Hery F, Barden N, Hery M, Boulenguez P. Central 5-HT(1) and 5-HT(2) binding sites in transgenic mice with reduced glucocorticoid receptor number. Brain Res. 2000;862:145-53 pubmed..These results suggest that some of the alterations of the serotonergic neurotransmission observed in depressed patients might be secondary to an altered glucocorticoid receptor function. ..
- Ishikawa C, Li H, Ogura R, Yoshimura Y, Kudo T, Shirakawa M, et al. Effects of gravity changes on gene expression of BDNF and serotonin receptors in the mouse brain. PLoS ONE. 2017;12:e0177833 pubmed publisher..The modulation of gene expression may constitute molecular bases that underlie behavioral alteration induced by gravity changes. ..
- Frankel W, Valenzuela A, Lutz C, Johnson E, Dietrich W, Coffin J. New seizure frequency QTL and the complex genetics of epilepsy in EL mice. Mamm Genome. 1995;6:830-8 pubmed..The serotonin receptor gene, Htr2a, maps near and is a candidate for El5, and linkages of other serotonin receptor genes to seizure frequency QTL are ..
- Uchida Kitajima S, Yamauchi T, Takashina Y, Okada Iwabu M, Iwabu M, Ueki K, et al. 5-Hydroxytryptamine 2A receptor signaling cascade modulates adiponectin and plasminogen activator inhibitor 1 expression in adipose tissue. FEBS Lett. 2008;582:3037-44 pubmed publisher..These findings indicate that antagonism of 5-HT(2A) receptors in adipocytes could improve the obesity-linked decreases in adiponectin expression and increases in PAI-1 expression. ..
- Shapiro D, Kristiansen K, Weiner D, Kroeze W, Roth B. Evidence for a model of agonist-induced activation of 5-hydroxytryptamine 2A serotonin receptors that involves the disruption of a strong ionic interaction between helices 3 and 6. J Biol Chem. 2002;277:11441-9 pubmed..L. Roth and D. A. Shapiro (2001) Expert Opin. Ther. Targets 5, 685-695) and others, that this may represent a general mechanism of activation for many, but not all, G-protein-coupled receptors. ..