Htr2a

Summary

Gene Symbol: Htr2a
Description: 5-hydroxytryptamine receptor 2A
Alias: 5-HT2A, 5Ht-2, 5-hydroxytryptamine receptor 2A, 5-HT-2, 5-HT-2A, 5-hydroxytryptamine (serotonin) receptor 2A, G protein-coupled, serotonin 5HT-2 receptor, serotonin receptor 2A
Species: rat
Products:     Htr2a

Top Publications

  1. Yabanoglu S, Akkiki M, Seguelas M, Mialet Perez J, Parini A, Pizzinat N. Platelet derived serotonin drives the activation of rat cardiac fibroblasts by 5-HT2A receptors. J Mol Cell Cardiol. 2009;46:518-25 pubmed publisher
    ..5-HT released by platelets appears to be a major contributor of platelet effects which are mediated through 5-HT2A receptors. ..
  2. 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. ..
  3. Jones K, Srivastava D, Allen J, Strachan R, Roth B, Penzes P. Rapid modulation of spine morphology by the 5-HT2A serotonin receptor through kalirin-7 signaling. Proc Natl Acad Sci U S A. 2009;106:19575-80 pubmed publisher
    ..These results suggest a potential role for serotonin signaling in modulating spine morphology and kalirin-7's function at cortical synapses. ..
  4. Cornea Hébert V, Riad M, Wu C, Singh S, Descarries L. Cellular and subcellular distribution of the serotonin 5-HT2A receptor in the central nervous system of adult rat. J Comp Neurol. 1999;409:187-209 pubmed
  5. Pichon X, Wattiez A, Becamel C, Ehrlich I, Bockaert J, Eschalier A, et al. Disrupting 5-HT(2A) receptor/PDZ protein interactions reduces hyperalgesia and enhances SSRI efficacy in neuropathic pain. Mol Ther. 2010;18:1462-70 pubmed publisher
    ..Disruption of these interactions might be a valuable strategy to design novel treatments for neuropathic pain and to increase the effectiveness of SSRIs. ..
  6. Miner L, Backstrom J, Sanders Bush E, Sesack S. Ultrastructural localization of serotonin2A receptors in the middle layers of the rat prelimbic prefrontal cortex. Neuroscience. 2003;116:107-17 pubmed
    ..The results further suggest that serotonin acts presynaptically via this receptor subtype, most likely at receptors on monoamine fibers, and only rarely directly on glutamate axons. ..
  7. Xia Z, Gray J, Compton Toth B, Roth B. A direct interaction of PSD-95 with 5-HT2A serotonin receptors regulates receptor trafficking and signal transduction. J Biol Chem. 2003;278:21901-8 pubmed
    ..Taken together, the present work elucidates novel roles for PSD-95 in regulating the functional activity and intracellular trafficking of 5-HT2A receptors and possibly other GPCRs. ..
  8. Iwasaki T, Otsuguro K, Kobayashi T, Ohta T, Ito S. Endogenously released 5-HT inhibits A and C fiber-evoked synaptic transmission in the rat spinal cord by the facilitation of GABA/glycine and 5-HT release via 5-HT(2A) and 5-HT(3) receptors. Eur J Pharmacol. 2013;702:149-57 pubmed publisher
    ..5-HT3 receptors may be involved in the facilitation of 5-HT release via a positive feedback process. ..
  9. Doly S, Madeira A, Fischer J, Brisorgueil M, Daval G, Bernard R, et al. The 5-HT2A receptor is widely distributed in the rat spinal cord and mainly localized at the plasma membrane of postsynaptic neurons. J Comp Neurol. 2004;472:496-511 pubmed
    ..These observations are consistent with a double role (pre- and postsynaptic) for serotonin on these receptors on various cellular targets. ..

More Information

Publications95

  1. Van Steenwinckel J, Noghero A, Thibault K, Brisorgueil M, Fischer J, Conrath M. The 5-HT2A receptor is mainly expressed in nociceptive sensory neurons in rat lumbar dorsal root ganglia. Neuroscience. 2009;161:838-46 pubmed publisher
  2. Thibault K, Van Steenwinckel J, Brisorgueil M, Fischer J, Hamon M, Calvino B, et al. Serotonin 5-HT2A receptor involvement and Fos expression at the spinal level in vincristine-induced neuropathy in the rat. Pain. 2008;140:305-22 pubmed publisher
    ..These data provide support to the idea that, in vincristine-induced neuropathy, 5-HT2AR are involved in the sensitization of peripheral nociceptors and spinal nociceptive processing. ..
  3. Cussac D, Boutet Robinet E, Ailhaud M, Newman Tancredi A, Martel J, Danty N, et al. Agonist-directed trafficking of signalling at serotonin 5-HT2A, 5-HT2B and 5-HT2C-VSV receptors mediated Gq/11 activation and calcium mobilisation in CHO cells. Eur J Pharmacol. 2008;594:32-8 pubmed publisher
  4. Bos R, Sadlaoud K, Boulenguez P, Buttigieg D, Liabeuf S, Brocard C, et al. Activation of 5-HT2A receptors upregulates the function of the neuronal K-Cl cotransporter KCC2. Proc Natl Acad Sci U S A. 2013;110:348-53 pubmed publisher
  5. Harvey P, Li X, Li Y, Bennett D. 5-HT2 receptor activation facilitates a persistent sodium current and repetitive firing in spinal motoneurons of rats with and without chronic spinal cord injury. J Neurophysiol. 2006;96:1158-70 pubmed
    ..With chronic injury, the developed 5-HT supersensitivity more than compensates for lost brain stem 5-HT, so that the Na PIC is large and motoneurons are very excitable, thus contributing to spasticity...
  6. Ding Z, Cowan A, Rawls S. 5-HT reuptake and 5-HT2 receptors modulate capsaicin-evoked hypothermia in rats. Neurosci Lett. 2008;430:191-6 pubmed
    ..p.) enhanced the hypothermic effect of capsaicin (1mg/kg, i.m.). The present data reveal that capsaicin-evoked hypothermia in rats is attenuated by the blockade of 5-HT reuptake and enhanced by the antagonism of 5-HT(2) receptors. ..
  7. Xu C, Giuliano F, Sun X, Brisorgueil M, Leclerc P, Vergé D, et al. Serotonin 5-HT2A and 5-HT5A receptors are expressed by different motoneuron populations in rat Onuf's nucleus. J Comp Neurol. 2007;502:620-34 pubmed
    ..This might have implications for pharmacological research targeting different pelvic functions e.g., micturition and ejaculation. ..
  8. Bonaventure P, Nepomuceno D, Miller K, Chen J, Kuei C, Kamme F, et al. Molecular and pharmacological characterization of serotonin 5-HT2A and 5-HT2B receptor subtypes in dog. Eur J Pharmacol. 2005;513:181-92 pubmed
    ..The availability of the full sequence and pharmacology of the canine 5-HT2A and canine 5-HT2B receptors provides useful information for the interpretation of previous and future pharmacological studies of 5-HT2A/2B ligands in dog. ..
  9. Kjørsvik Bertelsen A, Warsame Afrah A, Gustafsson H, Tjølsen A, Hole K, Stiller C. Stimulation of spinal 5-HT(2A/2C) receptors potentiates the capsaicin-induced in vivo release of substance P-like immunoreactivity in the rat dorsal horn. Brain Res. 2003;987:10-6 pubmed
    ..The observation that the highest dose of DOI failed to induce SP-LI release may be due to an inhibitory postsynaptic action at this dose. ..
  10. 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. ..
  11. Kato K, Sekiguchi M, Kikuchi S, Konno S. The effect of a 5-HT2A receptor antagonist on pain-related behavior, endogenous 5-hydroxytryptamine production, and the expression 5-HT2A receptors in dorsal root ganglia in a rat lumbar disc herniation model. Spine (Phila Pa 1976). 2015;40:357-62 pubmed publisher
    ..Selective 5-HT2A receptor antagonists may attenuate sciatica by blocking and downregulating 5-HT2A receptors in DRGs in lumbar disc herniation. NA. ..
  12. Zaniewska M, McCreary A, Przegalinski E, Filip M. Effects of the serotonin 5-HT2A and 5-HT2C receptor ligands on the discriminative stimulus effects of nicotine in rats. Eur J Pharmacol. 2007;571:156-65 pubmed
  13. Adriani W, Giannakopoulou D, Bokulic Z, Jernej B, Alleva E, Laviola G. Response to novelty, social and self-control behaviors, in rats exposed to neonatal anoxia: modulatory effects of an enriched environment. Psychopharmacology (Berl). 2006;184:155-65 pubmed
    ..Beneficial effects of stimulation by an enriched environment during the still-plastic window of adolescence are suggested in these animals. ..
  14. Kong X, Wienecke J, Hultborn H, Zhang M. Robust upregulation of serotonin 2A receptors after chronic spinal transection of rats: an immunohistochemical study. Brain Res. 2010;1320:60-8 pubmed publisher
    ..These results indicate that the upregulation of 5-HT2A receptors at least partly underlies the 5-HT denervation supersensitivity of spinal motoneurons after a complete spinal transection. ..
  15. Toppin V, Harris M, Kober A, Leiter J, ST JOHN W. Persistence of eupnea and gasping following blockade of both serotonin type 1 and 2 receptors in the in situ juvenile rat preparation. J Appl Physiol (1985). 2007;103:220-7 pubmed
    ..In greatly reduced in vitro preparations, the importance of any individual neuromodulator, such as serotonin, may be exaggerated compared with its role in more intact preparations. ..
  16. Sakai T, Kasahara K, Tomita K, Ikegaki I, Kuriyama H. 5-Hydroxytryptamine-induced bladder hyperactivity via the 5-HT2A receptor in partial bladder outlet obstruction in rats. Am J Physiol Renal Physiol. 2013;304:F1020-7 pubmed publisher
    ..These results suggest that the increased contractile responses to 5-HT in BOO rat bladder may be partly caused by 5-HT(2A) receptor upregulation in the detrusor smooth muscles. ..
  17. Zhang X, Andren P, Svenningsson P. Changes on 5-HT2 receptor mRNAs in striatum and subthalamic nucleus in Parkinson's disease model. Physiol Behav. 2007;92:29-33 pubmed
  18. Yuen E, Jiang Q, Chen P, Feng J, Yan Z. Activation of 5-HT2A/C receptors counteracts 5-HT1A regulation of n-methyl-D-aspartate receptor channels in pyramidal neurons of prefrontal cortex. J Biol Chem. 2008;283:17194-204 pubmed publisher
    ..These findings provide a framework for understanding the complex interactions between serotonin and NMDARs in PFC, which could be important for cognitive and emotional control in which both systems are highly involved. ..
  19. Kokubu N, Tsuchihashi K, Yuda S, Hase M, Eguchi M, Wakabayashi T, et al. Persistent insulin-sensitizing effects of sarpogrelate hydrochloride, a serotonin 2A receptor antagonist, in patients with peripheral arterial disease. Circ J. 2006;70:1451-6 pubmed
    ..001, r=-0.441). Sarpogrelate has a persistent insulin-sensitizing effect through adiponectin modification and might be beneficial for anti-atherosclerotic therapy, at least, in non-diabetic and non-medicated diabetic patients with PAD. ..
  20. Parrish J, Nichols D. Serotonin 5-HT(2A) receptor activation induces 2-arachidonoylglycerol release through a phospholipase c-dependent mechanism. J Neurochem. 2006;99:1164-75 pubmed
  21. Pehek E, Nocjar C, Roth B, Byrd T, Mabrouk O. Evidence for the preferential involvement of 5-HT2A serotonin receptors in stress- and drug-induced dopamine release in the rat medial prefrontal cortex. Neuropsychopharmacology. 2006;31:265-77 pubmed
    ..These findings may have implications for the pharmacological treatment of disorders resulting from or exacerbated by stress. ..
  22. Lopez Gimenez J, Vilaró M, Palacios J, Mengod G. Multiple conformations of 5-HT2A and 5-HT 2C receptors in rat brain: an autoradiographic study with [125I](±)DOI. Exp Brain Res. 2013;230:395-406 pubmed publisher
    ..Thus, [(125)I](±)DOI would label multiple conformations of both 5-HT2A and 5-HT2C receptors in rat brain, and M100907 and ketanserin would recognise these conformations with different affinities. ..
  23. Collins S, Huff C, Chiaia N, Gudelsky G, Yamamoto B. 3,4-methylenedioxymethamphetamine increases excitability in the dentate gyrus: role of 5HT2A receptor-induced PGE2 signaling. J Neurochem. 2016;136:1074-84 pubmed publisher
    ..EP1 receptor activation leads to eventual excitotoxicity and loss of PV interneurons resulting in reduced inhibition and lowered seizure threshold resulting in increased seizure susceptibility. ..
  24. Rothman R, Vu N, Wang X, Xu H. Endogenous CART peptide regulates mu opioid and serotonin 5-HT(2A) receptors. Peptides. 2003;24:413-7 pubmed
    ..The results demonstrated that anti-CART peptide IgG up-regulates mu and 5-HT(2A) receptor in the hippocampus and caudate We conclude that CART peptides in the cerebrospinal fluid may exert regulatory effects in the brain. ..
  25. Navarro S, Gutiérrez Ferre V, Flores P, Moreno M. Activation of serotonin 5-HT2A receptors inhibits high compulsive drinking on schedule-induced polydipsia. Psychopharmacology (Berl). 2015;232:683-97 pubmed publisher
    ..Thus, it may represent a potentially new marker of vulnerability and provides additional insight for potential treatments on compulsive behaviours in neuropsychiatric populations. ..
  26. Nocjar C, Alex K, Sonneborn A, Abbas A, Roth B, Pehek E. Serotonin-2C and -2a receptor co-expression on cells in the rat medial prefrontal cortex. Neuroscience. 2015;297:22-37 pubmed publisher
    ..Thus a complex interplay of cortical 5-HT2A and 5-HT2C receptor mechanisms exists, which if altered, could modulate efferent brain systems implicated in mental illness. ..
  27. de Paula Soares V, Zangrossi H. Stimulation of 5-HT1A or 5-HT2A receptors in the ventrolateral periaqueductal gray causes anxiolytic-, but not panicolytic-like effect in rats. Behav Brain Res. 2009;197:178-85 pubmed publisher
    ..In conclusion, our data show that the activation of 5-HT1A and 5-HT2A receptors in the vlPAG affects defensive responses related to generalized anxiety, but not panic disorder. ..
  28. Torres Escalante J, Barral J, Ibarra Villa M, Pérez Burgos A, Góngora Alfaro J, Pineda J. 5-HT1A, 5-HT2, and GABAB receptors interact to modulate neurotransmitter release probability in layer 2/3 somatosensory rat cortex as evaluated by the paired pulse protocol. J Neurosci Res. 2004;78:268-78 pubmed
    ..When the effect of GABA(B) receptor activation is maximal, however, the influence of 5-HT changes to the opposite direction, inhibiting PP facilitation (increasing glutamate release) through activation of 5-HT(2) receptors. ..
  29. Wang S, Wang K, Wang W, Sihra T. Unexpected inhibitory regulation of glutamate release from rat cerebrocortical nerve terminals by presynaptic 5-hydroxytryptamine-2A receptors. J Neurosci Res. 2006;84:1528-42 pubmed
    ..These observations invoke presynaptic inhibitory 5-HT(2A) receptor function as a potential target for drugs to mitigate the effects of excessive glutamatergic transmission. ..
  30. Cohen H. Anxiolytic effect and memory improvement in rats by antisense oligodeoxynucleotide to 5-hydroxytryptamine-2A precursor protein. Depress Anxiety. 2005;22:84-93 pubmed
    ..Receptor downregulation has been proposed as one of the central mechanisms for anxiolytic drug actions. Antisense-mediated downmanipulation of receptors in this study, especially of 5-HT2A, supports this theory. ..
  31. Navarrett S, Collier L, Cardozo C, Dracheva S. Alterations of serotonin 2C and 2A receptors in response to T10 spinal cord transection in rats. Neurosci Lett. 2012;506:74-8 pubmed publisher
    ..To this end, the influence of excitatory locomotor circuits on motor neurons in the thoracic spinal cord of rats requires further exploration. ..
  32. Park K, Sin P, Lee D, Cha S, Kim M, Kim N, et al. Switching-on of serotonergic calcium signaling in activated hepatic stellate cells. World J Gastroenterol. 2011;17:164-73 pubmed publisher
    ..The appearance of 5-HT-induced [Ca²+](i) response accompanied by upregulation of metabotropic 5-HT? receptors and Ca²+ transporting/chaperone ER proteins may participate in the activating process of HSCs. ..
  33. Chen C, Han X, Fan F, Liu Y, Wang T, Wang J, et al. Serotonin drives the activation of pulmonary artery adventitial fibroblasts and TGF-β1/Smad3-mediated fibrotic responses through 5-HT(2A) receptors. Mol Cell Biochem. 2014;397:267-76 pubmed publisher
    ..These results demonstrated that 5-HT can directly activate PAFs through 5-HT2A receptor and promote fibroblasts phenotypic alterations and adventitia fibrosis depending on the signaling of the TGF-β1/Smad3 pathway. ..
  34. Cerulo G, Tafuri S, De Pasquale V, Rea S, Romano S, Costagliola A, et al. Serotonin activates cell survival and apoptotic death responses in cultured epithelial thyroid cells. Biochimie. 2014;105:211-5 pubmed publisher
  35. Van Oekelen D, Megens A, Meert T, Luyten W, Leysen J. Functional study of rat 5-HT2A receptors using antisense oligonucleotides. J Neurochem. 2003;85:1087-100 pubmed
    ..Our analysis of the behavioural consequences of AO treatment and the use of different AOs and SOs has shown that specific receptor-mediated behaviour can be identified. ..
  36. Brattelid T, Qvigstad E, Birkeland J, Swift F, Bekkevold S, Krobert K, et al. Serotonin responsiveness through 5-HT2A and 5-HT4 receptors is differentially regulated in hypertrophic and failing rat cardiac ventricle. J Mol Cell Cardiol. 2007;43:767-79 pubmed
    ..While the 5-HT(2A)-mediated PIR is linearly correlated with the degree of hypertrophy, the 5-HT(4)-mediated PIR seems to increase with LV dilatation, as also seen in postinfarction CHF. ..
  37. Mackowiak M, Chocyk A, Sanak M, Czyrak A, Fijał K, Wedzony K. DOI, an agonist of 5-HT2A/2C serotonin receptor, alters the expression of cyclooxygenase-2 in the rat parietal cortex. J Physiol Pharmacol. 2002;53:395-407 pubmed
  38. Dwivedi Y, Mondal A, Payappagoudar G, Rizavi H. Differential regulation of serotonin (5HT)2A receptor mRNA and protein levels after single and repeated stress in rat brain: role in learned helplessness behavior. Neuropharmacology. 2005;48:204-14 pubmed
    ..These results demonstrate differential regulation of 5HT2A receptors in LH rats after single and repeated stress, which may be critical in the pathophysiology of depression/other stress-related disorders. ..
  39. Yamauchi M, Miyara T, Matsushima T, Imanishi T. Desensitization of 5-HT2A receptor function by chronic administration of selective serotonin reuptake inhibitors. Brain Res. 2006;1067:164-9 pubmed
    ..The desensitization of 5-HT2A receptor function might contribute to the therapeutic mechanism of action of these SSRIs, as seen with other classes of antidepressants. ..
  40. Pawlyk A, Cosmi S, Alfinito P, Maswood N, Deecher D. Effects of the 5-HT2A antagonist mirtazapine in rat models of thermoregulation. Brain Res. 2006;1123:135-44 pubmed
    ..These data support the concept that 5-HT(2A) receptors play a role in temperature regulation but that functional blockade of these receptors by mirtazapine is not a likely mechanism for restoring thermoregulatory processes in OVX rats. ..
  41. Dam H, Mellerup E, Plenge P, Winther R, Wortwein G. The serotonin transporter and 5HT2A receptor in rat brain after localized lesions. Neurol Res. 2007;29:717-22 pubmed
    ..No change was detected for 5HT2A receptor density. ..
  42. Frick L, Bernardez Vidal M, Hocht C, Zanutto B, Rapanelli M. Dual role of serotonin in the acquisition and extinction of reward-driven learning: involvement of 5-HT1A, 5-HT2A and 5-HT3 receptors. Behav Brain Res. 2015;277:193-203 pubmed publisher
    ..These data showed a differential role of 5-HT in the acquisition and extinction of an operant conditioning task, suggesting that it may have a dual function in reward encoding. ..
  43. Qvigstad E, Sjaastad I, Brattelid T, Nunn C, Swift F, Birkeland J, et al. Dual serotonergic regulation of ventricular contractile force through 5-HT2A and 5-HT4 receptors induced in the acute failing heart. Circ Res. 2005;97:268-76 pubmed
    ..Ca2+ transients were slightly decreased by 5-HT2A stimulation. The acute failing rat ventricle is, thus, dually regulated by serotonin through Gq-coupled 5-HT2A receptors and Gs-coupled 5-HT4 receptors. ..
  44. Luo B, Hu L, Liu C, Guo Y, Wang H. Activation of 5-HT2A/C receptor reduces glycine receptor-mediated currents in cultured auditory cortical neurons. Amino Acids. 2016;48:349-56 pubmed publisher
  45. Julius D, Huang K, Livelli T, Axel R, Jessell T. The 5HT2 receptor defines a family of structurally distinct but functionally conserved serotonin receptors. Proc Natl Acad Sci U S A. 1990;87:928-32 pubmed
    ..However, RNA blotting shows that these two receptor subtypes are differentially expressed in the central nervous system. In this manner, structurally and functionally homologous receptor subtypes may elicit distinct physiologic actions. ..
  46. Okamoto K, Imbe H, Morikawa Y, Itoh M, Sekimoto M, Nemoto K, et al. 5-HT2A receptor subtype in the peripheral branch of sensory fibers is involved in the potentiation of inflammatory pain in rats. Pain. 2002;99:133-43 pubmed
    ..These findings suggest that 5-HT2A receptors are mainly expressed in CGRP-synthesizing small DRG neurons and may be involved in the potentiation of inflammatory pain in the periphery. ..
  47. Okamoto K, Imbe H, Tashiro A, Kimura A, Donishi T, Tamai Y, et al. The role of peripheral 5HT2A and 5HT1A receptors on the orofacial formalin test in rats with persistent temporomandibular joint inflammation. Neuroscience. 2005;130:465-74 pubmed
  48. Mannoury la Cour C, Chaput C, Touzard M, Millan M. An immunocapture/scintillation proximity analysis of G alpha q/11 activation by native serotonin (5-HT)2A receptors in rat cortex: blockade by clozapine and mirtazapine. Synapse. 2009;63:95-105 pubmed publisher
    ..Quantification of 5-HT(2A) receptor-mediated G alpha q/11 activation in frontal cortex should prove instructive in characterizing the actions of diverse classes of psychotropic agent. ..
  49. Hofmann A, Friedmacher F, Hunziker M, Takahashi H, Duess J, Gosemann J, et al. Upregulation of serotonin-receptor-2a and serotonin transporter expression in the pulmonary vasculature of nitrofen-induced congenital diaphragmatic hernia. J Pediatr Surg. 2014;49:871-4; discussion 874-5 pubmed publisher
    ..It exerts its constricting effects on the vessels via Serotonin receptor 2A (5-HT2A) and induces pulmonary smooth muscle cell proliferation via the serotonin transporter (5-HTT)...
  50. 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
  51. Wischhof L, Irrsack E, Dietz F, Koch M. Maternal lipopolysaccharide treatment differentially affects 5-HT(2A) and mGlu2/3 receptor function in the adult male and female rat offspring. Neuropharmacology. 2015;97:275-88 pubmed publisher
    ..Since most studies in rodents almost exclusively include male subjects, our data further contribute to elucidating possible gender differences in the effects of prenatal infection on 5-HT2A and mGlu2/3 receptor function. ..
  52. Mbaki Y, Ramage A. Investigation of the role of 5-HT2 receptor subtypes in the control of the bladder and the urethra in the anaesthetized female rat. Br J Pharmacol. 2008;155:343-56 pubmed publisher
    ..Furthermore, 5-HT2B and 5-HT2C receptors do not seem to play an important role in the physiological regulation of micturition. ..
  53. Cavus I, Duman R. Influence of estradiol, stress, and 5-HT2A agonist treatment on brain-derived neurotrophic factor expression in female rats. Biol Psychiatry. 2003;54:59-69 pubmed
    ..The duration of the estradiol treatment and the duration of the ovarian hormone deprivation are important factors in the regulation of BDNF synthesis and possibly in the functional outcome of estrogen treatment. ..
  54. Rodriguez J, Garcia D, Pickel V. Subcellular distribution of 5-hydroxytryptamine2A and N-methyl-D-aspartate receptors within single neurons in rat motor and limbic striatum. J Comp Neurol. 1999;413:219-31 pubmed
    ..These results indicate that 5HT2A and NMDA receptors are coexpressed but differentially targeted in single spiny striatal neurons and are likely to play a major role in control of motor functions involving the dorsolateral CPN. ..
  55. Xie H, Dong Z, Ma F, Bauer W, Wang X, Wu G. Involvement of serotonin 2A receptors in the analgesic effect of tramadol in mono-arthritic rats. Brain Res. 2008;1210:76-83 pubmed publisher
    ..The increase in this receptor mRNA in the chronic study may contribute to the sustaining effect of tramadol long-term treatments in clinical practice. ..
  56. Fouad K, Rank M, Vavrek R, Murray K, Sanelli L, Bennett D. Locomotion after spinal cord injury depends on constitutive activity in serotonin receptors. J Neurophysiol. 2010;104:2975-84 pubmed publisher
    ..Thus while normal rats can compensate for loss of 5-HT(2) receptor activity, after severe spinal cord injury rats require constitutive activity in these 5-HT(2) receptors to produce locomotion. ..
  57. Pritchett D, Bach A, Wozny M, Taleb O, Dal Toso R, Shih J, et al. Structure and functional expression of cloned rat serotonin 5HT-2 receptor. EMBO J. 1988;7:4135-40 pubmed
    ..The agonist also elicited a current flow, blocked by spiperone, in Xenopus oocytes injected with in vitro synthesized RNA containing the cloned nucleotide sequences. ..
  58. Monti J, Jantos H. Effects of the serotonin 5-HT2A/2C receptor agonist DOI and of the selective 5-HT2A or 5-HT2C receptor antagonists EMD 281014 and SB-243213, respectively, on sleep and waking in the rat. Eur J Pharmacol. 2006;553:163-70 pubmed
    ..Thus, on the basis of these results it appears that serotonin 5-HT(2A) receptor mechanisms might be responsible for the DOI-induced effects on waking and slow wave sleep. ..
  59. Geurts F, De Schutter E, Timmermans J. Localization of 5-HT2A, 5-HT3, 5-HT5A and 5-HT7 receptor-like immunoreactivity in the rat cerebellum. J Chem Neuroanat. 2002;24:65-74 pubmed
  60. Radhakrishnan R, King E, Dickman J, Herold C, Johnston N, Spurgin M, et al. Spinal 5-HT(2) and 5-HT(3) receptors mediate low, but not high, frequency TENS-induced antihyperalgesia in rats. Pain. 2003;105:205-13 pubmed
    ..Furthermore, spinal noradrenergic receptors are not involved in either low or high frequency TENS antihyperalgesia. ..
  61. Nedergaard P, Sanchez C, Mellerup E. Different roles of 5-HT2A and 5-HT2C receptors in regulation of female rat paced mating behaviour. Behav Brain Res. 2004;149:151-7 pubmed
    ..The results may support the hypothesis that both 5-HT2A and 5-HT2C receptors are important in regulation of female sexual behaviour. ..
  62. Suwazono Y, Kobayashi E, Uetani M, Miura K, Morikawa Y, Ishizaki M, et al. The -1438A/G polymorphism in the 5-hydroxytryptamine receptor 2A gene is related to hyperuricemia, increased gamma-glutamyl transpeptidase and decreased high-density lipoprotein cholesterol level in the Japanese population: a prospective cohort study. Int J Mol Med. 2006;17:77-82 pubmed
  63. Minosyan T, Lu R, Eghbali M, Toro L, Stefani E. Increased 5-HT contractile response in late pregnant rat myometrium is associated with a higher density of 5-HT2A receptors. J Physiol. 2007;581:91-7 pubmed
    ..We conclude that the higher 5-HT-induced contractile response results from a higher density of 5-HT2A receptors having the same properties as in non-pregnant myometrium. ..
  64. Michishita M, Yano K, Kasahara K, Tomita K, Matsuzaki O. Increased expression of 5-HT(2A) and 5-HT(2B) receptors in detrusor muscle after partial bladder outlet obstruction in rats. Biomed Res. 2015;36:187-94 pubmed publisher
  65. McDonald A, Mascagni F. Neuronal localization of 5-HT type 2A receptor immunoreactivity in the rat basolateral amygdala. Neuroscience. 2007;146:306-20 pubmed
  66. Murray R, Hebbard J, Logan A, Vanchipurakel G, Gilbert Y, Horner K. Stress and withdrawal from d-amphetamine alter 5-HT2A receptor mRNA expression in the prefrontal cortex. Neurosci Lett. 2014;559:44-9 pubmed publisher
    ..Together, these data suggest that exposure to stress during extended AMPH withdrawal could prolong withdrawal-induced, 5-HT2AR mRNA expression which could be related to 5-HT2AR mediated deficits. ..
  67. Welsh D, Harnett M, MacLean M, Peacock A. Proliferation and signaling in fibroblasts: role of 5-hydroxytryptamine2A receptor and transporter. Am J Respir Crit Care Med. 2004;170:252-9 pubmed
    ..Taken together, these data suggest that selective 5-HT(2A) receptor antagonists may have a role in pulmonary artery fibroblast proliferation to hypoxia. ..
  68. Sumner B, Grant K, Rosie R, Hegele Hartung C, Fritzemeier K, Fink G. Raloxifene blocks estradiol induction of the serotonin transporter and 5-hydroxytryptamine2A receptor in female rat brain. Neurosci Lett. 2007;417:95-9 pubmed
  69. Umeda Y, Amano M, Suemaru K, Yamaguchi T, Kitamura Y, Gomita Y, et al. The Influence of hyperactivity of the hypothalamic-pituitary-adrenal axis and hyperglycemia on the 5-HT2A receptor-mediated wet-dog shake responses in rats. Acta Med Okayama. 2007;61:311-7 pubmed
    ..The results of the present study suggest that hyperglycemia is not strongly associated with the enhanced susceptibility of 5-HT2A receptors under the condition of hyperactivity of the HPA axis. ..
  70. Doyle J, Yamamoto B. Serotonin 2 receptor modulation of hyperthermia, corticosterone, and hippocampal serotonin depletions following serial exposure to chronic stress and methamphetamine. Psychoneuroendocrinology. 2010;35:629-33 pubmed publisher
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    ..Therefore, it is suggested that the 5-HT2A receptor may be partly involved in the pharmacological effects induced by the 5-HT4 receptor agonist, 5-methoxytryptamine. ..
  72. Wedzony K, Chocyk A, Mackowiak M. A search for colocalization of serotonin 5-HT2A and 5-HT1A receptors in the rat medial prefrontal and entorhinal cortices--immunohistochemical studies. J Physiol Pharmacol. 2008;59:229-38 pubmed
  73. Horner K, Gilbert Y, Noble E. Differential regulation of 5-HT2A receptor mRNA expression following withdrawal from a chronic escalating dose regimen of D-amphetamine. Brain Res. 2011;1390:10-20 pubmed publisher
  74. Takahashi T, Yano M, Minami J, Haraguchi T, Koga N, Higashi K, et al. Sarpogrelate hydrochloride, a serotonin2A receptor antagonist, reduces albuminuria in diabetic patients with early-stage diabetic nephropathy. Diabetes Res Clin Pract. 2002;58:123-9 pubmed
    ..Our study indicate that high levels of 5-HT in type 2 diabetics may be one of the underlying mechanisms of diabetic nephropathy, and that treatment with 5-HT(A2) receptor antagonists may reduce or inhibit the development of nephropathy. ..
  75. Xia Z, Hufeisen S, Gray J, Roth B. The PDZ-binding domain is essential for the dendritic targeting of 5-HT2A serotonin receptors in cortical pyramidal neurons in vitro. Neuroscience. 2003;122:907-20 pubmed
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    ..Glucose supplementation helped in managing the serotonergic functional alterations. This has immense clinical significance in neonatal care. ..
  77. Yu B, Wang A, Zhou G, Zhang W, Hu D, Li Q, et al. T102C genetic polymorphism of the 5-HT2A receptor in Chinese hypertensive patients and healthy controls. Clin Exp Pharmacol Physiol. 2004;31:847-9 pubmed
    ..We find that no correlation exists between the T102C genetic polymorphism and hypertension, which affords useful information on the pathogenesis of hypertension in the Chinese population. ..
  78. de Bortoli V, Yamashita P, Zangrossi H. 5-HT1A and 5-HT2A receptor control of a panic-like defensive response in the rat dorsomedial hypothalamic nucleus. J Psychopharmacol. 2013;27:1116-23 pubmed publisher
    ..Facilitation of 5-HT-mediated neurotransmission in the DMH may be implicated in the mode of action of antipanic drugs. ..
  79. 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. ..
  80. Anju T, Paulose C. Amelioration of hypoxia-induced striatal 5-HT(2A) receptor, 5-HT transporter and HIF1 alterations by glucose, oxygen and epinephrine in neonatal rats. Neurosci Lett. 2011;502:129-32 pubmed publisher
    ..The adverse effect of immediate oxygenation and epinephrine supplementation was also reported. This has immense clinical significance in establishing a proper resuscitation for the management of neonatal hypoxia. ..
  81. Popova N, Naumenko V, Kozhemiakina R, Pliusnina I. [Functional correlates of the brain 5-HT2A and 5-HT2C serotonin receptors and expression of 5-HT2A AND 5-HT2C genes in aggressive and nonaggressive Norway rats]. Ross Fiziol Zh Im I M Sechenova. 2009;95:99-105 pubmed
    ..The data indicate involvement of the brain 5-HT2C receptor rather than 5-HT2C receptors in the mechanisms of genetically predetermined suppression of fear-induced aggressive behavior. ..
  82. Martin Gronert M, Stocker C, Wargent E, Cripps R, Garfield A, Jovanovic Z, et al. 5-HT2A and 5-HT2C receptors as hypothalamic targets of developmental programming in male rats. Dis Model Mech. 2016;9:401-12 pubmed publisher
    ..These findings not only reveal a 5-HT-mediated mechanism underlying the programming of susceptibility to obesity, but also provide a promising means to correct it, by treatment with a 5-HT2AR agonist. ..
  83. Zaniewska M, Alenina N, Wydra K, Fröhler S, Kuśmider M, McCreary A, et al. Discovering the mechanisms underlying serotonin (5-HT)2A and 5-HT2C receptor regulation following nicotine withdrawal in rats. J Neurochem. 2015;134:704-16 pubmed publisher
    ..5-HT, serotonin; 5-HT2A R, 5-HT2A receptor; 5-HT2C R, 5-HT2C receptor. ..
  84. Kelly C, Sharif N. Pharmacological evidence for a functional serotonin-2B receptor in a human uterine smooth muscle cell line. J Pharmacol Exp Ther. 2006;317:1254-61 pubmed
    ..4 nM) in the HUSMC PI turnover assays. Taken together, these studies strongly suggest the presence of a functionally active 5-HT2B receptor subtype in HUSMCs. The physiological role of this receptor in these cells remains to be defined. ..
  85. Seebart B, Stoffel R, Behan M. Age-related changes in the serotonin 2A receptor in the hypoglossal nucleus of male and female rats. Respir Physiol Neurobiol. 2007;158:14-21 pubmed
    ..Data from the present study suggest that aging male rats fail to compensate adequately for reduced 5HT in the hypoglossal nucleus by upregulating the expression of the 5HT(2A) receptor. ..
  86. Knauer C, Campbell J, Chio C, Fitzgerald L. Pharmacological characterization of mitogen-activated protein kinase activation by recombinant human 5-HT2C, 5-HT2A, and 5-HT2B receptors. Naunyn Schmiedebergs Arch Pharmacol. 2009;379:461-71 pubmed publisher
    ..This profile differs from reports of "agonist-directed trafficking of receptor stimulus" between PI/Ca(2+) and AA pathways activated by 5-HT(2) receptors. ..