Summary: A selective serotonin receptor antagonist with weak adrenergic receptor blocking properties. The drug is effective in lowering blood pressure in essential hypertension. It also inhibits platelet aggregation. It is well tolerated and is particularly effective in older patients.

Top Publications

  1. Shen F, Wang J, Ni C, Yu J, Wang W, Su D. Ketanserin-induced baroreflex enhancement in spontaneously hypertensive rats depends on central 5-HT(2A) receptors. Clin Exp Pharmacol Physiol. 2007;34:702-7 pubmed
    1. Ketanserin may influence baroreflex function by blocking 5-HT(2A) receptors and/or alpha(1)-adrenoceptors through central and/or peripheral mechanisms. 2...
  2. Benekareddy M, Goodfellow N, Lambe E, Vaidya V. Enhanced function of prefrontal serotonin 5-HT(2) receptors in a rat model of psychiatric vulnerability. J Neurosci. 2010;30:12138-50 pubmed publisher
    ..Together, our results demonstrate enhanced prefrontal 5-HT(2) receptor function and persistent alterations in prefrontal gene expression in a rat model of psychiatric vulnerability. ..
  3. Koudas V, Nikolaou A, Hourdaki E, Giakoumaki S, Roussos P, Bitsios P. Comparison of ketanserin, buspirone and propranolol on arousal, pupil size and autonomic function in healthy volunteers. Psychopharmacology (Berl). 2009;205:1-9 pubmed publisher
    ..The human pupil may be a suitable physiological test system for the assessment of excessive daytime sleepiness (EDS), but pupillometric assessment could be confounded by medication for comorbid hypertension and mood disorders...
  4. Papageorgiou A, Denef C. Stimulation of growth hormone release by 5-hydroxytryptamine (5-HT) in cultured rat anterior pituitary cell aggregates: evidence for mediation by 5-HT2B, 5-HT7, 5-HT1B, and ketanserin-sensitive receptors. Endocrinology. 2007;148:4509-22 pubmed
    ..The GH response was fully blocked by combined administration of SB-206553+SB-269970 and SB-206553+ketanserin but not by SB-206553+spiperone...
  5. Blomeley C, Bracci E. Excitatory effects of serotonin on rat striatal cholinergic interneurones. J Physiol. 2005;569:715-21 pubmed
    ..Consistently, the 5-HT2 receptor antagonist ketanserin (10 microm) fully blocked the excitatory effects of serotonin...
  6. Xie H, Shen F, Cao Y, Li H, Su D. Effects of low-dose ketanserin on blood pressure variability, baroreflex sensitivity and end-organ damage in spontaneously hypertensive rats. Clin Sci (Lond). 2005;108:547-52 pubmed
    The present study was designed to investigate the effects of low-dose ketanserin on BPV (blood pressure variability), BRS (baroreflex sensitivity) and organ damage in SHR (spontaneously hypertensive rats)...
  7. Kommalage M, Höglund A. Involvement of spinal serotonin receptors in the regulation of intraspinal acetylcholine release. Eur J Pharmacol. 2005;509:127-34 pubmed
    ..hydrochloride and the 5-HT2A receptor selective antagonist ketanserin tartrate inhibited the 8-OH-DPAT and the m5-HT induced acetylcholine release...
  8. Miao C, Xie H, Yu H, Chu Z, Su D. Ketanserin stabilizes blood pressure in conscious spontaneously hypertensive rats. Clin Exp Pharmacol Physiol. 2003;30:189-93 pubmed
    ..The present study was designed to investigate the effect of ketanserin, a 5-HT2A receptor antagonist with a weak alpha1-adrenoceptor blocking effect, on BPV in conscious spontaneously ..
  9. Wang D, Gao Y, Ji H, Hong Y. Topical and systemic administrations of ketanserin attenuate hypersensitivity and expression of CGRP in rats with spinal nerve ligation. Eur J Pharmacol. 2010;627:124-30 pubmed publisher
    ..To evaluate a potential therapy the 5-HT(2A) receptor antagonist ketanserin was administered topically or subcutaneously in rats with L5 nerve ligation...

More Information


  1. Yu J, Song S, Shu H, Fan S, Liu A, Liu C, et al. Baroreflex deficiency hampers angiogenesis after myocardial infarction via acetylcholine-?7-nicotinic ACh receptor in rats. Eur Heart J. 2013;34:2412-20 pubmed publisher
    ..Human studies have associated arterial baroreflex (ABR) deficiency with higher rate of sudden death after MI. The present work was designed to examine whether ABR deficiency affects angiogenesis in MI rats...
  2. Wang X, Liao Y, Zou A, Li L, Tu D. Blockade action of ketanserin and increasing effect of potassium ion on Kv1.3 channels expressed in Xenopus oocytes. Pharmacol Res. 2007;56:148-54 pubmed
    The goal of this study was to investigate the pharmacological effects of ketanserin (KT) and elevated extracellular potassium ([K+]o) on Kv1.3 potassium channels. Kv1...
  3. Hong Y, Ji H, Wei H. Topical ketanserin attenuates hyperalgesia and inflammation in arthritis in rats. Pain. 2006;124:27-33 pubmed
    We investigated effects of topical application of ketanserin, a 5-HT2A receptor antagonist, on hyperalgesia and edema in the arthritic rat, a chronic pain model with inflammation...
  4. Obata H, Saito S, Sakurazawa S, Sasaki M, Usui T, Goto F. Antiallodynic effects of intrathecally administered 5-HT(2C) receptor agonists in rats with nerve injury. Pain. 2004;108:163-9 pubmed
    ..The preferential 5-HT(2A) receptor antagonist ketanserin (30 microg) did not reverse the effects...
  5. Lau W, Chan S, Law A, Ip M, Mak J. The role of MAPK and Nrf2 pathways in ketanserin-elicited attenuation of cigarette smoke-induced IL-8 production in human bronchial epithelial cells. Toxicol Sci. 2012;125:569-77 pubmed publisher
    ..Blockade of serotonin receptor 2A (5-HTR(2A)) with ketanserin has been found to improve lung function in COPD patients...
  6. Jacono F, Peng Y, Kumar G, Prabhakar N. Modulation of the hypoxic sensory response of the carotid body by 5-hydroxytryptamine: role of the 5-HT2 receptor. Respir Physiol Neurobiol. 2005;145:135-42 pubmed
    ..b>Ketanserin (40 microM), a 5-HT2 receptor antagonist completely prevented 5-HT-induced prolongation of the HSR, whereas had ..
  7. Pilar Cuéllar F, Vidal R, Pazos A. Subchronic treatment with fluoxetine and ketanserin increases hippocampal brain-derived neurotrophic factor, ?-catenin and antidepressant-like effects. Br J Pharmacol. 2012;165:1046-57 pubmed publisher well as 5-HT(1A) receptor function were measured in the hippocampus of rats treated with fluoxetine, ketanserin and fluoxetine + ketanserin for 7 days, followed by a forced swimming test (FST) to analyse antidepressant ..
  8. Liu C, Zhang G, Song S, Cai G, Liu W, Miao C, et al. Effects of ketanserin on endotoxic shock and baroreflex function in rodents. J Infect Dis. 2011;204:1605-12 pubmed publisher
    b>Ketanserin, a 5-hydroxytryptamine receptor antagonist, is clinically used as an antihypertensive agent and could enhance baroreflex function...
  9. Silveira J, Dias Q, Del Bel E, Prado W. Serotonin receptors are involved in the spinal mediation of descending facilitation of surgical incision-induced increase of Fos-like immunoreactivity in rats. Mol Pain. 2010;6:17 pubmed publisher
    ..V of atropine-treated rats; were inhibited in the ipsilateral lamina I/II by 5-HT1/2B/2C (methysergide), 5-HT2A (ketanserin) or 5-HT1/2A/2C/5/6/7 (methiothepin) receptors antagonists, in the ipsilateral lamina V by methysergide or ..
  10. Elbers P, Ozdemir A, van Iterson M, van Dongen E, Ince C. Microcirculatory imaging in cardiac anesthesia: ketanserin reduces blood pressure but not perfused capillary density. J Cardiothorac Vasc Anesth. 2009;23:95-101 pubmed publisher
    ..b>Ketanserin, a serotonin and alpha-1 adrenoceptor antagonist, is used in some countries to treat elevated blood pressure ..
  11. Fu Y, Shu H, Miao C, Wang M, Su D. Restoration of baroreflex function by ketanserin is not blood pressure dependent in conscious freely moving rats. J Hypertens. 2004;22:1165-72 pubmed
    ..In our previous studies, it was found that ketanserin lowered blood pressure (BP), decreased BP variability and enhanced baroreflex sensitivity (BRS)...
  12. Schneider T, Struijk P, Lotgering F, Wallenburg H. Placental transfer and maternal and fetal hemodynamic effects of ketanserin in the pregnant ewe. Eur J Obstet Gynecol Reprod Biol. 1996;68:179-84 pubmed
    To determine placental transfer of ketanserin and to assess the effect of serotonin-2 receptor blockade by ketanserin on serotonin- and phenylephrine-induced vasoconstriction.
  13. Gilles M, Wilke A, Kopf D, Nonell A, Lehnert H, Deuschle M. Antagonism of the serotonin (5-HT)-2 receptor and insulin sensitivity: implications for atypical antipsychotics. Psychosom Med. 2005;67:748-51 pubmed
    ..included in a double-blind, placebo-controlled crossover study of a single dose of 40 mg of the 5-HT2 antagonist ketanserin versus placebo. Insulin sensitivity was measured by means of the euglycemic-hyperinsulinemic clamp technique...
  14. Chang C, Chen S, Lin M. Ipsapirone and ketanserin protects against circulatory shock, intracranial hypertension, and cerebral ischemia during heatstroke. Shock. 2005;24:336-40 pubmed
    We assess the effects of ipsapirone (a 5-HT1A receptor agonist), ketanserin (a 5-HT2A receptor antagonist), (-)-pindolol (a 5-HT1A receptor antagonist), and DOI (a 5-HT2A receptor agonist) on heatstroke in a rat model...
  15. Glennon R, Metwally K, Dukat M, Ismaiel A, De los Angeles J, Herndon J, et al. Ketanserin and spiperone as templates for novel serotonin 5-HT(2A) antagonists. Curr Top Med Chem. 2002;2:539-58 pubmed
    The structures of ketanserin (1) and spiperone (2) were examined in detail to determine the role of various substituent groups on 5-HT(2A) receptor affinity and selectivity...
  16. Cogolludo A, Moreno L, Lodi F, Frazziano G, Cobeño L, Tamargo J, et al. Serotonin inhibits voltage-gated K+ currents in pulmonary artery smooth muscle cells: role of 5-HT2A receptors, caveolin-1, and KV1.5 channel internalization. Circ Res. 2006;98:931-8 pubmed
    ..The effects of 5-HT on KV currents and contraction were markedly prevented by the 5-HT2A receptor antagonist ketanserin. Incubation with inhibitors of phospholipase C (U73122), classic protein kinase Cs (Gö6976), or tyrosine ..
  17. Johnson J, Kitts C. Serotonergic mediation of a negative feedback effect of estrogen on luteinizing hormone release in ovariectomized rats. Endocrinology. 1988;123:2270-5 pubmed
    Effects of the serotonin receptor antagonists ketanserin, metergoline, and methysergide on LH release were tested in ovariectomized (OVX) rats pretreated with estradiol benzoate (EB) (5 micrograms/100 g BW) on each of the 2 days preceding ..
  18. Watts S. Serotonin-induced contraction in mesenteric resistance arteries: signaling and changes in deoxycorticosterone acetate-salt hypertension. Hypertension. 2002;39:825-9 pubmed
    ..5-HT-induced contraction in DOCA-salt small arteries was shifted competitively by the 5-HT2A receptor antagonist ketanserin (-log K(B) [mol/L] for both sham and DOCA-salt, 9.25+/-0...
  19. Sheets L, Cook L, Reiter L. Serotonergic modulation of the acoustic startle response in rats during preweaning development. Pharmacol Biochem Behav. 1989;33:415-22 pubmed
    ..The 5-HT2 receptor antagonists cyproheptadine (5 mg/kg) and ketanserin (5 mg/kg) blocked the effect of MeODMT at both ages, providing some evidence that MeODMT increased the ASR ..
  20. Fink G, Dow R, McQueen J, Bennie J, Carroll S. Serotonergic 5-HT2A receptors important for the oestradiol-induced surge of luteinising hormone-releasing hormone in the rat. J Neuroendocrinol. 1999;11:63-9 pubmed
    ..00 h of presumptive pro-oestrus. This oestradiol-induced surge of LHRH was blocked by ketanserin, ritanserin and the highly selective 5-HT2A receptor antagonist, RP62203, but not by fluoxetine...
  21. Varty G, Higgins G. Reversal of dizocilpine-induced disruption of prepulse inhibition of an acoustic startle response by the 5-HT2 receptor antagonist ketanserin. Eur J Pharmacol. 1995;287:201-5 pubmed
    ..The present study was therefore designed to examine the effect of the 5-HT2 receptor antagonist, ketanserin, against a dizocilpine-induced disruption of prepulse inhibition, as well as the behavioural stereotypy produced ..
  22. Moyanova S, Kortenska L, Kirov R. High-voltage electroencephalogram spindles in rats, aging and 5-HT2 antagonism. Brain Res. 1998;786:55-63 pubmed
    ..The EEG parameters were analyzed after i.p. administration of three 5-HT2 receptor antagonists: ketanserin, ritanserin and cyproheptadine...
  23. Ashton J, Ogletree M, Michel I, Golino P, McNatt J, Taylor A, et al. Cooperative mediation by serotonin S2 and thromboxane A2/prostaglandin H2 receptor activation of cyclic flow variations in dogs with severe coronary artery stenoses. Circulation. 1987;76:952-9 pubmed
    ..dogs, CFVs were established after constrictor placement, abolished with the serotonin (5HT2) receptor antagonist ketanserin, and reestablished by the continuous infusion of serotonin into the left atrium...
  24. Quatresooz P, Kharfi M, Paquet P, Vroome V, Cauwenbergh G, Pierard G. Healing effect of ketanserin on chronic leg ulcers in patients with diabetes. J Eur Acad Dermatol Venereol. 2006;20:277-81 pubmed
    The treatment of chronic leg ulcers remains a stubborn problem in many patients. Topical 2% ketanserin ointment, a 5HT2-serotoninergic blocking agent, has been reported to improve healing of decubitus, venous, diabetic and ischaemic ..
  25. Sheline Y, Mintun M, Barch D, Wilkins C, Snyder A, Moerlein S. Decreased hippocampal 5-HT(2A) receptor binding in older depressed patients using [18F]altanserin positron emission tomography. Neuropsychopharmacology. 2004;29:2235-41 pubmed
    ..04) than previously treated subjects (n = 10). It may be that prior medication treatment provides a compensatory upregulation of the 5-HT(2A) receptor. ..
  26. Günther L, Liebscher S, Jahkel M, Oehler J. Effects of chronic citalopram treatment on 5-HT1A and 5-HT2A receptors in group- and isolation-housed mice. Eur J Pharmacol. 2008;593:49-61 pubmed publisher
    ..Isolation-induced receptor binding changes were partly normalized by chronic citalopram treatment, suggesting the isolation housing model for further analyses of SSRI effects, especially at the behavioral level. ..
  27. Colmenares Aguilar M, Lima L. Role of 5-HT2 and 5-HT7 Serotonin Receptors, and Protein Kinases C and A on Taurine Transport in Lymphocytes of Rats Treated with Fluoxetine. Adv Exp Med Biol. 2017;975 Pt 2:1129-1140 pubmed publisher
    ..of 5-HT2 receptor, 1-(2,5-dimethoxy-4-iodophenyl)-?2-aminopropane (DOI) counteract this effect, and ketanserin provoked no change in fluoxetine effect...
  28. 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
    ..increases in body temperature and CORT secretion and that these increases are blocked by the 5-HT2 antagonist ketanserin. Furthermore, the combination of stress and methamphetamine depletes 5-HT content in the hippocampus 7 days ..
  29. Sousa F, Anversa R, Birmann P, de Souza M, Balaguez R, Alves D, et al. Contribution of dopaminergic and noradrenergic systems in the antinociceptive effect of ?-(phenylalanyl) acetophenone. Pharmacol Rep. 2017;69:871-877 pubmed publisher
    ..7mg/kg, ip), ketanserin (selective antagonist of serotonergic 5-HT2A/2C, 0...
  30. Akash K, Balarama K, Paulose C. Enhanced 5-HT(2A) receptor status in the hypothalamus and corpus striatum of ethanol-treated rats. Cell Mol Neurobiol. 2008;28:1017-25 pubmed publisher
    ..Brain is the major target for the actions of ethanol and it can affect the brain in a variety of ways. In the present study we have investigated the changes in 5-HT level and the 5-HT(2A) receptors in the ethanol-treated rats...
  31. Rezvani A, Caldwell D, Levin E. Nicotinic-serotonergic drug interactions and attentional performance in rats. Psychopharmacology (Berl). 2005;179:521-8 pubmed
    ..The current study served to determine the impact of a relatively selective 5-HT2A receptor antagonist, ketanserin, on attentional function in rats and the interactions of ketanserin with nicotine administration...
  32. Li J, Unzeitig A, Javors M, Rice K, Koek W, France C. Discriminative stimulus effects of 1-(2,5-dimethoxy-4-methylphenyl)-2-aminopropane (DOM), ketanserin, and (R)-(+)-{alpha}-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-pipidinemethanol (MDL100907) in rats. J Pharmacol Exp Ther. 2009;331:671-9 pubmed publisher
    ..0 mg/kg 5-HT(2A) receptor antagonist ketanserin, or 0...
  33. Huang J, Cai Q, Chen Y, Hong Y. Treatment with ketanserin produces opioid-mediated hypoalgesia in the late phase of carrageenan-induced inflammatory hyperalgesia in rats. Brain Res. 2009;1303:39-47 pubmed publisher
    ..The 5-HT(2A) receptor antagonist ketanserin administered
  34. Ding L, He S, Wu W, Jin H, Zhu P, Zhang J, et al. Discovery and Structure-Based Optimization of 6-Bromotryptamine Derivatives as Potential 5-HT2A Receptor Antagonists. Molecules. 2015;20:17675-83 pubmed publisher
    ..Remarkably, 6-bromo-N-hexanoyltryptamine (5) displayed the most effective inhibitory activity, which was 5-fold stronger than that of the parent compound 1 and showed 70% efficacy of the positive control (ketanserin tartrate).
  35. Ettrup A, Svarer C, McMahon B, da Cunha Bang S, Lehel S, Møller K, et al. Serotonin 2A receptor agonist binding in the human brain with [(11)C]Cimbi-36: Test-retest reproducibility and head-to-head comparison with the antagonist [(18)F]altanserin. Neuroimage. 2016;130:167-174 pubmed publisher
  36. Hsiao C, Wu N, Chandler S. Voltage-dependent calcium currents in trigeminal motoneurons of early postnatal rats: modulation by 5-HT receptors. J Neurophysiol. 2005;94:2063-72 pubmed
    ..the 5-HT1A antagonist 1-(2-methoxyphenyl)-4-[4-(2-phthalimido)butyl]piperazine hydrobromide (NAN-190) but not by ketanserin, a 5-HT(2/1C) antagonist...
  37. Blanckaert P, Burvenich I, Staelens S, De Bruyne S, Moerman L, Wyffels L, et al. Effect of cyclosporin A administration on the biodistribution and multipinhole muSPECT imaging of [123I]R91150 in rodent brain. Eur J Nucl Med Mol Imaging. 2009;36:446-53 pubmed publisher
    ..cyclosporin A injection was compared to the brain uptake in untreated animals, and a displacement study with ketanserin was performed in both groups...
  38. de Souza Moreno V, Bicego K, Szawka R, Anselmo Franci J, Gargaglioni L. Serotonergic mechanisms on breathing modulation in the rat locus coeruleus. Pflugers Arch. 2010;459:357-68 pubmed publisher
    ..6 and 56 mM), 8-OHDPAT (5-HT(1A/7) agonist, 7 and 15 mM), Ketanserin (5-HT(2A) antagonist, 3...
  39. Pobbe R, Zangrossi H. The lateral habenula regulates defensive behaviors through changes in 5-HT-mediated neurotransmission in the dorsal periaqueductal gray matter. Neurosci Lett. 2010;479:87-91 pubmed publisher
    ..The results showed that intra-dPAG injection of WAY-100635 or ketanserin, 5-HT(1A) and 5-HT(2A/2C) receptor antagonists, respectively, counteracted the anti-escape effect caused by ..
  40. Yasuda K, Suemaru K, Araki H, Gomita Y. Effect of nicotine cessation on the central serotonergic systems in mice: involvement of 5-HT(2) receptors. Naunyn Schmiedebergs Arch Pharmacol. 2002;366:276-81 pubmed
  41. Frokjaer V, Erritzoe D, Madsen J, Paulson O, Knudsen G. Gender and the use of hormonal contraception in women are not associated with cerebral cortical 5-HT 2A receptor binding. Neuroscience. 2009;163:640-5 pubmed publisher
    ..31). In conclusion, neither gender, nor the use of hormonal contraception in premenopausal women was associated with cortical 5-HT(2A) receptor binding. ..
  42. Hanff L, Visser W, Roofthooft D, Bulsink M, Vermes A, Steegers E, et al. Ketanserin in pre-eclamptic patients: transplacental transmission and disposition in neonates. BJOG. 2004;111:863-6 pubmed
    The aim of this prospective, observational study was to assess transplacental transmission of ketanserin, an antihypertensive drug used in pre-eclampsia, and to determine disposition and effects in the neonate after maternal ketanserin ..
  43. da Silva A, Gargaglioni L, Branco L. 5-HT2A serotoninergic receptor in the locus coeruleus participates in the first phase of lipopolysaccharide-induced fever. Can J Physiol Pharmacol. 2007;85:497-501 pubmed
    ..To this end, 5-HT1A (WAY-100635; 3 microg/100 nL) and 5-HT2A (ketanserin; 2 microg/100 nL) antagonists were microinjected into the LC and body temperature was monitored by biotelemetry...
  44. Mintun M, Sheline Y, Moerlein S, Vlassenko A, Huang Y, Snyder A. Decreased hippocampal 5-HT2A receptor binding in major depressive disorder: in vivo measurement with [18F]altanserin positron emission tomography. Biol Psychiatry. 2004;55:217-24 pubmed
    ..Altered serotoninergic function in the hippocampus is likely involved in the disturbances of mood regulation in major depressive disorder, although the specific role of the 5-HT(2A) receptor changes is still unclear. ..
  45. Aringhieri S, Kolachalam S, Gerace C, Carli M, Verdesca V, Brunacci M, et al. Clozapine as the most efficacious antipsychotic for activating ERK 1/2 kinases: Role of 5-HT2A receptor agonism. Eur Neuropsychopharmacol. 2017;27:383-398 pubmed publisher
    ..In relation to ERK1/2 activation, we found that 5-HT2A serotonin receptor antagonists Ketanserin and M100907, both partially reduced Clozapine effect...
  46. Yang C, Wu R, Wu C, Lin T, Tsai H. Sleep deprivation enhances peripheral serotonin secretion to regulate the large follicle steroidogenesis of rats. Taiwan J Obstet Gynecol. 2015;54:260-5 pubmed publisher
    ..The inhibitory effects of serotonin could be reduced by the serotonin receptor antagonist ketanserin. These findings suggest that decreased serum estradiol concentrations in SD rats may be the result of serotonin-..
  47. Löfdahl A, Wenglén C, Rydell Törmänen K, Westergren Thorsson G, Larsson Callerfelt A. Effects of 5-Hydroxytryptamine Class 2 Receptor Antagonists on Bronchoconstriction and Pulmonary Remodeling Processes. Am J Pathol. 2018;188:1113-1119 pubmed publisher
    ..were pretreated with 5-HT2B receptor antagonists (EXT5, EXT9, RS 127445, and PRX 08066), as well as ketanserin (5-HT2A/2C receptor antagonist) (1, 10 μmol/L), before addition of cumulative concentrations of 5-..
  48. Nguyen H, Nguyen H, Islam M, Obi T, Pothinuch P, Zar P, et al. Pharmacological characteristics of Artemisia vulgaris L. in isolated porcine basilar artery. J Ethnopharmacol. 2016;182:16-26 pubmed publisher
    ..was competitively inhibited by methiothepin (a 5-HT1 and 5-HT2 receptor antagonist) in the presence of ketanserin (a 5-HT2 receptor antagonist)...
  49. 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
    ..Brain 5-HT2A/2C receptors were analyzed on day 3 of nicotine withdrawal. Nicotine withdrawal increased [(3)H]ketanserin binding to 5-HT2A receptors in the ventral tegmental area and ventral dentate gyrus, yet decreased binding in ..
  50. Juárez P, Valdovinos M, May M, Lloyd B, Couppis M, Kennedy C. Serotonin?A/C receptors mediate the aggressive phenotype of TLX gene knockout mice. Behav Brain Res. 2013;256:354-61 pubmed publisher
    ..Dose-effect functions were established for clozapine (0.1-1.5mg/kg, ip), ketanserin (0.3-1.25 mg/kg, ip), and (±)-1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane [(±)DOI] (0.5-2.0 mg/kg, ip)...
  51. Hurlemann R, Schlaepfer T, Matusch A, Reich H, Shah N, Zilles K, et al. Reduced 5-HT(2A) receptor signaling following selective bilateral amygdala damage. Soc Cogn Affect Neurosci. 2009;4:79-84 pubmed publisher
    ..Our findings provide important insights into the molecular architecture of human anxiety behaviors and suggest the 5-HT(2A) receptor as a promising pharmacological target to control pathological anxiety. ..
  52. Quednow B, Kometer M, Geyer M, Vollenweider F. Psilocybin-induced deficits in automatic and controlled inhibition are attenuated by ketanserin in healthy human volunteers. Neuropsychopharmacology. 2012;37:630-40 pubmed publisher automatic and controlled inhibition in healthy humans could be attenuated by the 5-HT(2A/2C)R antagonist ketanserin. A total of 16 healthy participants received placebo, ketanserin (40?mg p.o.), psilocybin (260??g/kg p.o...
  53. Tang Q, Li Z, Li W, Guo J, Sun H, Zhang X, et al. The 5-HT2 antagonist ketanserin is an open channel blocker of human cardiac ether-à-go-go-related gene (hERG) potassium channels. Br J Pharmacol. 2008;155:365-73 pubmed publisher
    b>Ketanserin, a selective 5-HT receptor antagonist, prolongs the QT interval of ECG in patients...