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Submit ReviewKetanserin tartrate
Description: Selective 5-HT2A antagonist. Also antagonist at 5-HT1D
Alternative Names: R 41 468
Chemical Name: 3-[2-[4-(4-Fluorobenzoyl)-1-piperidinyl]ethyl]-2,4[1H,3H]-quinazolinedione tartrate
Purity: ≥97% (HPLC)
Biological Activity for Ketanserin tartrate
Ketanserin tartrate is a selective 5-HT2A serotonin receptor antagonist; can also be used to discriminate between 5-HT1D and 5-HT1B receptor subtypes.
Technical Data for Ketanserin tartrate
| M. Wt | 545.52 |
| Formula | C22H22FN3O3.C4H6O6 |
| Storage | Store at RT |
| Purity | ≥97% (HPLC) |
| CAS Number | 83846-83-7 |
| PubChem ID | 135348 |
| InChI Key | KMTLTEVOQLMYRS-UHFFFAOYSA-N |
| Smiles | OC(C(O)C(O)=O)C(O)=O.FC1=CC=C(C=C1)C(=O)C1CCN(CCN2C(=O)NC3=CC=CC=C3C2=O)CC1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Ketanserin tartrate
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 5.45 | 10 |
Preparing Stock Solutions for Ketanserin tartrate
The following data is based on the product molecular weight 545.52. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 18.33 mL | 91.66 mL | 183.31 mL |
| 0.5 mM | 3.67 mL | 18.33 mL | 36.66 mL |
| 1 mM | 1.83 mL | 9.17 mL | 18.33 mL |
| 5 mM | 0.37 mL | 1.83 mL | 3.67 mL |
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Product Datasheets for Ketanserin tartrate
References for Ketanserin tartrate
References are publications that support the biological activity of the product.
Leyson et al (1981) Receptor binding profile of R41 468, a novel antagonist at 5-HT2 receptors. Life Sci. 28 1015 PMID: 6261070
Razzaque et al (1995) Differences in the effects of ketanserin and GR 127935 on 5-HT-receptor mediated responses in rabbit saphenous vein and guinea-pig jugular vein. Eur.J.Pharmacol. 283 199 PMID: 7498311
Van Nueten et al (1981) Vascular effects of ketanserin (R41 468), a novel antagonist of 5-HT2 serotonergic receptors. J.Pharmacol.Exp.Ther. 218 217 PMID: 6113280
Zgombick et al (1995) Ketanserin and ritanserin discriminate between recombinant human 5-HT1Dα and 5-HT1Dβ receptor subtypes. Eur.J.Pharmacol. 291 9 PMID: 8549648
If you know of a relevant reference for Ketanserin tartrate, please let us know.
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Keywords: Ketanserin tartrate, Ketanserin tartrate supplier, Selective, 5-HT2A, antagonist, 5-HT1D, Serotonin, Receptors, R41468, R, 41, 468, 0908, Tocris Bioscience
23 Citations for Ketanserin tartrate
Citations are publications that use Tocris products. Selected citations for Ketanserin tartrate include:
Saxena et al (2013) Neuroprotection through excitability and mTOR required in ALS motoneurons to delay disease and extend survival. Neuron 80 80 PMID: 24094105
Kuo et al (2014) A xanthine-derivative K(+)-channel opener protects against serotonin-induced cardiomyocyte hypertrophy via the modulation of protein kinases. Int J Biol Sci 10 64 PMID: 24391452
González-Maeso et al (2007) Hallucinogens recruit specific cortical 5-HT(2A) receptor-mediated signaling pathways to affect behavior. Mol Ther 53 439 PMID: 17270739
Morecroft et al (2012) Gene therapy by targeted adenovirus-mediated knockdown of pulmonary endothelial Tph1 attenuates hypoxia-induced pulmonary hypertension. Cereb Cortex 20 1516 PMID: 22525513
Ratner et al (2012) Cerebral markers of the serotonergic system in rat models of obesity and after Roux-en-Y gastric bypass. Neuron 20 2133 PMID: 22450706
Morecroft et al (2010) In vivo effects of a combined 5-HT1B receptor/SERT antagonist in experimental pulmonary hypertension. Int J Neuropsychopharmacol 85 593 PMID: 19736308
Mbaki (2008) 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 155 343 PMID: 18604238
Hampson et al (2007) Stimulation of glycogen synthesis and inactivation of phosphorylase in hepatocytes by serotonergic mechanisms, and counter-regulation by atypical antipsychotic drugs. Diabetologia 50 1743 PMID: 17579833
Wood et al (2011) Serotonin, via HTR2 receptors, excites neurons in a cortical-like premotor nucleus necessary for song learning and production. J Neurosci 31 13808 PMID: 21957243
Kleinbongard et al (2011) Vasoconstrictor potential of coronary aspirate from patients undergoing stenting of saphenous vein aortocoronary bypass grafts and its pharmacological attenuation. Circ Res 108 344 PMID: 21183739
Johnson et al (2011) Serotonin receptor activity is necessary for olfactory learning and memory in Drosophila melanogaster. Neuroscience 192 372 PMID: 21749913
Watakabe et al (2009) Enriched expression of serotonin 1B and 2A receptor genes in macaque visual cortex and their bidirectional modulatory effects on neuronal responses. Br J Pharmacol 19 1915 PMID: 19056862
Digranes et al (2023) High and hyper: fentanyl induces psychomotor side-effects in healthy pigs. Animals 13 1671 PMID: 37238100
Morecroft et al (1999) 5-hydroxytryptamine receptors mediating contraction in human small muscular pulmonary arteries: importance of the 5-HT1B receptor. Obesity (Silver Spring) 128 730 PMID: 10516655
Fanarioti et al (2015) Behavioral and neurochemical changes in mesostriatal DArgic regions of the rat after chronic administration of the cannabinoid receptor agonist WIN55,212-2. Synapse 18 PMID: 25522428
Kasper et al (2015) Serotonin-2C receptor agonists decrease potassium-stimulated GABA release in the nucleus accumbens. Neuropharmacology 69 78 PMID: 25382408
Jiang et al (2015) Potentiation of 5-methoxy-N,N-dimethyltryptamine-induced hyperthermia by harmaline and the involvement of activation of 5-HT1A and 5-HT2A receptors. Br J Pharmacol 89 342 PMID: 25446678
Huang et al (2009) Repeated cocaine administration decreases 5-HT(2A) receptor-mediated serotonergic enhancement of synaptic activity in rat medial prefrontal cortex. Neuropsychopharmacology 34 1979 PMID: 19212317
Marinelli et al (2004) Serotonergic and nonserotonergic dorsal raphe neurons are pharmacologically and electrophysiologically heterogeneous. J Neurophysiol 92 3532 PMID: 15254076
Nguyen et al (2019) Potentiation of the glycine response by serotonin on the substantia gelatinosa neurons of the trigeminal subnucleus caudalis in mice. Korean J Physiol Pharmacol 23 271 PMID: 31297011
Medrihan et al (2017) Initiation of Behavioral Response to Antidepressants by Cholecystokinin Neurons of the Dentate Gyrus. Neuron 95 564 PMID: 28735749
Hirono (2017) Monoaminergic modulation of GABAergic transmission onto cerebellar globular cells. Neuropharmacology 118 79 PMID: 28300552
Courtiol et al (2018) Maternal Regulation of Pups' Cortical Activity: Role of Serotonergic Signaling. Eneuro 5 PMID: 30073196
Do you know of a great paper that uses Ketanserin tartrate from Tocris? Please let us know.
Reviews for Ketanserin tartrate
Average Rating: 5 (Based on 2 Reviews.)
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Filter by:
Ketanserin.
By
Nora Digranes on 05/14/2024
Species: Other
As a 5HT2A antagonist in a porcine model
Tocris was very helpful in providing information on how to solve to powder.
Antidepressantsby Cholecystokinin Neurons of the Dentate Gyrus.
By
Anonymous on 02/03/2020
Assay Type: In Vivo
Species: Mouse
20mM ketanserin
Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
5-HT Receptors Scientific Review
Written by Nicholas M. Barnes and John F. Neumaier, this review summarizes the various serotonin receptor subtypes and their importance in mediating the role of serotonin in numerous physiological and pharmacological processes. Compounds available from Tocris are listed.
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Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.
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Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.