| Chemical & Physical Properties | |
|---|---|
| CAS Number | 83846-83-7 |
| Catalog No. | 2A-1172668 |
| Chinese Name | 酒石酸酮色林 |
| Synonyms | EINECS 281-062-8; MFCD00084651; Ketanserin tartrate salt; Ketanserin tartrate; Ketanserin (tartrate) |
| Molecular Formula | C26H28FN3O9 |
| Molecular Weight | 545.514 |
| Boiling Point | 780.4ºC at 760 mmHg |
| Appearance | solid | white |
| Water Solubility | ethanol: 3.3mg/mL |
| Storage Condition | 2-8°C |
| Application | Ketanserin tartrate is a selective 5-HT receptor antagonist. Ketanserin tartrate also inhibits hERG currents (IhERG) with an IC50 of 0.11 μM, and this effect is concentration-dependent. |
| PubChem ID | 24278121 |
| SMILES | O=C(O)C(O)C(O)C(=O)O.O=C(c1ccc(F)cc1)C1CCN(CCn2c(=O)[nH]c3ccccc3c2=O)CC1 |
| InChI | InChI=1S/C22H22FN3O3.C4H6O6.H2O/c23-17-7-5-15(6-8-17)20(27)16-9-11-25(12-10-16)13-14-26-21(28)18-3-1-2-4-19(18)24-22(26)29;5-1(3(7)8)2(6)4(9)10;/h1-8,16H,9-14H2,(H,24,29);1-2,5-6H,(H,7,8)(H,9,10);1H2 |
| InChI Key | KMTLTEVOQLMYRS-UHFFFAOYSA-N |
| Hazard Symbols | 6.1 |
| MSDS | msds/172947_2_83846_83_7.pdf |
| Bioactivity | Ketanserin tartrate is a selective 5-HT receptor antagonist. Ketanserin tartrate also blocks hERG current (IhERG) in a concentration-dependent manner (IC50=0.11 μM). Related Catalog Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor Signaling Pathways >> Autophagy >> Autophagy Signaling Pathways >> Membrane Transporter/Ion Channel >> Potassium Channel Natural Products >> Alkaloid Research Areas >> Neurological Disease Target IC50: 0.11 μM (hERG current)[1] IC50: 152±23 μM (5-HT receptor)[2] In Vitro Ketanserin at 0.3 μM inhibits the voltage-dependent step current (IhERG.step) and tail current (IhERG.tail) of hERG channels with a 5-min exposure[1]. The synergistic effect observed for AA with 5-HT is, also, blocked by the 5-HT receptor blockers cyproheptadine (IC50=22.0±7 μM), Ketanserin (IC50=152±23 μM). Ketanserin (50-350 μM) inhibits the synergism by blocking the receptor in a dose-dependent manner. The IC50 value of Cyproheptadine is 22±7 μM and Ketanserin is 152±23 μM[2]. Ketanserin inhibits platelet aggregation with an IC50 of 240 (169-339) nM[3]. In Vivo Ketanserin is a 5-HT2A receptor antagonist. Ketanserin significantly reduces BDNF protein levels in numerous brain regions (CA1 and CA3 of the hippocampus, prefrontal cortex, central amygdaloid nucleus, dorsomedial hypothalamic nucleus, dentate gyrus, shell of the nucleus accumbens and midbrain periaqueductal gray). 5-HT2A antagonist Ketanserin can significantly reduce BDNF mRNA levels in various brain regions[4]. Cell Assay The established HEK 293 cell line stably expressing hERG channels is cultured in Dulbecco's modified Eagle's medium (DMEM) supplemented with 10% foetal bovine serum, 400 μg/mL G418. The HEK 293 cell line stably expressing recombinant human cardiac KCNQ1/KCNE1 channel current (IKs) is maintained in DMEM containing 10% foetal bovine serum and 100 μg/mL hygromycin. Cells used for electrophysiology are seeded on a glass coverslip. The mutant hERG channels are constructed, and are transiently expressed in HEK 293 cells using 10 μL of Lipofectamine 2000 with 4 μg of hERG mutant cDNA in pCDNA3 vector[1]. Animal Admin Rat[4] A total of 155 specific-pathogen-free 2-month-old male Sprague-Dawley rats, weighing 180-220 g, are used. The rats are randomly divided into the following six groups: 5-HT1A receptor agonist (8-OH-DPAT) PS group (DPAT-PS group, n=30); 5-HT1A receptor antagonist (MDL73005) PS group (MDL-PS group, n=30); 5-HT2A receptor agonist (DOI) PS group (DOI-PS group, n=30); 5-HT2A receptor antagonist (Ketanserin) PS group (Ketan-PS group, n=30); the solvent control no-stress group (0.9% physiological saline group, CON group); and the PS only group (PS group, n=30). The DPAT-PS, MDL-PS, DOI-PS, Ketan-PS and PS groups are further divided into six subgroups (n=5 each) according to the time between the stress and analysis; immediately after stress, and 0.5, 1, 2, 6 and 24 hours after stress. The CON group (n=5) receive normal feed. For the Ketan-PS group, Ketanserin, dissolved in 0.9% physiological saline, is injected intraperitoneally at 5 mg/kg at 1 hour before each stress exposure. References [1]. Tang Q, 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 Oct;155(3):365-73. [2]. Khan N, et al. Investigation of cyclooxygenase and signaling pathways involved in human platelet aggregation mediated by synergistic interaction of various agonists. Drug Des Devel Ther. 2015 Jul 6;9:3497-506. [3]. Kekewska A, et al. Antiserotonergic properties of terguride in blood vessels, platelets, and valvular interstitial cells. J Pharmacol Exp Ther. 2012 Feb;340(2):369-76. [4]. Jiang DG, et al. Serotonin regulates brain-derived neurotrophic factor expression in select brain regions during acute psychological stress. Neural Regen Res. 2016 Sep;11(9):1471-1479. Chemical & Physical Properties Boiling Point 780.4ºC at 760 mmHg Molecular Formula C26H28FN3O9 Molecular Weight 545.514 Flash Point 425.8ºC Exact Mass 545.180969 PSA 190.23000 LogP 0.23910 Appearance of Characters solid | white InChIKey KMTLTEVOQLMYRS-UHFFFAOYSA-N SMILES O=C(O)C(O)C(O)C(=O)O.O=C(c1ccc(F)cc1)C1CCN(CCn2c(=O)[nH]c3ccccc3c2=O)CC1 Storage condition 2-8°C Water Solubility ethanol: 3.3mg/mL |
| Use of | Ketanserin tartrate is a selective 5-HT receptor antagonist. Ketanserin tartrate also blocks hERG current (IhERG) in a concentration-dependent manner (IC50=0.11 μM). Properties Name Ketanserin Tartrate Synonym More Synonyms Ketanserin tartrate Biological Activity Description Ketanserin tartrate is a selective 5-HT receptor antagonist. Ketanserin tartrate also blocks hERG current (IhERG) in a concentration-dependent manner (IC50=0.11 μM). Related Catalog Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor Signaling Pathways >> Autophagy >> Autophagy Signaling Pathways >> Membrane Transporter/Ion Channel >> Potassium Channel Natural Products >> Alkaloid Research Areas >> Neurological Disease In Vivo Ketanserin is a 5-HT2A receptor antagonist. Ketanserin significantly reduces BDNF protein levels in numerous brain regions (CA1 and CA3 of the hippocampus, prefrontal cortex, central amygdaloid nucleus, dorsomedial hypothalamic nucleus, dentate gyrus, shell of the nucleus accumbens and midbrain periaqueductal gray). 5-HT2A antagonist Ketanserin can significantly reduce BDNF mRNA levels in various brain regions[4]. References [1]. Tang Q, 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 Oct;155(3):365-73. [2]. Khan N, et al. Investigation of cyclooxygenase and signaling pathways involved in human platelet aggregation mediated by synergistic interaction of various agonists. Drug Des Devel Ther. 2015 Jul 6;9:3497-506. [3]. Kekewska A, et al. Antiserotonergic properties of terguride in blood vessels, platelets, and valvular interstitial cells. J Pharmacol Exp Ther. 2012 Feb;340(2):369-76. [4]. Jiang DG, et al. Serotonin regulates brain-derived neurotrophic factor expression in select brain regions during acute psychological stress. Neural Regen Res. 2016 Sep;11(9):1471-1479. Chemical & Physical Properties Molecular Formula C26H28FN3O9 Exact Mass 545.180969 PSA 190.23000 LogP 0.23910 Appearance of Characters solid | white InChIKey KMTLTEVOQLMYRS-UHFFFAOYSA-N |
| Transport Info | Shipping Name: UN |
| MSDS Transport Info | Module 14. Shipping information 14.1 UN dangerous goods number European Dangerous Regulations for land transport: 2811 International Dangerous Regulations for sea transport: 2811 International Dangerous Regulations for air transport: 2811 14.2 United Nations shipping name European Land Transport Dangerous Regulations: TOXIC SOLID, ORGANIC, N.O.S. (3-[2-[4-(4-Fluorobenzoyl)piperidino]ethyl]quinazoline- 2,4(1H3H)-dione [R-(R*,R*)]-tartrate) IMDG: TOXIC SOLID, ORGANIC, N.O.S. (3-[2-[4-(4-Fluorobenzoyl)piperidino]ethyl]quinazoline- 2,4(1H3H)-dione [R-(R*,R*)]-tartrate) International air transport hazard regulations: Toxic solid, organic, n.o.s. (3-[2-[4-(4-Fluorobenzoyl)piperidino]ethyl]quinazoline-2,4(1H3H)- dione [R-(R*,R*)]-tartrate) 14.3 Transport hazard categories European Land Transport Danger Regulations: 6.1 International Maritime Transport Danger Regulations: 6.1 International Air Transport Danger Regulations: 6.1 14.4 Package group European Land Transport Danger Regulations: III International Maritime Transport Danger Regulations: III International Air Transport Danger Regulations: III 14.5 Environmental hazards European Land Transport Danger Regulations: No International Maritime Danger Regulations International Air Transport Danger Regulations: No Marine pollutants (yes/no): No 14.6 Special reminder to users No data available |
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