WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H558350
CAS#: 76330-73-9
Description: Ketanserinol is the metabolite of ketanserin, a hypotensive drug with 5-HT2 receptor antagonism. Ketanserin is used to reverse pulmonary hypertension caused by protamine.
Hodoodo Cat#: H558350
Name: Ketanserinol
CAS#: 76330-73-9
Chemical Formula: C22H24FN3O3
Exact Mass: 397.18
Molecular Weight: 397.450
Elemental Analysis: C, 66.48; H, 6.09; F, 4.78; N, 10.57; O, 12.08
This product is not in stock, which may be available by custom synthesis.
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Synonym: Ketanserinol; Reduced ketanserin;
IUPAC/Chemical Name: 2,4(1H,3H)-Quinazolinedione, 3-(2-(4-((4-fluorophenyl)hydroxymethyl)-1-piperidinyl)ethyl)-
InChi Key: CSAITASUWRGAOT-UHFFFAOYSA-N
InChi Code: InChI=1S/C22H24FN3O3/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/h1-8,16,20,27H,9-14H2,(H,24,29)
SMILES Code: O=C(N1CCN2CCC(C(C3=CC=C(F)C=C3)O)CC2)NC4=C(C=CC=C4)C1=O
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >3 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.03.00
More Info:
| Biological target: | |
| In vitro activity: | |
| In vivo activity: |
The following data is based on the product molecular weight 397.45 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 |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | |
| In vitro protocol: | |
| In vivo protocol: |
1: Schoenwald RD, Zhu J. The ocular pharmacokinetics of ketanserin and its metabolite, ketanserinol, in albino rabbits. J Ocul Pharmacol Ther. 2000 Oct;16(5):481-95. PubMed PMID: 11110040.
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6: Hanff LM, Visser W, Roofthooft DW, Bulsink MJ, Vermes A, Steegers EA, Vulto AG. Ketanserin in pre-eclamptic patients: transplacental transmission and disposition in neonates. BJOG. 2004 Aug;111(8):863-6. PubMed PMID: 15270938.
7: Waller PC, Tucker GT, Ramsay LE. The pharmacokinetics of ketanserin after a single dose and at steady-state in hypertensive subjects. Eur J Clin Pharmacol. 1987;33(4):423-6. PubMed PMID: 3443148.
8: Cameron HA, Waller PC, Ramsay LE. Prolongation of the QT interval by ketanserin. Postgrad Med J. 1988 Feb;64(748):112-7. PubMed PMID: 3050936; PubMed
Central PMCID: PMC2428798.
9: Gould SE, Silas JH, Hosie J. Could the increased antihypertensive efficacy of
ketanserin in the elderly be due to altered pharmacokinetics? Cardiovasc Drugs Ther. 1990 Jan;4 Suppl 1:89-92. PubMed PMID: 2285655.
10: Williams FM, Leeser JE, Rawlins MD. Pharmacodynamics and pharmacokinetics of
single doses of ketanserin and propranolol alone and in combination in healthy volunteers. Br J Clin Pharmacol. 1986 Sep;22(3):301-8. PubMed PMID: 3768242; PubMed Central PMCID: PMC1401118.
11: Barendregt JN, Van Peer A, Van Der Hoeven JG, Van Oene JC, Tjandra YI. Ketanserin pharmacokinetics in patients with renal failure. Br J Clin Pharmacol.
1990 Jun;29(6):715-23. PubMed PMID: 2378791; PubMed Central PMCID: PMC1380174.
12: Meuldermans W, Van Houdt J, Mostmans E, Knaeps F, Verluyten W, Heykants J. Plasma protein binding of ketanserin and its distribution in blood. Arzneimittelforschung. 1988 Jun;38(6):794-800. PubMed PMID: 3178920.
13: Heykants J, Van Peer A, Woestenborghs R, Gould S, Mills J. Pharmacokinetics of ketanserin and its metabolite ketanserin-ol in man after intravenous, intramuscular and oral administration. Eur J Clin Pharmacol. 1986;31(3):343-50. PubMed PMID: 3792432.
14: Van Peer A, Woestenborghs R, Embrechts L, Heykants J. Pharmacokinetic approach to equilibrium between ketanserin and ketanserin-ol. Eur J Clin Pharmacol. 1986;31(3):339-42. PubMed PMID: 3792431.
15: Klimiuk PS, Kay EA, Mitchell WS, Taylor L, Gush R, Gould S, Jayson MI. Ketanserin: an effective treatment regimen for digital ischaemia in systemic sclerosis. Scand J Rheumatol. 1989;18(2):107-11. PubMed PMID: 2734594.
16: Heykants J, Michiels M, Woestenborghs R, Awouters F, Leysen JE, Schuurkes J,
Van Nueten JM. Pharmacokinetic evaluation of the in vitro and in vivo pharmacological profile of the major metabolites of ketanserin in the rat. Arzneimittelforschung. 1988 Jun;38(6):785-8. PubMed PMID: 3178918.
17: Drozdov I, Kidd M, Gustafsson BI, Svejda B, Joseph R, Pfragner R, Modlin IM.
Autoregulatory effects of serotonin on proliferation and signaling pathways in lung and small intestine neuroendocrine tumor cell lines. Cancer. 2009 Nov 1;115(21):4934-45. doi: 10.1002/cncr.24533. PubMed PMID: 19634160; PubMed Central PMCID: PMC2767432.
18: Ochs HR, Greenblatt DJ, Höller M, Labedzky L. The interactions of propranolol and ketanserin. Clin Pharmacol Ther. 1987 Jan;41(1):55-60. PubMed PMID: 3802706.
19: Lindelauf F. Determination of ketanserin and its major metabolite (reduced ketanserin) in human plasma by high-performance liquid chromatography. J Chromatogr. 1983 Oct 14;277:396-400. PubMed PMID: 6643628.
20: Meuldermans W, Hendrickx J, Woestenborghs R, Van Peer A, Lauwers W, De Cree J, Heykants J. Absorption, metabolism and excretion of ketanserin in man after oral administration. Arzneimittelforschung. 1988 Jun;38(6):789-94. PubMed PMID: 3178919.
