MedKoo Cat#: 558350 | Name: Ketanserinol

Description:

WARNING: This product is for research use only, not for human or veterinary use.

Ketanserinol is the metabolite of ketanserin, a hypotensive drug with 5-HT2 receptor antagonism. Ketanserin is used to reverse pulmonary hypertension caused by protamine.

Chemical Structure

Ketanserinol
Ketanserinol
CAS#76330-73-9

Theoretical Analysis

MedKoo Cat#: 558350

Name: Ketanserinol

CAS#: 76330-73-9

Chemical Formula: C22H24FN3O3

Exact Mass: 397.1800

Molecular Weight: 397.45

Elemental Analysis: C, 66.48; H, 6.09; F, 4.78; N, 10.57; O, 12.08

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
No Data
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

Preparing Stock Solutions

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.

Recalculate based on batch purity %
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
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. 2: Kurowski M. Simultaneous determination of ketanserin and ketanserinol in biological fluids using ion-pair liquid chromatography and fluorometric detection. J Chromatogr. 1985 May 31;341(1):208-12. PubMed PMID: 3160719. 3: Yassen A, Hanff LM, Vulto AG. Simultaneous quantitative analysis of ketanserin and ketanserinol in plasma by RP-HPLC with fluorescence detection. Biomed Chromatogr. 2003 Dec;17(8):517-21. PubMed PMID: 14648608. 4: Frenken M, Kaumann AJ. Interaction of ketanserin and its metabolite ketanserinol with 5HT2 receptors in pulmonary and coronary arteries of calf. Naunyn Schmiedebergs Arch Pharmacol. 1984 Jul;326(4):334-9. PubMed PMID: 6482982. 5: Lebrec D, Hadengue A, Gaudin C, Levron JC, Fraitag B, Berthelot P, Benhamou JP. Pharmacokinetics of ketanserin in patients with cirrhosis. Clin Pharmacokinet. 1990 Aug;19(2):160-6. PubMed PMID: 2379381. 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.