A 2000
Cochrane Review found that, compared to placebo, ketanserin did not provide significant relief for people suffering from
Raynaud's phenomenon attacks in the setting of
progressive systemic sclerosis (an autoimmune disorder). While the frequency of the attacks was unaffected by ketanserin, there was a reduction in the duration of the individual attacks. However, due to the significant adverse effect burden, the authors concluded that ketanserin's utility for this indication is likely unbeneficial.[12]
Ketanserin is a selective 5-HT2A receptor antagonist that was initially developed as an anti-hypertensive medicine. However, now the drug is available as a
topical gel formulation for treating wounds, burns, ulcers, and anal fissures. Its action is through the acceleration of epithelialization.
An autoradiography study of the human
cerebellum has found an increasing binding of 3H-ketanserin with
age (from below 50
femtomol per milligram tissue at around 30 years of age to over 100 above 75 years).[15] The same research team found no significant correlation with age in their
homogenate binding study.
Ketanserin has also been used with
carbon (11C)
radioactively labeled NNC112 in order to image cortical
D1 receptors without contamination by 5-HT2 receptors.[16]
Increasing research into the use of
psychedelics as
antidepressants has seen ketanserin used to both block the hallucinogenic experience, and to disentangle the specific cognitive effects of 5-HT2A activation.[17]
Either 3-(2-Chloroethyl)quinazoline-2,4(1H,3H)-dione [5081-87-8] (1a), or alternatively 2,3-dihydro-[1,3]oxazolo[2,3-b]quinazolin-5-one [52727-44-3] (1b) can be used as starting material. Attachment of the sidechain to 4-(4-Fluorobenzoyl)piperidine [56346-57-7] (2) completes synthesis synthesis of Ketanserin (3).
^Elbers PW, Ozdemir A, van Iterson M, van Dongen EP, Ince C (February 2009). "Microcirculatory Imaging in Cardiac Anesthesia: Ketanserin Reduces Blood Pressure But Not Perfused Capillary Density". Journal of Cardiothoracic and Vascular Anesthesia. 23 (1): 95–101.
doi:
10.1053/j.jvca.2008.09.013.
PMID19058975.
^Eickhoff SB, Schleicher A, Scheperjans F, Palomero-Gallagher N, Zilles K (February 2007). "Analysis of neurotransmitter receptor distribution patterns in the cerebral cortex". NeuroImage. 34 (4): 1317–1330.
doi:
10.1016/j.neuroimage.2006.11.016.
PMID17182260.
S2CID23363050.
^Pazos A, Probst A, Palacios JM (April 1987). "Serotonin receptors in the human brain--IV. Autoradiographic mapping of serotonin-2 receptors". Neuroscience. 21 (1): 123–139.
doi:
10.1016/0306-4522(87)90327-7.
PMID3601071.
S2CID23711420.
^Eastwood SL, Burnet PW, Gittins R, Baker K, Harrison PJ (November 2001). "Expression of serotonin 5-HT(2A) receptors in the human cerebellum and alterations in schizophrenia". Synapse. 42 (2): 104–114.
doi:
10.1002/syn.1106.
PMID11574947.
S2CID40304220.
^Creed-Carson M, Oraha A, Nobrega JN (June 2011). "Effects of 5-HT(2A) and 5-HT(2C) receptor antagonists on acute and chronic dyskinetic effects induced by haloperidol in rats". Behavioural Brain Research. 219 (2): 273–279.
doi:
10.1016/j.bbr.2011.01.025.
PMID21262266.
S2CID205882443.
^US 4335127, Vandenberk J, Kennis L, Van der Aa M, Van Heertum A, issued 1982, assigned to Janssen Pharmaceutica, N.V.
^EP 0098499, Signorini R, Verga A, issued 1984, assigned to Ravizza SpA
^CN 106866625, Shiwen R, et al., issued 2017, assigned to Shanghai Ding Ya Pharmaceutical Chemistry Science And Technology Ltd)
^Fakhraian H, Heydary M (January 2014). "Reinvestigation of the Synthesis of Ketanserin (5) and its Hydrochloride Salt (5. HCl) via 3-(2-Chloroethyl)-2, 4-(1H, 3H)-quinazolinedione (2) or Dihydro-5H-oxazole (2, 3-b) quinazolin-5-one (1)". Journal of Heterocyclic Chemistry. 51 (1): 151–156.
doi:
10.1002/jhet.1897..
^Herndon JL, Ismaiel A, Ingher SP, Teitler M, Glennon RA (December 1992). "Ketanserin analogues: structure-affinity relationships for 5-HT2 and 5-HT1C serotonin receptor binding". Journal of Medicinal Chemistry. 35 (26): 4903–10.
doi:
10.1021/jm00104a017.
PMID1479590.