Details
Stereochemistry | ACHIRAL |
Molecular Formula | C22H22FN3O3 |
Molecular Weight | 395.4268 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
FC1=CC=C(C=C1)C(=O)C2CCN(CCN3C(=O)NC4=C(C=CC=C4)C3=O)CC2
InChI
InChIKey=FPCCSQOGAWCVBH-UHFFFAOYSA-N
InChI=1S/C22H22FN3O3/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/h1-8,16H,9-14H2,(H,24,29)
Molecular Formula | C22H22FN3O3 |
Molecular Weight | 395.4268 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/17147663
Sources: https://www.ncbi.nlm.nih.gov/pubmed/17147663
Ketanserin is a selective 5HT2A receptor antagonist which was initially developed as an anti-hypertensive medicine. However, now the drug is available as a topical gel formulation for the treatment of wounds, burns, ulcers and anal fissure (Sufrexal brand name). The drug action is explained by its ability to accelerate epithelialization.
CNS Activity
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
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Target ID: CHEMBL224 Sources: https://www.ncbi.nlm.nih.gov/pubmed/12569067 |
2.7 nM [Ki] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Curative | Sufrexal Approved UseNon-neoplastic dermal and uterine cervix ulcers. Traumatic wounds such as decubitus ulcers. Preparation of tissue for grafting and flaps. Uninfected burns. Regeneration of the uterine cervix. Anal fissure |
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Curative | Sufrexal Approved UseNon-neoplastic dermal and uterine cervix ulcers. Traumatic wounds such as decubitus ulcers. Preparation of tissue for grafting and flaps. Uninfected burns. Regeneration of the uterine cervix. Anal fissure |
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Curative | Sufrexal Approved UseNon-neoplastic dermal and uterine cervix ulcers. Traumatic wounds such as decubitus ulcers. Preparation of tissue for grafting and flaps. Uninfected burns. Regeneration of the uterine cervix. Anal fissure |
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Curative | Sufrexal Approved UseNon-neoplastic dermal and uterine cervix ulcers. Traumatic wounds such as decubitus ulcers. Preparation of tissue for grafting and flaps. Uninfected burns. Regeneration of the uterine cervix. Anal fissure |
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Curative | Sufrexal Approved UseNon-neoplastic dermal and uterine cervix ulcers. Traumatic wounds such as decubitus ulcers. Preparation of tissue for grafting and flaps. Uninfected burns. Regeneration of the uterine cervix. Anal fissure |
PubMed
Title | Date | PubMed |
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The role of serotonin(2) receptors in mediating cocaine-induced convulsions. | 2000 Apr |
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Mechanism of airway hyperresponsiveness to adenosine induced by allergen challenge in actively sensitized Brown Norway rats. | 2001 Apr |
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Roles of 5-HT receptors in the release and action of secretin on pancreatic secretion in rats. | 2001 Apr |
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Blood pressure patterns in pregnant patients on oral ketanserin. | 2001 Apr-May |
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Monocyte 5-HT1A receptors mediate pindobind suppression of natural killer cell activity: modulation by catalase. | 2001 Feb |
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Pharmacological characterisation of the decrease in 5-HT synthesis in the mouse brain evoked by the selective serotonin re-uptake inhibitor citalopram. | 2001 Feb |
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Intestinal serotonin acts as a paracrine substance to mediate vagal signal transmission evoked by luminal factors in the rat. | 2001 Feb 1 |
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Activation of nicotinic receptors on GABAergic amacrine cells in the rabbit retina indirectly stimulates dopamine release. | 2001 Jan-Feb |
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Analyses of [(18)F]altanserin bolus injection PET data. II: consideration of radiolabeled metabolites in humans. | 2001 Jul |
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Affinity of serotonin receptor antagonists and agonists to recombinant and native alpha1-adrenoceptor subtypes. | 2001 Jun |
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Effect of bile salts on colonic mucus secretion in isolated vascularly perfused rat colon. | 2001 Jun |
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Could the 5-HT1B receptor inverse agonism affect learning consolidation? | 2001 Mar |
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The inhibitory effect of serotonin on the spontaneous discharge of suprachiasmatic neurons in hypothalamic slice is mediated by 5-HT(7) receptor. | 2001 Mar 1 |
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Systemic vascular effects of thrombin and thrombin receptor activating peptide in rats. | 2001 Mar 15 |
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Association study of the 5-HT(2A) receptor gene polymorphism, T102C and essential hypertension. | 2001 May |
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Electrophysiological effects of cocaethylene, cocaine, and ethanol on dopaminergic neurons of the ventral tegmental area. | 2001 May |
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Phrenic long-term facilitation requires 5-HT receptor activation during but not following episodic hypoxia. | 2001 May |
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Antidepressant-like effects of aniracetam in aged rats and its mode of action. | 2001 Nov |
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Enhanced contraction to 5-hydroxytryptamine is not due to "unmasking" of 5-hydroxytryptamine(1b) receptors in the mesenteric artery of the deoxycorticosterone acetate-salt rat. | 2001 Oct |
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Ketanserin attenuates the behavioural effects of corticosterone: implications for 5-HT(2A) receptor regulation. | 2001 Oct 5 |
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Prostaglandins may participate in opioidergic and cholinergic control of the diurnal changes of tuberoinfundibular dopaminergic neuronal activity and serum prolactin level in ovariectomized, estrogen-treated rats. | 2001 Sep 1 |
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Serotonin receptors modulate GABA(A) receptor channels through activation of anchored protein kinase C in prefrontal cortical neurons. | 2001 Sep 1 |
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Stimulation of 5-HT2 receptors in the nucleus tractus solitarius enhances NMDA receptor-mediated reflex-evoked bradycardiac responses in the rat. | 2001 Sep 17 |
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Effects of 5-HT(2) receptor antagonists on the anti-immobility effects of imipramine in the forced swimming test with mice. | 2001 Sep 21 |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/17147663
Apply a thin layer twice a day (topical gel) or use one applicator every 24 hours at night before bed for two weeks (vaginal application). In case of anal fissure, apply a small amount of the gel digitally in the anus area 3 times a day, preferably after bowel movement and cleaning the area with soap and water. The minimum recommended treatment time is 15 days.
Route of Administration:
Topical
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/17147663
2% and 20% topical ketanserin significantly accelerates both the vascular epithelial rates of wound healing in full-thickness nonpathologic skin wounds.
Substance Class |
Chemical
Created
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admin
on
Edited
Thu Jul 06 23:15:23 UTC 2023
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Record UNII |
97F9DE4CT4
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Record Status |
Validated (UNII)
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Record Version |
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WHO-VATC |
QD03AX90
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WHO-ATC |
C02KD01
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NCI_THESAURUS |
C66885
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WHO-VATC |
QC02KD01
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277-680-2
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1524
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C604
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DB12465
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CHEMBL51
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D007650
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KETANSERIN
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M6614
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SUB08366MIG
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6131
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LABELED -> NON-LABELED |
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TARGET -> INHIBITOR |
Binding Assay
IC50
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SALT/SOLVATE -> PARENT |
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ACTIVE MOIETY |
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