Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C22H22FN3O3.C4H6O6 |
| Molecular Weight | 545.5136 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
O[C@H]([C@@H](O)C(O)=O)C(O)=O.FC1=CC=C(C=C1)C(=O)C2CCN(CCN3C(=O)NC4=C(C=CC=C4)C3=O)CC2
InChI
InChIKey=KMTLTEVOQLMYRS-LREBCSMRSA-N
InChI=1S/C22H22FN3O3.C4H6O6/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)/t;1-,2-/m.1/s1
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 |
|---|---|---|---|
Target ID: CHEMBL224 |
2.7 nM [Ki] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| 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 |
|||
| 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 |
|||
| 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 |
|||
| 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 |
|---|---|---|
| Central serotonergic mechanisms on head twitch response induced by benzodiazepine receptor agonists. | 2001 |
|
| An endogenous 5-HT(7) receptor mediates pigment granule dispersion in Xenopus laevis melanophores. | 2001 Apr |
|
| Role of prostanoids and endothelins in the prevention of cyclosporine-induced nephrotoxicity. | 2001 Apr-May |
|
| Disturbance of serotonin 5HT2 receptors in remitted patients suffering from hereditary depressive disorder. | 2001 Aug |
|
| In vivo evaluation of 4-[123I]iodo-N-[2[4-(6-trifluoromethyl-2-pyridinyl)-1-piperazinyl]ethyl]benzamide, a potential SPECT radioligand for the 5-HT1A receptor. | 2001 Aug |
|
| Complex interaction of ergovaline with 5-HT2A, 5-HT1B/1D, and alpha1 receptors in isolated arteries of rat and guinea pig. | 2001 Aug |
|
| Role of 5-HT(2) receptor subtypes in depletion of 5-HT induced by p-chloroamphetamine in the mouse frontal cortex. | 2001 Aug 24 |
|
| Serotonin(2) receptors mediate respiratory recovery after cervical spinal cord hemisection in adult rats. | 2001 Dec |
|
| Influence of serotonin on the glutamate-induced excitations of secondary vestibular neurons in the rat. | 2001 Dec |
|
| Inhibitory presynaptic 5-hydroxytryptamine(2A) receptors regulate evoked glutamate release from rat cerebellar mossy fibers. | 2001 Dec |
|
| Monocyte 5-HT1A receptors mediate pindobind suppression of natural killer cell activity: modulation by catalase. | 2001 Feb |
|
| Ex vivo binding of flibanserin to serotonin 5-HT1A and 5-HT2A receptors. | 2001 Feb |
|
| The distribution of a kinin-like peptide and its co-localization with a CRF-like peptide in the blood-feeding bug, Rhodnius prolixus. | 2001 Feb |
|
| A predicted cortical serotonergic/cholinergic/GABAergic interface as a site of pathology in schizophrenia. | 2001 Jan-Feb |
|
| Researching the antidepressant actions of Hypericum perforatum (St. John's wort) in animals and man. | 2001 Jul |
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| Analyses of [(18)F] altanserin bolus injection PET data. I: consideration of radiolabeled metabolites in baboons. | 2001 Jul |
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| The effects of hypothyroidism on 5-HT1A and 5-HT2A receptors and the serotonin transporter protein in the rat brain. | 2001 Jul-Aug |
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| The cloned human 5-HT7 receptor splice variants: a comparative characterization of their pharmacology, function and distribution. | 2001 Jun |
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| Relaxation induced by serotonin and sumatriptan in isolated guinea pig gallbladder strips. | 2001 Mar |
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| Could the 5-HT1B receptor inverse agonism affect learning consolidation? | 2001 Mar |
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| Pharmacological characterization of locomotor sensitization induced by chronic phencyclidine administration. | 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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| Do mucosal mast cells contribute to the immediate asthma response? | 2001 May |
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| Conditioned antinociception and freezing using electrical stimulation of the dorsal periaqueductal gray or inferior colliculus as unconditioned stimulus are differentially regulated by 5-HT2A receptors in rats. | 2001 May |
|
| Association study of the 5-HT(2A) receptor gene polymorphism, T102C and essential hypertension. | 2001 May |
|
| Electrophysiological effects of cocaethylene, cocaine, and ethanol on dopaminergic neurons of the ventral tegmental area. | 2001 May |
|
| Phrenic long-term facilitation requires 5-HT receptor activation during but not following episodic hypoxia. | 2001 May |
|
| Anxiolytic effects of aniracetam in three different mouse models of anxiety and the underlying mechanism. | 2001 May 18 |
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| Expression of serotonin 5-HT(2A) receptors in the human cerebellum and alterations in schizophrenia. | 2001 Nov |
|
| Activation of Erk mitogen-activated protein kinase proteins by vascular serotonin receptors. | 2001 Oct |
|
| Multiple conformations of native and recombinant human 5-hydroxytryptamine(2a) receptors are labeled by agonists and discriminated by antagonists. | 2001 Oct |
|
| Inverse agonist actions of typical and atypical antipsychotic drugs at the human 5-hydroxytryptamine(2C) receptor. | 2001 Oct |
|
| Neuroepithelial bodies in mammalian lung express functional serotonin type 3 receptor. | 2001 Oct |
|
| On the role of serotonin2A/2C receptors in the sensitization to cocaine. | 2001 Sep |
|
| 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 |
|
| Serotonin receptors modulate GABA(A) receptor channels through activation of anchored protein kinase C in prefrontal cortical neurons. | 2001 Sep 1 |
|
| 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
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
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NCI_THESAURUS |
C66885
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281-062-8
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100000086461
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758959
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m6614
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83846-83-7
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645498QK7H
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SUB02831MIG
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16219944
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DTXSID701003945
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C2036
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ACTIVE MOIETY
PARENT (SALT/SOLVATE)
SUBSTANCE RECORD
