Product Code Database
Ketanserin, sold under the brand name Sufrexal, is an antihypertensive agent which is used to treat arterial hypertension and vasospasm. It is also used in scientific research as an antiserotonergic medication in the study of the serotonin system; specifically, the 5-HT2 receptor family. The drug is taken orally.
of ketanserin include dizziness, tiredness, edema, dry mouth, weight gain, and QT interval prolongation. Ketanserin acts as a selective antagonist of the serotonin 5-HT2A, α1-adrenergic, and histamine H1 receptors. It also shows lower affinity for various other targets.
Ketanserin was discovered at Janssen Pharmaceutica in 1980. It was the first serotonin 5-HT2A receptor antagonist to be discovered that showed selectivity over other serotonin receptors. The drug is not available in the United States and is mostly no longer marketed throughout the rest of the world.
It has been used to reverse pulmonary hypertension caused by protamine (which in turn was administered to reverse the effects of heparin overdose).
The reduction in hypertension is not associated with reflex tachycardia.
It has been used in cardiac surgery.
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.
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 gels 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 aging (from below 50 Molarity per milligram tissue at around 30 years of age to over 100 above 75 years). The same research team found no significant correlation with age in their homogenate binding study.
Ketanserin has also been used with carbon (11C) Radioactivity labeled NNC112 in order to image cortical D1 receptors without contamination by 5-HT2 receptors.
Increasing research into the use of psychedelic drug as has seen ketanserin used to both trip killer, and to disentangle the specific cognitive effects of 5-HT2A activation. Ketanserin has been found to block the psychedelic effects of psilocybin, lysergic acid diethylamide (LSD), mescaline, and ayahuasca (dimethyltryptamine) in clinical studies.
| + Human molecular targets of ketanserin NIMH Psychoactive Drug Screening Program ! Target ! Affinity (Ki) ! Ref(s) | ||
| 5-HT1A | 1,044–>10,000 nM | |
| 5-HT1B | 2,515–6,300 nM | |
| 5-HT1D | 32–>10,000 nM | |
| 5-HT1E | >10,000 nM | |
| 5-HT1F | 1.25–>10,000 nM | |
| 5-HT2A | 0.20–9.8 nM | |
| 5-HT2B | 200–3,236 nM | |
| 5-HT2C | 17–186 nM | |
| 5-HT3 | >10,000 nM (rodent) | |
| 5-HT4L | 1,000 nM (rat) | |
| 5-HT5A | 20,000 nM | |
| 5-HT5B | 1,000–1,585 nM (rodent) | |
| 5-HT6 | 2,800 nM | |
| 5-HT7 | 320–1,334 nM | |
| D1 | 190–464 nM | |
| D2 | >10,000 nM | |
| D3 | ? | |
| D4 | 148 nM (canine) | |
| D5 | 2,500 nM | |
| α1A | 6.3 nM | |
| α1B | 6.3 nM | |
| α1D | 16 nM | |
| α2A | 372 nM (HT29) | |
| α2B | 199 nM | |
| α2C | 159 nM (opossum) | |
| H1 | 1.79 nM | |
| DAT | >10,000 nM | |
| VMAT1 | 1,600 nM | |
| VMAT2 | 22–540 nM |
Occupancy of the serotonin 5-HT2A receptor by ketanserin in humans has been studied.
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