Ketanserin
Ketanserin is an inhibitor of 5-HT2A receptors that exhibits antihypertensive, vasodilatory, analgesic, and pro-angiogenic activities. In animal models of hypertension, ketanserin decreases blood pressure and improves baroreceptor sensitivity and vagal tonic activity, improving left ventricular remodeling and overall cardiac function. In animal models of myocardial infarction, ketanserin increases expression of VEGF and increases capillary density in myocardial tissue. In other animal models, this compound inhibits transient receptor potential vanilloid 1 (TRPV1) channel-evoked thermal hyperalgesia. Through downstream targets, ketanserin may also inhibit α1-adrenergic receptors.
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18936492
| Cas No. |
74050-98-9 |
|---|---|
| Purity |
≥97% |
| Formula |
C22H22F3O3 |
| Formula Wt. |
395.43 |
| Chemical Name |
3-[2-[4-(4-Fluorobenzoyl)-1-piperidinyl]ethyl]-2,4[1H,3H]-quinazolinedione |
| IUPAC Name |
3-[2-[4-(4-fluorobenzoyl)piperidin-1-yl]ethyl]-1H-quinazoline-2,4-dione |
| Synonym |
Perketan; Serefrex; Ketensin |
| Melting Point |
227-235°C |
| Appearance |
Almost White Powder |
Yu JG, Zhang EH, Liu AJ, et al. Ketanserin improves cardiac performance after myocardial infarction in spontaneously hypertensive rats partially through restoration of baroreflex function. Acta Pharmacol Sin. 2013 Dec;34(12):1508-14. PMID: 24241347.
Loyd DR, Chen PB, Hargreaves KM. Anti-hyperalgesic effects of anti-serotonergic compounds on serotonin- and capsaicin-evoked thermal hyperalgesia in the rat. Neuroscience. 2012 Feb 17;203:207-15. PMID: 22209919.
van Zwieten PA, Blauw GJ, van Brummelen P. Serotonergic receptors and drugs in hypertension. Pharmacol Toxicol. 1992 Jun;70(6 Pt 2):S17-22. PMID: 1354865.
Koss MC. Mechanism of ketanserin-induced sympatho-inhibition. Eur J Pharmacol. 1991 Mar 5;194(2-3):161-6. PMID: 1676374.
Kato S, Matsuda N, Matsumoto K, et al. Dual role of serotonin in the pathogenesis of indomethacin-induced small intestinal ulceration: pro-ulcerogenic action via 5-HT3 receptors and anti-ulcerogenic action via 5-HT4 receptors. Pharmacol Res. 2012 Sep;66(3):226-234. PMID: 22699012.
