Urapidil hydrochloride Chemische Eigenschaften,Einsatz,Produktion Methoden
R-Sätze Betriebsanweisung:
R22:Gesundheitsschädlich beim Verschlucken.
R36/37/38:Reizt die Augen, die Atmungsorgane und die Haut.
S-Sätze Betriebsanweisung:
S26:Bei Berührung mit den Augen sofort gründlich mit Wasser abspülen und Arzt konsultieren.
S36:DE: Bei der Arbeit geeignete Schutzkleidung tragen.
Beschreibung
Urapidil is an antagonist of α
1-adrenergic receptors (α
1-ARs) and a partial agonist of the serotonin (5-HT) receptor subtype 5-HT
1A. It selectively binds to α
1- over α
2-ARs (IC
50s = 0.74 and 42 μM, respectively) and to 5-HT
1A over 5-HT
1B and 5-HT
2 receptors (IC
50s = 0.4, 20.4, and >10 μM, respectively) in rat cortex. Urapidil inhibits cAMP accumulation induced by forskolin in calf hippocampus as a functional model for 5-HT
1A receptors (EC
50 = 390 nM). It is also a β
1-AR antagonist that inhibits the positive chronotropic response induced by isoproterenol in isolated rat atria (pA
2 = 6.05). Urapidil (1 μmol/kg, i.v.) lowers mean arterial pressure (MAP) in anesthetized cats, an effect that is reduced by central administration of the 5-HT
1A receptor antagonist spiroxatrine.
Chemische Eigenschaften
White to Off-White Crystalline Powder
Verwenden
a1-Adrenergic antagonist; derivative of Uracil. Antihypertensive
Biologische Aktivität
α 1 -adrenoceptor antagonist and 5-HT 1A receptor agonist (pIC 50 values are 6.13 and 6.4 respectively). Clinically used hypotensive agent.
Nebenwirkungen
Side effects that may occur during treatment with uradil antihypertension include dizziness, fatigue, nausea, and light-headedness effects. The increases in systolic blood pressure heart rate caused by three progressive work loads bicycle exercise were not affected during urapidil, A slight reduction in forced expiratory volume was observed in some patients during treatment with beta-blocker. There was no case orthostatic hypotension during urapidil administration, despite its alpha1-blocking action. Side-effects were rare negligible
[1].
Urapidil hydrochloride Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
