Urapidil hydrochloride

Bezeichnung:Urapidil hydrochloride

CAS-Nr64887-14-5

Englisch Name:Urapidil hydrochloride

CBNumberCB6332466

SummenformelC20H30ClN5O3

Molgewicht423.94

MOL-Datei64887-14-5.mol

Urapidil hydrochloride physikalisch-chemischer Eigenschaften

Schmelzpunkt	156-1580C
storage temp.	Keep in dark place,Inert atmosphere,Room temperature
Löslichkeit	H₂O: soluble
Aggregatzustand	solid
Farbe	white
Wasserlöslichkeit	Soluble to 50 mM in water
InChI	InChI=1S/C20H29N5O3.ClH/c1-22-18(15-19(26)23(2)20(22)27)21-9-6-10-24-11-13-25(14-12-24)16-7-4-5-8-17(16)28-3;/h4-5,7-8,15,21H,6,9-14H2,1-3H3;1H
InChIKey	KTMLZVUAXJERAT-UHFFFAOYSA-N
SMILES	O(C1C=CC=CC=1N1CCN(CCCNC2=CC(=O)N(C)C(=O)N2C)CC1)C.Cl

Sicherheit

Kennzeichnung gefährlicher	Xn
R-Sätze:	22-36/37/38
S-Sätze:	26-36
WGK Germany	3
RTECS-Nr.	YQ9862000

Gefahreninformationscode (GHS)

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 α₁-adrenergic receptors (α₁-ARs) and a partial agonist of the serotonin (5-HT) receptor subtype 5-HT_1A. It selectively binds to α₁- over α₂-ARs (IC₅₀s = 0.74 and 42 μM, respectively) and to 5-HT_1A over 5-HT_1B and 5-HT₂ receptors (IC₅₀s = 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 (EC₅₀ = 390 nM). It is also a β₁-AR antagonist that inhibits the positive chronotropic response induced by isoproterenol in isolated rat atria (pA₂ = 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
Antihypertensive;Serotonergic receptor agonist
Verwenden
α1-Adrenergic antagonist; derivative of Uracil (U801000). Antihypertensive.
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].
Einzelnachweise
[1] G LEONETTI. Comparison of the antihypertensive effect of urapidil and metoprolol in hypertension.[J]. European Journal of Clinical Pharmacology, 1986, 30 6: 637-640. DOI:10.1007/BF00608208.

Urapidil hydrochloride Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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