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HomeProduct name listUrapidil hydrochloride

Urapidil hydrochloride

Synonym(s):6-[[3-[4-(o-Methoxyphenyl)-1-piperazinyl]propyl]amino]-1,3-dimethyluracil hydrochloride

  • CAS NO.:64887-14-5
  • Empirical Formula: C20H30ClN5O3
  • Molecular Weight: 423.94
  • MDL number: MFCD00078601
  • EINECS: 636-348-0
  • SAFETY DATA SHEET (SDS)
  • Update Date: 2024-11-04 20:04:50
Urapidil hydrochloride Structural

What is Urapidil hydrochloride?

Description

Urapidil is an antagonist of α1-adrenergic receptors (α1-ARs) and a partial agonist of the serotonin (5-HT) receptor subtype 5-HT1A. It selectively binds to α1- over α2-ARs (IC50s = 0.74 and 42 μM, respectively) and to 5-HT1A over 5-HT1B 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-HT1A 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-HT1A receptor antagonist spiroxatrine.

Chemical properties

White to Off-White Crystalline Powder

The Uses of Urapidil hydrochloride

α1-Adrenergic antagonist; derivative of Uracil (U801000). Antihypertensive.

The Uses of Urapidil hydrochloride

Antihypertensive;Serotonergic receptor agonist

The Uses of Urapidil hydrochloride

a1-Adrenergic antagonist; derivative of Uracil. Antihypertensive

What are the applications of Application

Urapidil HCl is an adrenergic α1-AR antagonist and a serotonin 5-HT1A (SR-1A) receptor agonist

Biological Activity

α 1 -adrenoceptor antagonist and 5-HT 1A receptor agonist (pIC 50 values are 6.13 and 6.4 respectively). Clinically used hypotensive agent.

Side Effects

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].

References

[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.

Properties of Urapidil hydrochloride

Melting point: 156-1580C
storage temp.  Keep in dark place,Inert atmosphere,Room temperature
solubility  H2O: soluble
form  solid
color  white
Water Solubility  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

Safety information for Urapidil hydrochloride

Signal word Warning
Pictogram(s)
ghs
Exclamation Mark
Irritant
GHS07
GHS Hazard Statements H302:Acute toxicity,oral
Precautionary Statement Codes P264:Wash hands thoroughly after handling.
P264:Wash skin thouroughly after handling.
P270:Do not eat, drink or smoke when using this product.
P301+P312:IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
P501:Dispose of contents/container to..…

Computed Descriptors for Urapidil hydrochloride

InChIKey KTMLZVUAXJERAT-UHFFFAOYSA-N
SMILES O(C1C=CC=CC=1N1CCN(CCCNC2=CC(=O)N(C)C(=O)N2C)CC1)C.Cl

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