Urapidil

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Urapidil
Systematic (IUPAC) name
6-({3-[4-(2-methoxyphenyl)piperazin-1-yl]propyl}amino)-1,3-dimethylpyrimidine-2,4(1H,3H)-dione
Clinical data
AHFS/Drugs.com International Drug Names
Legal status ℞ Prescription only
Routes Oral
Identifiers
CAS number 34661-75-1
64887-14-5 (HCl)
ATC code C02CA06
PubChem CID 5639
ChemSpider 5437
UNII A78GF17HJS YesY
ChEMBL CHEMBL279229
Chemical data
Formula C20H29N5O3 
Mol. mass 387.48 g/mol

Urapidil is a sympatholytic antihypertensive drug. It acts as an α1-adrenoceptor antagonist and as an 5-HT1A receptor agonist[1] Although an initial report suggested that urapidil was also an α2-adrenoceptor agonist,[2] this was not substantiated in later studies that demonstrated it was devoid of agonist actions in the dog saphenous vein and the guinea-pig ileum.[3] Unlike some other α1-adrenoceptor antagonists, urapidil does not elicit reflex tachycardia, and this may be related to its weak β1-adrenoceptor antagonist activity,[4][5] as well as its effect on cardiac vagal drive.[6] Urapidil is currently not approved by the U.S. Food and Drug Administration, but it is available in Europe.

See also

References

  1. ↑ Ramage AG (April 1991). "The mechanism of the sympathoinhibitory action of urapidil: role of 5-HT1A receptors". Br. J. Pharmacol. 102 (4): 998–1002. PMC 1917978. PMID 1855130. 
  2. ↑ Eltze M (1979). "Investigations on the mode of action of a new antihypertensive drug, urapidil, in the isolated vas deferens". Eur. J. Pharmacol. 59 (1–2): 1–9. doi:10.1016/0014-2999(79)90018-9. PMID 228944. 
  3. ↑ Verberne AJM, Rand MJ (1984). "Pharmacological activities of the antihypertensive drug urapidil in the rat". Clin. Exp. Pharmacol. Physiol. 11 (4): 407–412. doi:10.1111/j.1440-1681.1984.tb00289.x. PMID 6097380. 
  4. ↑ Schoetensack W, Bruckschen EG, Zech K (1983). "Urapidil". New Drugs Annual: Cardiovascular Drugs. p. 19. 
  5. ↑ Verberne AJM, Rand MJ (1985). "Effect of urapidil on β-adrenoceptors of rat atria". Eur. J. Pharmacol. 108 (2): 193–196. doi:10.1016/0014-2999(85)90725-3. PMID 2984023. 
  6. ↑ Ramage AG (1990). "Influence of 5-HT1A receptor agonists on sympathetic and parasympathetic nerve activity". J. Cardiovasc. Pharmacol. 15: S75–S85. PMID 1702490. 
Sympatholytic (and closely related) antihypertensives (C02)
Sympatholytics
(antagonize α-adrenergic
vasoconstriction)
Central
α2 agonist
Adrenergic release inhibitors
Peripheral
Indirect
Tyrosine hydroxylase inhibitor
Direct
Non-selective α blocker
Other antagonists

M: VAS

anat (a:h/u/t/a/l,v:h/u/t/a/l)/phys/devp/cell/prot

noco/syva/cong/lyvd/tumr, sysi/epon, injr

proc, drug (C2s+n/3/4/5/7/8/9)

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