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Urapidil

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Urapidil
File:Urapidil.svg
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
  • (Prescription only)
Oral
Identifiers
34661-75-1
64887-14-5 (HCl)
C02CA06
PubChem CID 5639
ChemSpider 5437
UNII A78GF17HJS 7pxY
ChEMBL CHEMBL279229
Chemical data
Formula C20H29N5O3
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. doi:10.1111/j.1476-5381.1991.tb12290.x. 
  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. PMID 228944. doi:10.1016/0014-2999(79)90018-9. 
  3. Verberne AJM, Rand MJ (1984). "Pharmacological activities of the antihypertensive drug urapidil in the rat". Clin. Exp. Pharmacol. Physiol. 11 (4): 407–412. PMID 6097380. doi:10.1111/j.1440-1681.1984.tb00289.x. 
  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. PMID 2984023. doi:10.1016/0014-2999(85)90725-3. 
  6. Ramage AG (1990). "Influence of 5-HT1A receptor agonists on sympathetic and parasympathetic nerve activity". J. Cardiovasc. Pharmacol. 15: S75–S85. PMID 1702490.