Urapidil

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
Pregnancy cat.	?
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
ChEMBL	CHEMBL279229
Chemical data
Formula	C20H29N5O3
Mol. mass	387.48 g/mol
	SMILES O=C1\C=C(/N(C(=O)N1C)C)NCCCN3CCN(c2ccccc2OC)CC3;

Urapidil is a sympatholytic antihypertensive drug. It acts as an α₁-adrenoceptor antagonist and as an 5-HT_1A 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.

[edit] See also

^ 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. //www.ncbi.nlm.nih.gov/pmc/articles/PMC1917978/.
^ 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.
^ 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.
^ Schoetensack W, Bruckschen EG, Zech K (1983). Urapidil. pp. 19.
^ 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.
^ Ramage AG (1990). "Influence of 5-HT1A receptor agonists on sympathetic and parasympathetic nerve activity". J. Cardiovasc. Pharmacol. 15: S75–S85. PMID 1702490.