Urapidil
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Clinical data | |
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AHFS/Drugs.com | International Drug Names |
Routes of administration |
Oral |
ATC code | C02CA06 (WHO) |
Legal status | |
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Identifiers | |
Systematic (IUPAC) name: 6-({3-[4-(2-methoxyphenyl)piperazin-1-yl]propyl}amino)-1,3-dimethylpyrimidine-2,4(1H,3H)-dione
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CAS Number | 34661-75-1 64887-14-5 (HCl) |
PubChem (CID) | 5639 |
ChemSpider | 5437 |
UNII | A78GF17HJS ![]() |
ChEMBL | CHEMBL279229 |
Chemical and physical data | |
Formula | C20H29N5O3 |
Molar mass | 387.48 g/mol |
3D model (Jmol) | Interactive image |
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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[edit]
References[edit]
- ^ Ramage AG (April 1991). "The mechanism of the sympathoinhibitory action of urapidil: role of 5-HT1A receptors". Br. J. Pharmacol. 102 (4): 998–1002. doi:10.1111/j.1476-5381.1991.tb12290.x. PMC 1917978
. PMID 1855130.
- ^ 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. New Drugs Annual: Cardiovascular Drugs. p. 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.
Sympatholytics (antagonize α-adrenergic vasoconstriction) |
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Other antagonists |
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Simple piperazines (no additional rings) |
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Phenylpiperazines |
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Benzylpiperazines | |
Diphenylalkylpiperazines (benzhydrylalkylpiperazines) |
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Pyrimidinylpiperazines | |
Pyridinylpiperazines | |
Benzo(iso)thiazolylpiperazines | |
Tricyclics (piperazine attached via side chain) |
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Others/Uncategorized |
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