Urapidil

Urapidil
(IUPAC) ime
	6-({3-[4-(2-methoxyphenyl)piperazin-1-yl]propyl}amino)-1,3-dimethylpyrimidine-2,4(1H,3H)-dione
Klinički podaci
Identifikatori
CAS broj	34661-75-1 ; 64887-14-5 (HCl)
ATC kod	C02CA06
PubChem	5639
ChemSpider	5437
UNII	A78GF17HJS
Hemijski podaci
Formula	C20H29N5O3
Mol. masa	387.48 g/mol
SMILES	eMolekuli & PubHem
InChI
	InChI=1S/C20H29N5O3/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 ; Key: ICMGLRUYEQNHPF-UHFFFAOYSA-N
Farmakoinformacioni podaci
Trudnoća	?
Pravni status	℞ Prescription only
Način primene	Oralno

Urapidil je simpatolitički antihipertenzivni lek. On deluje kao antagonist α₁-adrenergičkog receptora i agonist 5-HT_1A receptora^[4] Mada je jedan inicijalni izveštaj izneo da je urapidil takođe agonist α₂-adrenergičkog receptora,^[5] to nije potvrđeno u kasnijim studijama.^[6] Za razliku od drugih antagonista α₁-adrenergičkog receptora, urapidil ne izaziva refleks tahikardije, što može da bude posledica njegove slabe antagonističke aktivnosti na β₁-adrenoceptoru,^[7]^[8] kao i usled njegovog uticaja na srčani vagalni disk.^[9] Urapidil trenutno nije odobren od strane FDA, ali je dostupan u Evropi.

Reference

↑ Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519. edit
↑ Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1.
↑ Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). „Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining”. J Cheminform 2 (1): 3. DOI:10.1186/1758-2946-2-3. PMID 20331846. 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. 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: 407–412. DOI:10.1111/j.1440-1681.1984.tb00289.x. PMID 6097380.
↑ Schoetensack W, Bruckschen EG, Zech K (1983). Urapidil. str. 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.

Literatura

Schoetensack W, Bruckschen EG, Zech K (1983). Urapidil. str. 19.

[1] Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519. edit

[2] Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1.

[3] Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). „Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining”. J Cheminform 2 (1): 3. DOI:10.1186/1758-2946-2-3. PMID 20331846. edit

[pmid1855130-4] 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.

[pmid228944-5] 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.

[pmid6097380-6] Verberne AJM, Rand MJ (1984). „Pharmacological activities of the antihypertensive drug urapidil in the rat”. Clin. Exp. Pharmacol. Physiol. 11: 407–412. DOI:10.1111/j.1440-1681.1984.tb00289.x. PMID 6097380.

[7] Schoetensack W, Bruckschen EG, Zech K (1983). Urapidil. str. 19.

[pmid2984023-8] 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.

[pmid1702490-9] Ramage AG (1990). „Influence of 5-HT1A receptor agonists on sympathetic and parasympathetic nerve activity”. J. Cardiovasc. Pharmacol. 15: S75–S85. PMID 1702490.

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