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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/07/08 20:08:49」(JST)

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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.

References

^ 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.

UpToDate Contents

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1. 本態性高血圧における治療選択：推奨 choice of therapy in essential hypertension recommendations
2. 前立腺肥大症の内科的治療 medical treatment of benign prostatic hyperplasia
3. 降圧剤と脂質 antihypertensive drugs and lipids
4. 男性における下部尿路症状 lower urinary tract symptoms in men
5. 夜間頻尿：臨床症状、診断、および治療治療 nocturia clinical presentation diagnosis and treatment

English Journal

Effects of α(1)-adrenoceptor antagonists on phenylephrine-induced salivary secretion and intraurethral pressure elevation in anesthetized rats.

Yanai-Inamura H, Ohtake A, Noguchi Y, Hatanaka T, Suzuki M, Ueshima K, Sato S, Sasamata M.Abstractα(1)-Adrenoceptor antagonists are widely used for the treatment of voiding dysfunction associated with benign prostatic hyperplasia. Activation of α(1)-adrenoceptors is reported to induce salivary secretion in rats and humans. However, the effects of α(1)-adrenoceptor antagonists on salivary secretion remain unknown. Here, we investigated the effects of the α(1)-adrenoceptor antagonists prazosin, silodosin, tamsulosin and urapidil on phenylephrine-induced salivary secretion and compared the results with the effects on phenylephrine-induced intraurethral pressure (IUP) elevation in anesthetized rats. All antagonists inhibited phenylephrine-induced salivary secretion and IUP elevation in a dose-dependent fashion. Comparison of DR(10) values (the dose required to shift the dose-response curve 10-fold to the right) in both tissues showed that the inhibitory effect of silodosin was significantly more potent in the salivary gland than in the urethra (18-fold), but tamsulosin (2.3-fold), prazosin (1.7-fold) and urapidil (1.1-fold) did not show comparable tissue selectivity. These results suggest that α(1)-adrenoceptor antagonists inhibit not only urethral contraction but also salivary secretion, and that high tissue selectivity for the salivary gland over the urethra as shown by silodosin may contribute to the incidence of dry mouth.
European journal of pharmacology.Eur J Pharmacol.2012 Feb 1. [Epub ahead of print]
α(1)-Adrenoceptor antagonists are widely used for the treatment of voiding dysfunction associated with benign prostatic hyperplasia. Activation of α(1)-adrenoceptors is reported to induce salivary secretion in rats and humans. However, the effects of α(1)-adrenoceptor antagonists on salivary secr
PMID 22314219

Tamsulosin potently and selectively antagonizes human recombinant α(1A/1D)-Adrenoceptors: slow dissociation from the α(1A)-adrenoceptor may account for selectivity for α(1A)-adrenoceptor over α(1B)-adrenoceptor subtype.

Sato S, Hatanaka T, Yuyama H, Ukai M, Noguchi Y, Ohtake A, Taguchi K, Sasamata M, Miyata K.SourceApplied Pharmacology Research Laboratories, Drug Discovery Research, Astellas Pharma Inc, Miyukigaoka, Tsukuba, Ibaraki 305–8585, Japan. shuichi.sato@jp.astellas.com
Biological & pharmaceutical bulletin.Biol Pharm Bull.2012;35(1):72-7.
We determined the binding affinity of tamsulosin, a selective α(1)-adrenoceptor antagonist, for human α(1)-adrenoceptor subtypes in comparison with those of other α(1)-adrenoceptor antagonists including silodosin, prazosin, 5-methylurapidil, terazosin, alfuzosin, nafopidil, urapidil and BMY7378.
PMID 22223340

Japanese Journal

女性排尿障害患者に対するウラピジル単独およびコリン作動薬との併用療法の有用性

柳澤良三
西日本泌尿器科 73(5), 240-247, 2011-05-20
NAID 10029070127

過活動膀胱患者におけるα1受容体遮断薬の併用は生活の質を向上しうるか? : 抗コリン剤(塩酸プロビベリン)単独群および抗コリン剤α1受容体遮断薬(ウラピジル)併用群間の多施設前向きランダム化試験

松山豪泰,清水芳幸,上領頼啓,城甲啓治,島袋智之,須賀昭信,竹本雅彦,井本勝彦,原好弘,山本憲男,金田芳孝,原田規章,内藤克輔
日本泌尿器科學會雜誌 98(4), 604-613, 2007-05-20
(目的)過活動膀胱(以下OAB)による排尿障害は患者の生活の質を低下させる.本研究の目的はOAB患者の治療に抗コリン剤とα1受容体遮断薬を併用した際の有用性を明らかにすることである.(対象,方法)合計100名(男性:43,女性:57,平均年齢71.3歳)の頻尿(一日8回以上)および尿意切迫(週3回以上)を主訴とする患者を2群(塩酸プロビベリン単独群[52例]および塩酸プロビベリン,ウラピジル併用群 …
NAID 110006273454

Related Pictures

★リンクテーブル★

リンク元	「ウラピジル」
拡張検索	「5-methylurapidil」

「ウラピジル」

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 of; administration	Oral
Identifiers
CAS Registry Number	34661-75-1; 64887-14-5 (HCl)
ATC code	C02CA06
PubChem	CID: 5639
ChemSpider	5437
UNII	A78GF17HJS
ChEMBL	CHEMBL279229
Chemical data
Formula	C20H29N5O3
Molecular mass	387.48 g/mol
	SMILES O=C1\C=C(/N(C(=O)N1C)C)NCCCN3CCN(c2ccccc2OC)CC3 ;