関: azasetron hydrochloride

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2017/07/19 15:13:19」(JST)

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Azasetron is an antiemetic which acts as a 5-HT₃ receptor antagonist , pK_i = 9.27 ^[1] It is used in the management of nausea and vomiting induced by cancer chemotherapy (such as cisplatin chemotherapy). Azasetron hydrochloride is given in a usual dose of 10 mg once daily by mouth or intravenously. It is approved for marketing in Japan, and marketed exclusively by Torii Pharmaceutical Co., Ltd. under the trade names "Serotone® I.V. Injection 10 mg" and "Serotone® Tablets 10 mg".^[2] Pharmacokinetics data from S. Tsukagoshi.^[3]

References

^ "Azasetron". http://drugcentral.org/. UNM School of Medicine. 2016-07-31. Retrieved 2016-11-11. External link in |website= (help)
^ "Torii Pharmaceutical to Solely Market Antiemetic Drugs". Torii Pharmaceutical Co Ltd. 2009-01-13. Retrieved 2016-11-11.
^ Tsukagoshi, S. (1999-06-01). "[Pharmacokinetics of azasetron (Serotone), a selective 5-HT3 receptor antagonist]". Gan to Kagaku Ryoho. Cancer & Chemotherapy. 26 (7): 1001–1008. ISSN 0385-0684. PMID 10396331.

This drug article relating to the gastrointestinal system is a stub. You can help Wikipedia by expanding it.

English Journal

Theoretical evaluation of antiemetic effects of 5-HT3 receptor antagonists for prevention of vomiting induced by cisplatin.

Nakamura H1, Yokoyama H, Takayanagi R, Yoshimoto K, Nakajima A, Okuyama K, Iwase O, Yamada Y.
European journal of drug metabolism and pharmacokinetics.Eur J Drug Metab Pharmacokinet.2014 Jan 28. [Epub ahead of print]
5-HT3 receptor antagonists are widely used as antiemetic agents in clinical setting, of which palonosetron, with a long elimination half life (t 1/2), has recently become available. It is important to evaluate the concentration of serotonin when investigating the antiemetic effects of 5-HT3 receptor
PMID 24470169

A Randomized Double-Blind, Double-Dummy, Multicenter Trial of Azasetron versus Ondansetron to Evaluate Efficacy and Safety in the Prevention of Delayed Nausea and Vomiting Induced by Chemotherapy.

Lee HY1, Kim HK1, Lee KH2, Kim BS3, Song HS4, Yang SH5, Kim JH6, Kim YH7, Kim JG8, Kim SW9, Kim DW10, Kim SY11, Park HS12.
Cancer research and treatment : official journal of Korean Cancer Association.Cancer Res Treat.2014 Jan;46(1):19-26. doi: 10.4143/crt.2014.46.1.19. Epub 2014 Jan 15.
PURPOSE: This study was conducted to evaluate the efficacy and safety of azasetron compared to ondansetron in the prevention of delayed chemotherapy-induced nausea and vomiting.MATERIALS AND METHODS: This study was a multi-center, prospective, randomized, double-dummy, double-blind and parallel-grou
PMID 24520219

Synergistic effect of 5-HT1A and σ1 receptor activation on prefrontal dopaminergic transmission under circulating steroid deficiency.

Hiramatsu N1, Ago Y1, Hasebe S1, Nishimura A1, Mori K1, Takuma K1, Matsuda T2.
Neuropharmacology.Neuropharmacology.2013 Dec;75:53-61. doi: 10.1016/j.neuropharm.2013.06.026. Epub 2013 Jul 9.
Serotonin (5-HT)1A and σ1 receptors have been implicated in psychiatric disorders. We previously found that combined 5-HT reuptake inhibition and σ1 receptor activation has a synergistic effect on prefrontal dopaminergic transmission in adrenalectomized/castrated mice lacking circulating steroid h
PMID 23851260

Japanese Journal

がん化学療法施行中患者における5-hydroxytryptamine Receptor type 3(5-HT_3受容体)拮抗薬の摂食状況に基づく臨床評価

奥山清,吉元公一,岩瀬理,大関健志,山田安彦
藥學雜誌 128(4), 649-655, 2008-04-01
… At eating points in which combination therapy with steroids and central antiemetic agents was not given, antiemetic effects of granisetron, azasetron and ramosetron were compared and revealed that azaseton was the most effective antiemetic agent. …
NAID 110006656203

Laxative Effect of Agarwood Leaves and Its Mechanism

HARA Hideaki,ISE Yasuaki,MORIMOTO Nobutaka,SHIMAZAWA Masamitsu,ICHIHASHI Koji,OHYAMA Masayoshi,IINUMA Munekazu
Bioscience, biotechnology, and biochemistry 72(2), 335-345, 2008-02-23
… This ileal contraction induced by compound 4 was inhibited by atropine, but not by azasetron, suggesting that the effect of compound 4 was mediated by acetylcholine receptors, and not by serotonin. …
NAID 10027523933

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★リンクテーブル★

リンク元	「アザセトロン」
拡張検索	「azasetron hydrochloride」

「アザセトロン」

Azasetron
Clinical data
AHFS/Drugs.com	International Drug Names
Routes of; administration	Oral
ATC code	none;
Pharmacokinetic data
Bioavailability	90%
Excretion	60-70%
Identifiers
	IUPAC name N-(1-azabicyclo[2.2.2]octan-8-yl)-6-chloro-4-methyl-3-oxo-1,4-benzoxazine-8-carboxamide;
CAS Number	123039-99-6;
PubChem CID	2264;
IUPHAR/BPS	2285;
ChemSpider	2177 ;
UNII	77HC7URR9Z;
KEGG	D07481 ;
ChEMBL	CHEMBL1598608;
Chemical and physical data
Formula	C17H20ClN3O3
Molar mass	349.81 g/mol
3D model (JSmol)	Interactive image;
	SMILES CN1C(=O)COC2=C1C=C(C=C2C(=O)NC3CN4CCC3CC4)Cl ;
	InChI InChI=1S/C17H20ClN3O3/c1-20-14-7-11(18)6-12(16(14)24-9-15(20)22)17(23)19-13-8-21-4-2-10(13)3-5-21/h6-7,10,13H,2-5,8-9H2,1H3,(H,19,23) ; Key:WUKZPHOXUVCQOR-UHFFFAOYSA-N ;
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英: azasetron、
化: 塩酸アザセトロン、azasetron hydrochloride、アザセトロン塩酸塩
商: セロトーン
関: その他の消化器官用薬

「azasetron hydrochloride」

　　[★]

塩酸アザセトロン

関: azasetron

[1] "Azasetron". http://drugcentral.org/. UNM School of Medicine. 2016-07-31. Retrieved 2016-11-11. External link in |website= (help)

[2] "Torii Pharmaceutical to Solely Market Antiemetic Drugs". Torii Pharmaceutical Co Ltd. 2009-01-13. Retrieved 2016-11-11.

[3] Tsukagoshi, S. (1999-06-01). "[Pharmacokinetics of azasetron (Serotone), a selective 5-HT3 receptor antagonist]". Gan to Kagaku Ryoho. Cancer & Chemotherapy. 26 (7): 1001–1008. ISSN 0385-0684. PMID 10396331.

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azasetron