Azasetron

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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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". drugcentral.org/. UNM School of Medicine. 2016-07-31. Retrieved 2016-11-11.
↑ "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.

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[1] "Azasetron". drugcentral.org/. UNM School of Medicine. 2016-07-31. Retrieved 2016-11-11.

[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.

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^Y
UNII	77HC7URR9Z
KEGG	D07481^Y
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)^Y Key:WUKZPHOXUVCQOR-UHFFFAOYSA-N^Y
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