Azasetron hydrochloride | CAS#123040-16-4 | antiemetic

Azasetron hydrochloride
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 341074

CAS#: 123040-16-4

Description: Azasetron is an antiemetic.

Chemical Structure

Azasetron hydrochloride

CAS# 123040-16-4

Instruction

Theoretical Analysis

MedKoo Cat#: 341074
Name: Azasetron hydrochloride
CAS#: 123040-16-4
Chemical Formula: C17H21Cl2N3O3
Exact Mass: 385.10
Molecular Weight: 386.273
Elemental Analysis: C, 52.86; H, 5.48; Cl, 18.35; N, 10.88; O, 12.43

Price and Availability

Size	Price	Availability	Quantity
10mg	USD 350
25mg	USD 600
50mg	USD 1050
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Synonym: Azasetron hydrochloride;Y 25130; Y-25130; Y25130.

IUPAC/Chemical Name: 2H-1,4-Benzoxazine-8-carboxamide, 3,4-dihydro-N-1-azabicyclo(2.2.2)oct-3-yl-6-chloro-4-methyl-3-oxo-, monohydrochloride

InChi Key: DBMKBKPJYAHLQP-BTQNPOSSSA-N

InChi Code: InChI=1S/C17H20ClN3O3.ClH/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);1H/t13-;/m1./s1

SMILES Code: c1(cc(C(N[C@@H]2CN3CCC2CC3)=O)c2c(c1)N(C)C(=O)CO2)Cl.Cl

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Instruction:

View handling instruction

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 386.27 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Fang BX, Chen FC, Zhu D, Guo J, Wang LH. Stability of azasetron-dexamethasone mixture for chemotherapy-induced nausea and vomiting administration. Oncotarget. 2017 Oct 31;8(63):106249-106257. doi: 10.18632/oncotarget.22174. eCollection 2017 Dec 5. PubMed PMID: 29290945; PubMed Central PMCID: PMC5739730.

2: Ahmadi-Mahmoodabadi N, Nasehi M, Emam Ghoreishi M, Zarrindast MR. Synergistic effect between prelimbic 5-HT3 and CB1 receptors on memory consolidation deficit in adult male Sprague-Dawley rats: An isobologram analysis. Neuroscience. 2016 Mar 11;317:173-83. doi: 10.1016/j.neuroscience.2015.12.010. Epub 2015 Dec 14. PubMed PMID: 26701293.

3: Hasebe S, Ago Y, Nishiyama S, Oka S, Hashimoto H, Takuma K, Matsuda T. Pharmacological profile of encounter-induced hyperactivity in isolation-reared mice. Behav Pharmacol. 2015 Oct;26(7 Spec No):681-90. doi: 10.1097/FBP.0000000000000140. PubMed PMID: 25932719.

4: Nasehi M, Kafi F, Khakpai F, Zarrindast MR. Involvement of the serotonergic system of the ventral hippocampus (CA3) on amnesia induced by ACPA in mice. Behav Brain Res. 2015 Jun 1;286:356-63. doi: 10.1016/j.bbr.2015.03.011. Epub 2015 Mar 11. PubMed PMID: 25771207.

5: Bell R, Duke AA, Gilmore PE, Page D, Bègue L. Anxiolytic-like effects observed in rats exposed to the elevated zero-maze following treatment with 5-HT2/5-HT3/5-HT4 ligands. Sci Rep. 2014 Jan 24;4:3881. doi: 10.1038/srep03881. PubMed PMID: 24457553; PubMed Central PMCID: PMC5379192.

6: Lin G, Ma J, Zhu J, Yang X, Hu L, Wang X. Determination of azasetron hydrochloride in rabbit plasma by liquid chromatography tandem mass spectrometry and its application. Biomed Chromatogr. 2011 Oct;25(10):1107-11. doi: 10.1002/bmc.1578. Epub 2010 Dec 29. PubMed PMID: 21204117.

7: Ataee R, Ajdary S, Rezayat M, Shokrgozar MA, Shahriari S, Zarrindast MR. Study of 5HT3 and HT4 receptor expression in HT29 cell line and human colon adenocarcinoma tissues. Arch Iran Med. 2010 Mar;13(2):120-5. PubMed PMID: 20187666.

8: Ataee R, Ajdary S, Zarrindast M, Rezayat M, Shokrgozar MA, Ataee A. Y25130 hydrochloride, a selective 5HT3 receptor antagonist has potent antimitogenic and apoptotic effect on HT29 colorectal cancer cell line. Eur J Cancer Prev. 2010 Mar;19(2):138-43. doi: 10.1097/CEJ.0b013e3283354901. PubMed PMID: 20010428.

9: Yamada Y, Fujita M, Okuyama K, Takayanagi R, Ozeki T, Yokoyama H, Iga T. [Analysis of antiemetic effect of various dosage regimens of azasetron hydrochloride based on 5-HT3 receptor occupancy of serotonin]. Yakugaku Zasshi. 2007 Feb;127(2):353-7. Japanese. PubMed PMID: 17268155.

10: Hayakawa T, Sato M, Konaka M, Makino A, Hirohata T, Totsu S, Wada Y, Sato H, Inotsume N, Fujita A, Sekine K. [Comparison of ramosetron and azasetron for prevention of acute and delayed cisplatin-induced emesis in lung cancer patients]. Gan To Kagaku Ryoho. 2006 May;33(5):633-8. Japanese. PubMed PMID: 16685162.

11: Ju Yeon Ban, Yeon Hee Seong. Blockade of 5-HT(3) receptor with MDL 72222 and Y 25130 reduces beta-amyloid protein (25--35)-induced neurotoxicity in cultured rat cortical neurons. Eur J Pharmacol. 2005 Sep 27;520(1-3):12-21. PubMed PMID: 16150439.

12: Lee HJ, Ban JY, Seong YH. Blockade of 5-HT(3) receptor with MDL7222 and Y25130 reduces hydrogen peroxide-induced neurotoxicity in cultured rat cortical cells. Life Sci. 2005 Dec 5;78(3):294-300. Epub 2005 Aug 19. PubMed PMID: 16112139.

13: Grandoso L, Torrecilla M, Pineda J, Ugedo L. alpha(2)-Adrenoceptor involvement in the in vitro inhibitory effect of citalopram on a subpopulation of rat locus coeruleus neurons. Eur J Pharmacol. 2005 Jul 4;517(1-2):51-8. PubMed PMID: 15975573.

14: Dougherty KJ, Bannatyne BA, Jankowska E, Krutki P, Maxwell DJ. Membrane receptors involved in modulation of responses of spinal dorsal horn interneurons evoked by feline group II muscle afferents. J Neurosci. 2005 Jan 19;25(3):584-93. PubMed PMID: 15659594; PubMed Central PMCID: PMC1890036.

15: Shimada S, Yagi Y, Kuramoto M, Aoki N, Ogawa M. Second-line chemotherapy with combined irinotecan and low-dose cisplatin for patients with metastatic gastric carcinoma resistant to 5-fluorouracil. Oncol Rep. 2003 May-Jun;10(3):687-91. PubMed PMID: 12684644.

16: Haga K, Inaba K, Syoji H, Hashimoto T. [Delayed emesis induced by the chemotherapeutic agent doxorubicin hydrochloride in dogs]. Nihon Yakurigaku Zasshi. 2000 Nov;116(5):313-20. Japanese. PubMed PMID: 11215382.

17: Beppu T, Ogawa M, Yamanaka T, Egami H, Ohara C, Masuda Y, Kudo S, Kuramoto M, Doi K, Matsuda T. [Clinical evaluation of Azasetron Hydrochloride: a new selective 5-HT3 receptor antagonist--antiemetic profile and plasma concentration in transcatheter arterial chemoembolization using CDDP for unresectable hepatocellular carcinoma]. Gan To Kagaku Ryoho. 1998 Jul;25(8):1197-202. Japanese. PubMed PMID: 9679583.

18: Moriyama Y, Arimori K, Nakano M. Absorption characteristics of azasetron from rectal and oral routes in rabbits. Biol Pharm Bull. 1997 Jun;20(6):701-3. PubMed PMID: 9212995.

19: Katayama K, Asano K, Haga K, Fukuda T. High affinity binding of azasetron hydrochloride to 5-hydroxytryptamine3 receptors in the small intestine of rats. Jpn J Pharmacol. 1997 Apr;73(4):357-60. PubMed PMID: 9165374.

20: Yakushiji T, Akaike N. Blockade of 5-HT3 receptor-mediated currents in dissociated frog sensory neurones by benzoxazine derivative, Y-25130. Br J Pharmacol. 1992 Nov;107(3):853-7. PubMed PMID: 1472977; PubMed Central PMCID: PMC1907744.

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