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Itasetron

Catalog No. T24184 CAS 123258-84-4

Synonyms: DAU6215CL, UNII-00S0D0OEKR, U-98079A, U 98079A, DAU 6215CL

Itasetron (U 98079A) is a 5-hydroxytryptamine 3-receptor antagonist used to prevent age-related memory deficits in rats.Itasetron's antiemetic activity in animal models of cancer chemotherapy and radiation therapy may be useful in the study of amnesia.

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Itasetron, CAS 123258-84-4

Pack Size	Availability	Price/USD
1 mg	In stock	$ 350.00
5 mg	In stock	$ 828.00
10 mg	In stock	$ 1,130.00
25 mg	In stock	$ 1,590.00
50 mg	In stock	$ 1,980.00
100 mg	In stock	$ 2,500.00
500 mg	In stock	$ 4,900.00

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Purity: 100%

ee: 99.86%

Purity: 99.63%

ee: 100%

Biological Description

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Storage & Solubility Information

Description

In vivo

Itasetron orally is rapidly absorbed (about 90 min), is highly bioavailable (greater than 90%), and has a long half-life (about 12 h). Itasetron (0.5, 1, 2, 4, and 8 mg; twice daily) in comparison with 8 mg b.i.d. ondansetron. Assessments were made in patients (n = 104) with histologically confirmed cancer (excluding head and neck tumors) and about to receive their first course of moderately emetogenic chemotherapy. Itasetron demonstrated comparable efficacy to ondansetron; no statistically significant between-group differences were observed in the primary (complete response rate) or secondary (nausea and delayed emesis) efficacy criteria. The tolerability of Itasetron was assessed as 'very good' or 'rather good' by 81% of patients and 89% of physicians. In conclusion, Itasetron is effective and well tolerated in patients receiving moderately emetogenic chemotherapy. Oral doses of 1 mg b.i.d. or above will be used in further clinical studies.[1]

Synonyms	DAU6215CL, UNII-00S0D0OEKR, U-98079A, U 98079A, DAU 6215CL
Molecular Weight	300.36
Formula	C16H20N4O2
CAS No.	123258-84-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 45 mg/mL (149.82 mM)

References and Literature

1. Goldschmidt H, et al. Comparison of oral itasetron with oral ondansetron: results of a double-blind, active-controlled phase II study in chemotherapy-naive patients receiving moderately emetogenic chemotherapy. Anticancer Drugs. 1997 Jun;8(5):436-44. 2. Patoia L, et al. Intravenous itasetron: establishing the effective dose range for the prophylactic control of acute emesis in cancer patients undergoing high-dose cisplatin chemotherapy. Clin Oncol (R Coll Radiol). 1999;11(2):99-104. 3. Volonté M, et al. Effect of the 5-hydroxytryptamine3 receptor antagonist itasetron (DAU 6215) on (+)-N-allylnormetazocine-induced dopamine release in the nucleus accumbens and in the corpus striatum of the rat: an in vivo microdialysis study. J Pharmacol Exp Ther. 1995 Oct;275(1):358-67. 4. Pitsikas N, et al. Itasetron (DAU 6215) prevents age-related memory deficits in the rat in a multiple choice avoidance task. Eur J Pharmacol. 1996 Sep 12;311(2-3):115-9.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library GPCR Compound Library Membrane Protein-targeted Compound Library Drug Repurposing Compound Library Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Bioactive Compounds Library Max Anti-Cancer Compound Library Bioactive Compound Library

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Keywords

Itasetron 123258-84-4 GPCR/G Protein Neuroscience 5-HT Receptor DAU6215CL UNII-00S0D0OEKR U-98079A U 98079A DAU 6215CL inhibitor inhibit

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