123258-84-4|Itasetron|1H-Benzimidazole-1-carboxamide, 2,3-dihydro-N-(8-methyl-8-azabicyclo(3.2.1)oct-3-yl)-2-oxo, endo-|-范德生物科技公司

Itasetron

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names：
1H-Benzimidazole-1-carboxamide, 2,3-dihydro-N-(8-methyl-8-azabicyclo(3.2.1)oct-3-yl)-2-oxo, endo-
CAS号：
123258-84-4
MDL Number：
MF(分子式)： C16H20N4O2 MW(分子量)： 300.36
EINECS: Reaxys Number:
Pubchem ID: Brand:BIOFOUNT

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中文别名	Itasetron
英文别名	Itasetron; DAU 6215CL; DAU6215CL; U 98079A; U-98079A; UNII-00S0D0OEKR;
CAS号	123258-84-4
Inchi	InChI=1S/C16H20N4O2/c1-19-11-6-7-12(19)9-10(8-11)17-15(21)20-14-5-3-2-4-13(14)18-16(20)22/h2-5,10-12H,6-9H2,1H3,(H,17,21)(H,18,22)
InchiKey	RWXRJSRJIITQAK-UHFFFAOYSA-N
分子式 Formula	C16H20N4O2
分子量 Molecular Weight	300.36
溶解度Solubility
性状	Solid powder
储藏条件 Storage conditions	Dry, dark and store at 0-4℃ for short term (days to weeks) or -20℃ for long term (Store correctly 2-3years).

产品说明	Itasetron(CAS:123258-84-4):仅限应用于工业或者科学研究过程中非医疗目的，不应用于人类或动物的临床诊断以及治过程疗，该产品非药用，非食用。
Introduction	Itasetron is a potent 5HT-3 receptor antagonist. Itasetron hydrochloride is a new 5-hydroxytryptamine3 (5-HT3) antagonist with potent antiemetic properties. It is more potent than ondansetron in animal models and in early clinical studies it demonstrates a long half-life and does not undergo hepatic biotransformation before elimination. itasetron hydrochloride is effective in the dose range 35-280 microg/kg in preventing cisplatin-induced emesis.
Application1
Application2
Application3

警示图
危险性	Warning
危险性警示
安全声明
安全防护
备注

[1]Patoia L, Del Favero A, Giglietti A, Malacarne P, Donati D, Indelli M, Bensi G, Palladino MA, Cigarini P, Kempe R, Voigt T. 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. PubMed PMID: 10378635.

[2]Goldschmidt H, Salwender H, Egerer G, Kempe R, Voigt T. 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. PubMed PMID: 9215605.

[3] Volonté M, Ceci A, Borsini F. 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. PubMed PMID: 7562571.

[4] Pitsikas N, Borsini F. 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. PubMed PMID: 8891590.

[5] Itasetron. DAU 6215, U 98079. Drugs R D. 1999 Oct;2(4):243-4. PubMed PMID: 10659399.

6: Pitsikas N, Brambilla A, Borsini F. DAU 6215, a novel 5-HT3 receptor antagonist, improves performance in the aged rat in the Morris water maze task. Neurobiol Aging. 1993 Nov-Dec;14(6):561-4. PubMed PMID: 8295658.7: Schiavi GB, Brunet S, Rizzi CA, Ladinsky H. Identification of serotonin 5-HT4 recognition sites in the porcine caudate nucleus by radioligand binding. Neuropharmacology. 1994 Mar-Apr;33(3-4):543-9. PubMed PMID: 7984293.8: Sagrada A, Turconi M, Bonali P, Schiantarelli P, Micheletti R, Montagna E, Nicola M, Algate DR, Rimoldi EM, Donetti A. Antiemetic activity of the new 5-HT3 antagonist DAU 6215 in animal models of cancer chemotherapy and radiation. Cancer Chemother Pharmacol. 1991;28(6):470-4. PubMed PMID: 1834359.9: Invernizzi R, Pozzi L, Samanin R. Selective reduction of extracellular dopamine in the rat nucleus accumbens following chronic treatment with DAU 6215, a 5-HT3 receptor antagonist. Neuropharmacology. 1995 Feb;34(2):211-5. PubMed PMID: 7617146.10: Rizzi CA, Prudentino A, Giraldo E. Effects on general behaviour and neurotransmitter functions of a new 5-hydroxytryptamine3 receptor antagonist with potential therapeutic relevance in central nervous system disturbances. Arzneimittelforschung. 1993 Oct;43(10):1033-41. PubMed PMID: 7903536.1

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