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
SMILES	O=C(N1C2=CC=CC=C2NC1=O)NC3CC(N4C)CCC4C3
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
闪点 FP
熔点 Melting point
沸点 Boiling point
Polarizability极化度
密度 Density
蒸汽压 Vapor Pressure
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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