In vitro evaluation, biodistribution in rats of radiolabeled raloxifene

被引：18

作者：

Bayrak, Elif ^{[1
]}

Lambrecht, Fatma Yurt ^{[1
]}

Durkan, Kubra ^{[1
]}

Yilmaz, Osman ^{[2
]}

机构：

[1] Ege Univ, Inst Nucl Sci, Dept Nucl Applicat, TR-35100 Izmir, Turkey

[2] Dokuz Eylul Univ, Dept Anim, Res Ctr, Izmir, Turkey

来源：

APPLIED RADIATION AND ISOTOPES | 2010年 / 68卷 / 01期

关键词：

Raloxifene; I-131; Iodogen; Rats; Uterus; I-131-raloxifene; METABOLITES;

D O I：

10.1016/j.apradiso.2009.09.027

中图分类号：

O61 [无机化学];

学科分类号：

070301 ; 081704 ;

摘要：

Raloxifene is a selective estrogen receptor modulator that produces both estrogen agonistic effects on bone and lipid metabolism and estrogen-antagonistic effects on uterine endometrium and breast tissue. In the present study, raloxifene was labeled with I-131 by iodogen method and investigated for its radiopharmaceutical potential. Radiolabeling yield is 91 +/- 0.7%, as determined by radio thin layer chromatography (RTLC). Results of in vitro study indicated I-131-raloxifene has high stability (4 h) in serum. Biodistribution study was carried out with Albino wistar female rats. The result has shown that the radioiodinated raloxifene has higher uptake in uterus than breast and ovarian. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：33 / 36

页数：4

共 9 条

[1] Raloxifene [J].

Balfour, JA ;

Goa, KL .

DRUGS & AGING, 1998, 12 (04) :335-341

[2] Raloxifene pharmacokinetics in males with normal and impaired renal function [J].

Czock, D ;

Keller, F ;

Heringa, M ;

Rasche, FM .

BRITISH JOURNAL OF CLINICAL PHARMACOLOGY, 2005, 59 (04) :479-482

[3] Synthesis and estrogen receptor binding affinities of the major human metabolites of raloxifene (LY139481) [J].

Dodge, JA ;

Lugar, CW ;

Cho, S ;

Osborne, JJ ;

Phillips, DL ;

Glasebrook, AL ;

Frolik, CA .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1997, 7 (08) :993-996

[4] Evaluation of the major metabolites of raloxifene as modulators of tissue selectivity [J].

Dodge, JA ;

Lugar, CW ;

Cho, S ;

Short, LL ;

Sato, M ;

Yang, NN ;

Spangle, LA ;

Martin, MJ ;

Phillips, DL ;

Glasebrook, AL ;

Osborne, JJ ;

Frolik, CA ;

Bryant, HU .

JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY, 1997, 61 (1-2) :97-106

[5] Pharmacokinetics of raloxifene and its clinical application [J].

Hochner-Celnikier, D .

EUROPEAN JOURNAL OF OBSTETRICS & GYNECOLOGY AND REPRODUCTIVE BIOLOGY, 1999, 85 (01) :23-29

[6] Disposition mechanisms of raloxifene in the human intestinal Caco-2 model [J].

Jeong, EJ ;

Lin, HM ;

Hu, M .

JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS, 2004, 310 (01) :376-385

[7] Concentration-dependent effects of a selective estrogen receptor modulator raloxifene on proliferation and apoptosis in human uterine leiomyoma cells cultured in vitro [J].

Liu, Jin ;

Matsuo, Hiroya ;

Xu, Qin ;

Chen, Wei ;

Wang, Jiayin ;

Maruo, Takeshi .

HUMAN REPRODUCTION, 2007, 22 (05) :1253-1259

[8]

SCOTT JA, 1997, J STEROID BIOCHEM, V61, P97

[9] Labeling of apigenin with 131I and bioactivity of 131I-apigenin in male and female rats [J].

Seyitoglu, B. ;

Lambrecht, F. Yurt ;

Durkan, K. .

JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY, 2009, 279 (03) :867-873

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