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Development of a new Iodine contrast agent excreted into bile and urine based on the transporter selectivity

Research Project

Project/Area Number 26670388
Research Category

Grant-in-Aid for Challenging Exploratory Research

Allocation TypeMulti-year Fund
Research Field Gastroenterology
Research InstitutionSt. Marianna University School of Medicine

Principal Investigator

Matsumoto Nobuyuki  聖マリアンナ医科大学, 医学部, 准教授 (60300951)

Co-Investigator(Kenkyū-buntansha) JUTABHA Promsuk  獨協医科大学, 医学部, 助教 (90541748)
Co-Investigator(Renkei-kenkyūsha) ANZAI Naohiko  千葉大学, 大学院医学研究院, 教授 (70276054)
Project Period (FY) 2014-04-01 – 2016-03-31
Project Status Completed (Fiscal Year 2015)
Budget Amount *help
¥2,600,000 (Direct Cost: ¥2,000,000、Indirect Cost: ¥600,000)
Fiscal Year 2015: ¥1,040,000 (Direct Cost: ¥800,000、Indirect Cost: ¥240,000)
Fiscal Year 2014: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
Keywords造影剤
Outline of Final Research Achievements

We designed two candidates of a new iodine-containing contrast agent by giving a side chain to Iohexol. We named them as I-A, and I-B. They were applied to chemical transport experiment. I-A significantly inhibited the substrate uptake from OATP1B3 and OATP2B1. I-B strongly inhibited the substrate uptake from OATP1B1, 1B3, and 2B1. Iohexol did not inhibit the substrate uptake from any OATP transporters. Animal experiment revealed bile duct excretion of I-A. We confirmed if the density of I-A is less than 125mg/ml, it can be administered to mice without any obvious side effects. However we could not identify the bile duct excretion of I-B. Because of the heigh viscosity of I-B dissolved into water, mice could not survive after the administration of I-B. We successfully gave an existing Iodine contrast agent a new function to accumulate in cells through hepatocyte specific transporters. And one of them was excreted into bile.

Report

(3 results)
  • 2015 Annual Research Report   Final Research Report ( PDF )
  • 2014 Research-status Report

URL: 

Published: 2014-04-04   Modified: 2017-05-10  

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