A procedure is described for the synthesis of p-[(bisacarboxymethyl)aminomethyl carbamino] hippuric acid (PAHIDA). The compound was identified by i.r. and NMR spectroscopy. A lyophilized complex was prepared and labeled with 99mTc. The purity of the preparation is better than 98%. The stability of the 99mTc-PAHIDA complex is achieved 8 h after labeling. Biodistribution tested on white rats shows a maximum accumulation in kidneys of 6-10% within 2 min after injection, while the accumulation in the liver is 2-4% of the administrated dose. Preliminary clinical studies of 99mTc-PAHIDA on patients and its comparison with 131I-hippuran showed that the 99Tc-PAHIDA preparation has excellent characteristics for visualization of kidneys. However, it has slightly slower urinary elimination compared to hippuran, which it makes possible to use PAHIDA as a replacement of hippuran to a certain extent.
Download full-text PDF |
Source |
---|---|
http://dx.doi.org/10.1016/0883-2889(89)90152-4 | DOI Listing |
Chem Biol Interact
August 2024
Key Laboratory of Radiopharmacokinetics for Innovative Drugs, Chinese Academy of Medical Sciences, and Institute of Radiation Medicine, Chinese Academy of Medical Sciences and Peking Union Medical College, No. 238, Baidi Road, Tianjin, 300192, China. Electronic address:
Pharmacokinetic changes induced by radiation following radiotherapy ("RT-PK" phenomenon) are of great significance to the effectiveness and safety of chemotherapeutic agents in clinical settings. The aims of this study were to clarify the organic anion transporters (Oats) involved in the "RT-PK" phenomenon of bestatin in rats following X-ray irradiation and to elucidate its potential mechanism via vitamin D signalling. Pharmacokinetic studies, uptake assays using rat kidney slices and primary proximal tubule cells, and molecular biological studies were performed.
View Article and Find Full Text PDFJ Nucl Med
June 2024
Department of Nuclear Medicine, West German Cancer Center, University Hospital Essen, University of Duisburg-Essen, Essen, Germany.
-aminohippurate, also known as -aminohippuric acid (PAH), is used clinically to measure effective renal plasma flow. Preclinically, it was shown to reduce Lu-DOTATOC uptake in the kidneys while improving bioavailability compared with amino acid (AA) coinfusion. We report the safety and efficacy of PAH coinfusion during peptide receptor radiotherapy in patients with neuroendocrine tumors.
View Article and Find Full Text PDFInt J Mol Sci
October 2023
Department of Pharmacology, Faculty of Medicine and University Hospital Cologne, University of Cologne, Gleueler Straße 24, 50931 Cologne, Germany.
Chronic kidney disease (CKD) is a global health concern affecting millions worldwide. One of the critical challenges in CKD is the accumulation of uremic toxins such as p-cresol sulfate (pCS) and indoxyl sulfate (IS), which contribute to systemic damage and CKD progression. Understanding the transport mechanisms of these prominent toxins is essential for developing effective treatments.
View Article and Find Full Text PDFXenobiotica
February 2023
Drug Metabolism & Pharmacokinetics Research Laboratories, Daiichi Sankyo Co., Ltd, Tokyo, Japan.
Cimetidine at a clinical dosage decreased the renal clearance (CLr) of mirogabalin in humans by inhibition of renal secretion. Mirogabalin is a substrate of human OAT1/3, OCT2, MATE1 and/or MATE2-K. To clarify the mechanism behind the above interaction, it was investigated whether cimetidine inhibits the process of mirogabalin uptake at the basolateral side or the process of its efflux at the apical side in rat kidney .
View Article and Find Full Text PDFPharmaceutics
October 2022
Department of Pharmacy, The First Hospital of Lanzhou University, Lanzhou 730013, China.
Background: Organic anion transporter 1 (OAT1) and OAT3 have an overlapping spectrum of substrates such that one can exert a compensatory effect when the other is dysfunctional. As a result, the knockout of either OAT1 or OAT3 is not reflected in a change in the excretion of organic anionic substrates. To date, only the mOAT1 and mOAT3 individual knockout mouse models have been available.
View Article and Find Full Text PDFEnter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!