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Technetium-99m labeled imaging agents

An imaging agent, imaging technology, applied in the patent application WO 88/07382 describes a radiodiagnostic reagent using Tc-, which can solve the problems of unsuitable scintigraphic imaging quality requirements and the like

Inactive Publication Date: 2002-07-24
DIATECH PTY LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Alternatively, other radionuclides have significantly lower (eg iodine-125) or significantly higher (eg iodine-131) radiant energy than Tc-99m and thus are not suitable for the quality requirements of scintigraphic imaging
In addition, there are many unsuitable radionuclides that cannot be produced with on-site generators

Method used

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Examples

Experimental program
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Effect test

Embodiment 1

[0141] Solid Phase Peptide Synthesis

[0142] Using an Applied Biosynthesis Model 431A Peptide Synthesizer and using 9-fluorenylmethoxycarbonyl (Fmoc) terminal amino protection, with dicyclohexylcarbodiimide / hydroxybenzotriazole 2-(1H-benzo- Triazol-1-yl)-1,1,3,3-tetramethylurea hexafluorophosphate / hydroxybenzotriazole (HBTU / HOBT) coupling and using p-hydroxymethylphenoxy-methyl poly Styrene (HMP) or Sasrin for carboxy terminated acids Tm The resin, or Rink amide resin for carboxyl terminated amides, was performed on a 0.25 millimolar (mmole) scale for solid phase peptide synthesis (SPPS).

[0143] Homocysteine ​​is prepared by alkaline hydrolysis of L-homocysteine ​​lactone. Fmoc Hcy (S-trityl) and Fmoc Pen (S-trityl) were obtained by tritylation with trityl alcohol in trifluoroacetic acid, followed by a method as described by Atherton et al. ., (1989, Solid Phase Peptide Synthesis, IRL Press: Oxford) described in Fmoc derivatization prepared. Using...

Embodiment 2

[0151] A common method for radioactive labeling with Tc-99m

[0152] Dissolve 0.1 mg of the peptide reagent prepared in Example 1 in 0.1 ml of water, or 50:50 aqueous ethanol, or phosphate-buffered saline (PBS), or 50 mM potassium phosphate buffer (pH=5, 6 or 7.4). Tc-99m glucoheptonate was prepared as follows: Take a Glucoscan vial (E.I. DuPont deNemours, Inc) filled with 1.0ml of Tc-99m sodium pertechnetate up to 200mCi, and let it cool at room temperature. Leave on for 15 minutes. Then 25ml of Tc-99m glucoheptonate was added to the reagent, the reaction was allowed to proceed at room temperature or 100°C for 15-30 minutes, and then filtered through a 0.2 μm filter.

[0153] The purity of the Tc-99m-labeled peptide reagent was determined by HPLC. The conditions used in HPLC were: a WatersDelta-Pak RP-18 analytical column with a size of 5 μm × 4.6 mm × 220 mm was filled with each radiolabeled peptide, and then 1 mL / min Solvent flow rate elution, gradient elution tak...

Embodiment 3

[0169] inhibition of platelet aggregation test

[0170] Platelet aggregation was fundamentally studied as described by Zucker (1989, Methods in Enzymol, 169: 117-133). Briefly, platelet aggregation assays were performed with platelet-rich human plasma (300,000 platelets per milliliter) in the presence or absence of recognized platelet aggregation-inhibiting compounds. A final concentration of 10-15 millimolar adenosine diphosphate solution was added to induce platelet aggregation, and the degree of platelet aggregation was monitored with a Bio / Data aggregometer (Bio / Data Corp., Horsham, PA). The concentration of the platelet aggregation inhibitory compound used varied from 0.1 to 500 μg / mL. From the graph of inhibitor concentration - degree of platelet aggregation, determine the concentration of the inhibitor that reduces the degree of platelet aggregation by 50% (called IC 50 ). The inhibition curve of one peptide RGDS was determined as a positive control...

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Abstract

This invention relates to radiolabeled scintigraphic imaging agents and reagents for preparing such imaging agents and methods for producing and using such reagents. Specifically, the invention relates to reagents for preparing scintigraphic imaging agents for imaging sites in a mammalian body comprising a specific binding compound including specific-binding peptide embodiments thereof, covalently linked to a radiolabel complexing moiety. Reagents, methods and kits for making such reagents, and methods for using such reagents labeled with technetium-99m (Tc-99m) via Tc-99m complexing moieties comprising said reagents, are provided.

Description

Background of the Invention [0001] technical field of invention [0002] The present invention relates to radiodiagnostic agents and methods for producing labeled radiodiagnostic agents. In particular, it relates to scintigraphic imaging agents for imaging sites in mammals, the scintigraphic imaging agents containing a specific binding compound labeled with technetium-99m (Tc-99m) by means of a binding complex with Tc-99m The radiolabeled part is done. The present invention provides radiolabeled scintillation imaging agents, reagents for preparing the above-mentioned radiolabeled scintigraphic imaging agents, methods of labeling the above-mentioned reagents, and kits containing the non-radioactive specific reagents and other components of the present invention, and the kits are used for the preparation of The scintigraphic imaging agent of the present invention. [0003] Description of the prior art [0004] Doctors can use non-invasive means to determine the location of t...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K51/00A61K51/08C07K5/08C07K5/10C07K7/08
CPCA61K51/088A61K2123/00A61K51/083
Inventor 里查德·T·迪安约翰·利斯特-詹姆斯威廉·麦克布赖德
Owner DIATECH PTY LTD
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