77679-27-7

Usage

InChI:InChI=1/C8H10IN3/c9-7-3-1-2-6(4-7)5-12-8(10)11/h1-4H,5H2,(H4,10,11,12)/i9+4

Upstream product

• 420-04-2 CYANAMID 
• 222729-15-9 1-(-3-bromobenzyl)-2,2,5,5-tetramethyl-1,2,5-azadisilolidine 
• 80663-95-2 (3-iodobenzyl)guanidine 
• 80663-96-3 m-Iodobenzylguanidine hemisulfate 
• 87862-25-7 meta-Iodobenzylguanidinium sulfate 

Relevant academic research and scientific papers

Polymer-supported radiopharmaceuticals: [131I]MIBG and [123I]MIBG

A new method has been developed that produces no-carrier-added [131I]MIBG in ≥ 90% radiochemical yield and high chemical purity. Isolation and purification are simple involving just filtration and absorption and desorption onto a C18 Sep-Pak(TM) cartridge. No-carrier-added material should avoid the potential pharmacological side effects accompanying the current method of production.

Rational evaluation of the therapeutic effect and dosimetry of auger electrons for radionuclide therapy in a cell culture model

Objective: Radionuclide therapy with low-energy auger electron emitters may provide high antitumor efficacy while keeping the toxicity to normal organs low. Here we evaluated the usefulness of an auger electron emitter and compared it with that of a beta emitter for tumor treatment in in vitro models and conducted a dosimetry simulation using radioiodine-labeled metaiodobenzylguanidine (MIBG) as a model compound. Methods: We evaluated the cellular uptake of 125I-MIBG and the therapeutic effects of 125I- and 131I-MIBG in 2D and 3D PC-12 cell culture models. We used a Monte Carlo simulation code (PHITS) to calculate the absorbed radiation dose of 125I or 131I in computer simulation models for 2D and 3D cell cultures. In the dosimetry calculation for the 3D model, several distribution patterns of radionuclide were applied. Results: A higher cumulative dose was observed in the 3D model due to the prolonged retention of MIBG compared to the 2D model. However, 125I-MIBG showed a greater therapeutic effect in the 2D model compared to the 3D model (respective EC50 values in the 2D and 3D models: 86.9 and 303.9?MBq/cell), whereas 131I-MIBG showed the opposite result (respective EC50 values in the 2D and 3D models: 49.4 and 30.2?MBq/cell). The therapeutic effect of 125I-MIBG was lower than that of 131I-MIBG in both models, but the radionuclide-derived difference was smaller in the 2D model. The dosimetry simulation with PHITS revealed the influence of the radiation quality, the crossfire effect, radionuclide distribution, and tumor shape on the absorbed dose. Application of the heterogeneous distribution series dramatically changed the radiation dose distribution of 125I-MIBG, and mitigated the difference between the estimated and measured therapeutic effects of 125I-MIBG. Conclusions: The therapeutic effect of 125I-MIBG was comparable to that of 131I-MIBG in the 2D model, but the efficacy was inferior to that of 131I-MIBG in the 3D model, since the crossfire effect is negligible and the homogeneous distribution of radionuclides was insufficient. Thus, auger electrons would be suitable for treating small-sized tumors. The design of radiopharmaceuticals with auger electron emitters requires particularly careful consideration of achieving a homogeneous distribution of the compound in the tumor.

A tin precursor for the synthesis of no-carrier-added [*I]MIBG and [211At]MABG

Radioiodinated MIBG has shown considerable promise as an imaging agent for cardiac and oncologic applications, and also as a targeted radio therapeutic for treating patients with neuroendocrine tumors. This radiolabeled agent, synthesized at a no-carrier-

A convenient method for the preparation of radioiodinated meta-iodobenzylguanidine at a no-carrier-added level

Radioiodinated meta-iodobenzylguanidine (MIBG) in high effective specific activity was prepared using 3-tributylstannylbenzylguanidine as the precursor. The labeling was carried out in aqueous solution with the insoluble and lyophilized precursor suspende

Radioactive iodine labeling method

The invention discloses a radioactive iodine labeling method. Ar-B(OH)2 is allowed to react with NaI in a reaction solvent in the presence of a copper coordination compound so as to obtain Ar-I, so radioactive iodine labeling is realized. The method

A suitable for the clinical application of carrier-free [* I] MIBG preparation method and application of (by machine translation)

The invention provides a method suitable for the clinical application of carrier-free [* I] MIBG preparation method, through three ding xi base animal pen guanidine is dissolved in alcohol solvent and added to the amount of phosphate buffer in

A Highly Efficient Copper-Mediated Radioiodination Approach Using Aryl Boronic Acids

A convenient and quantitative radioiodination method by copper-mediated cross-coupling of aryl boronic acids was developed. The mild labeling conditions, ready availability of the boronic acid substrate, simple operation, broad functional group tolerance and excellent radiochemical yield (RCY) make this a practical strategy for radioiodine labeling without further purification.

Preparation method of 131I-labeled metaiodobenzylguanidine

The invention relates to a method for preparing 131I-metaiodobenzylguanidine with high radioactive specific activity and without a carrier. The method comprises the following steps: performing normal-temperature reaction on a labeled precursor N,N'-di(t-butyloxycarboryl)-3-(tributyltin)-bethanidine, a buffer solution, an oxidizing agent and Na131I for 20 minutes, and adding a reducing agent and heating to 100 DEG C to react for 20 minutes; standing after the reaction is finished, cooling to room temperature, adding anion exchange resin and lightly stirring for 2 minutes; absorbing supernate and passing through a microfiltration membrane to obtain the product. The 131I-metaiodobenzylguanidine, prepared by using hydrogen peroxide--trifluoroacetic acid or N-chlorosuccinimide--sodium pyrosulfite as the oxidizing agent and the reducing agent, has high radiochemical purity and high radioactive specific activity. Reaction byproducts are removed from the 131I-metaiodobenzylguanidine solution after anion exchange resin treatment and microfiltration membrane filtration, and the tin amount is reduced to trace amount, so the 131I-labeled metaiodobenzylguanidine is suitable for clinical diagnosis and treatment. The condition of the labeling reaction is mild and simple, so preparation can be finished in a hospital, and high cost and decay loss of medicines caused by transportation are avoided.

Preparation method of meto-Iodobenzylguanidine

The invention relates to a preparation method of I-MIBG (meto-Iodobenzylguanidine). The method comprises the following steps: heating meto-Iodobenzylguanidine sulfate, stannous mono-sulphate, a reducing agent, copper sulfate and NaI in a boiling water bath, standing after finishing the reaction, taking a supernatant liquid, and filtering the supernatant liquid with a microfiltration membrane. Sodium thiosulfate and/or sodium thiosulfate are/is taken as the reducing agent to prepare the meto-Iodobenzylguanidine sulfate, the prepared I-MIBG is high in radiochemical purity and good in stability, and the radiochemical purity of the prepared I-MIBG is still at a relatively high level after 48 hours.

Preparation method of radioisotope labeling compound using carbon nanotube

Disclosed herein is a method for the preparation of radioisotope-labeled compounds using CNT. It comprises filling the carbon nanotube with a radioisotope; and labeling a physiologically active material with the radioisotope charged in the carbon nanotube. Taking advantage of CNT, the method can prepare a radioisotope-labeled compound invention at a high yield and in a simple manner. Also, the radioisotope, when remaining unreacted, can be recovered by the filtration of the CNT, thereby achieving the prevention of radioactive contamination and the reduction of radioactive waste. Further, the radioisotope-labeled compound is useful as a contrast medium for imaging the hepatobiliary system.