Copper-mediated radiofluorination (CMRF) of organoboronic precursors is the method of choice for late-stage radiofluorination of aromatic compounds as positron emission tomography (PET) radiotracers. However, CMRF generally requires harsh reaction conditions, a large amount of substrates, and harsh solvents (e.g., DMA) to proceed, affording variable radiochemical yields (RCYs). Using [¹⁸F]tosyl fluoride as the source of [¹⁸F]fluoride, we have found a highly efficient CMRF of organoboronic precursors, assisted by a directing group (DG) at the ortho position. The reaction can be carried out under mild conditions (even at room temperature) in acetonitrile and results in high RCYs, providing a novel strategy for the radiofluorination of aromatic compounds. The exploration of this strategy also provided more information about side reactions in CMRF. Using this strategy, [¹⁸F]olaparib has been radiosynthesized in high RCYs, with high molar activity and high chemical and radiochemical purities, demonstrating the great potential of DG-assisted CMRF in the preparation of ¹⁸F-labeled PET radiotracers.

01 Mar 2021·Journal of the Mechanical Behavior of Biomedical MaterialsQ2 · ENGINEERING & TECHNOLOGY

Ex-vivo biomechanical testing of pig femur diaphysis B type fracture fixed by novel biodegradable bone glue

Q2 · ENGINEERING & TECHNOLOGY

Article

Author: Krtička, Milan ; Michlovská, Lenka ; Valová, Kristýna ; Nekuda, Vladimír ; Vojtová, Lucy ; Poláček, Petr ; Žídek, Jan ; Kaiser, Jozef ; Zikmund, Tomáš

AIMSThe aim of this study was to answer the question whether our newly developed injectable biodegradable "self-setting" polymer-composite as a bone adhesive is a good "bone-glue" candidate to efficiently fix comminuted fractures of pig femoral bones used as an ex-vivo experimental model.METHODSMechanical properties of adhesive prepared from α-tricalcium phosphate (TCP) powder and thermogelling copolymer were optimized by selecting the appropriate composition with adhesion enhancers based on dopamine and sodium iodinate. Setting time and injectability were controlled by rheology. Ex-vivo experiments of fixed pig bones were provided in terms of either the three-point bending test of bending wedge type fractured pig femurs (with LCP) or the axial compression test of 45° oblique fractured femurs (without LCP) in physiological saline solution at 37 °C. Fractured bones treated with optimized adhesive before and after bending tests were imaged by X-ray microtomography (μCT).RESULTSBased on the rheological measurement, the adhesive modified with both dopamine and sodium iodinate exhibited optimal thixotropic properties required for injection via thin 22 G needle. This optimal adhesive composition showed an 8 min lag phase (processing time) followed by fast increase in storage modulus at 37 °C up to 1 GPa within 110 min. Self-setting of dopamine/iodinate modified adhesive was completed in 48 h exhibiting the maximum strength at compression of 7.98 MPa ± 1.39 MPa. Whereas unmodified adhesive failed in glue-to-bone adhesion, dopamine and dopamine/iodinate modified adhesive used for 45° oblique fracture fixation showed good and similar strength at compression (3.05 and 2.79 MPa, respectively). However, significantly higher elasticity of about 250% exhibited adhesive with iodinate enhancer. Moreover, mechanical properties of B2 fractures fixed with both LCP and dopamine/iodinate adhesive were approaching closely to the properties of original bone. Excellent adhesion between the adhesive and the bone fragments was proved by μCT.CONCLUSIONThe polymer-composite bone adhesive modified with dopamine/iodinate exhibited very good fixation ability of femoral artificial comminuted fractures in an experimental model.

01 Dec 2018·BMC Research Notes

First in vivo evaluation of a potential SPECT brain radiotracer for the gonadotropin releasing hormone receptor

Article

Author: Riss, Patrick J ; Martin-Armas, Montserrat ; Kuttner, Samuel ; Oteiza, Ana ; Fjellaksel, Richard ; Hjelstuen, Ole Kristian ; Sundset, Rune ; Hansen, Jørn H

OBJECTIVESIn vivo evaluations of a gonadotropin releasing hormone-receptor single photon emission computed tomography radiotracer for non-invasive detection of gonadotropin releasing homone-receptors in brain.RESULTSWe have used a simple, robust and high-yielding procedure to radiolabel an alpha-halogenated bioactive compound with high radiochemical yield. Literature findings showed similar alpha-halogenated compounds suitable for in vivo evaluations. The compound was found to possess nano molar affinity for the gonadotropin releasing hormone-receptor in a competition dependent inhibition study. Furthermore, liquid chromatography-mass spectrometry analysis in saline, human and rat serum resulted in 46%, 52% and 44% stability after incubation for 1 h respectively. In addition, rat brain single photon emission computed tomography and biodistribution studies gave further insight into the nature of the compound as a radiotracer.

100 Deals associated with Sodium Iodinate(123I)

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Indication	Country/Location	Organization	Date
Thyroid Cancer	Australia	Australian Nuclear Science & Technology Organisation	31 May 2005
Thyroid Diseases	Japan	Nihon Medi-Physics Co., Ltd.	13 Mar 1979

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