A remote controlled system for the preparation of 7α-[18F]fluoro-17α-methyl 5α-dihydrotestosterone ([18F]FMDHT) using microwave

Garg, Sudha; Lynch, Andrew J.H.; Doke, Aniruddha K.; Minton, Richard C.; Garg, Pradeep

doi:10.1016/j.apradiso.2008.01.017

Cited by 5 publications

(5 citation statements)

References 14 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The trapped [ 18 F]fluoride was eluted from the cartridge with 1.5 mL of kryptofix (K 2.2.2. ) solution prepared as described previously [ 32 ]. The remaining water from this mixture was removed azeotropically using acetonitrile.…”

Section: Methodsmentioning

confidence: 99%

Selective targeting of melanoma using N-(2-diethylaminoethyl) 4-[18F]fluoroethoxy benzamide (4-[18F]FEBZA): a novel PET imaging probe

Garg

Nazih

et al. 2017

EJNMMI Res

Self Cite

View full text Add to dashboard Cite

BackgroundThe purpose of this study was to develop a positron emission tomography (PET) imaging probe that is easy to synthesize and selectively targets melanoma in vivo. Herein, we report the synthesis and preclinical evaluation of N-(2-diethylaminoethyl) 4-[18F]Fluoroethoxy benzamide (4-[18F]FEBZA).A one-step synthesis was developed to prepare 4-[18F]FEBZA in high radiochemical yields and specific activity. The binding affinity, the in vitro binding, and internalization studies were performed using B16F1 melanoma cell line. The biodistribution studies were performed in C57BL/6 normal mice, C57BL/6 mice bearing B16F1 melanoma tumor xenografts, and nu/nu athymic mice bearing HT-29 human adenocarcinoma tumor and C-32 amelanotic melanoma tumor xenografts. MicroPET studies were performed in mice bearing B16F1 and HT-29 tumor xenografts.Results4-[18F]FEBZA was prepared in 53 ± 14% radiochemical yields and a specific activity of 8.7 ± 1.1 Ci/μmol. The overall synthesis time for 4-[18F]FEBZA was 54 ± 7 min. The in vitro binding to B16F1 cells was 60.03 ± 0.48% after 1 h incubation at 37 °C. The in vivo biodistribution studies show a rapid and high uptake of F-18 in B16F1 tumor with 8.66 ± 1.02%IA/g in this tumor at 1 h. In contrast, the uptake at 1 h in HT-29 colorectal adenocarcinoma and C-32 amelanotic melanoma tumors was significantly lower with 3.68 ± 0.47%IA/g and 3.91 ± 0.23%IA/g in HT-29 and C-32 tumors, respectively. On microPET images, the melanoma tumor was clearly visible by 10 min post-injection and the intensity in the tumor continued to increase with time. In contrast, the HT-29 tumor was not visible on the microPET scans.ConclusionsA rapid and facile synthesis of 4-[18F]FEBZA is developed. This method offers a reliable production of 4-[18F]FEBZA in high radiochemical yields and specific activity. A high binding affinity to melanoma cells and high uptake in tumor was noted. The microPET scan clearly delineates the melanoma tumor by 10 min post-injection. The results from these preclinical studies support the potential of 4-[18F]FEBZA as an effective probe to image melanoma.

show abstract

Section: Methodsmentioning

confidence: 99%

Selective targeting of melanoma using N-(2-diethylaminoethyl) 4-[18F]fluoroethoxy benzamide (4-[18F]FEBZA): a novel PET imaging probe

Garg

Nazih

et al. 2017

EJNMMI Res

Self Cite

View full text Add to dashboard Cite

show abstract

“…The radiosynthesis of [ 18 F]FMDHT has been translated onto a remote-controlled automatic system to improve RCY (20-30%), purity (> 99%), and synthesis time (60-70 minutes). 66 Further investigation into the specificity of [ 18 F]FMDHT to AR-rich tissues in chemically castrated rats showed favourable biodistribution that can be blocked with 5-DHT. 67 The authors' final statement suggests that the full potential of [ 18 F] FMDHT as a radioligand should be sought by evaluating uptake in mice bearing tumor xenografts and imaging characteristics in higher species.…”

Section: Ar Radioligandsmentioning

confidence: 98%

PET Imaging of Steroid Hormone Receptor Expression

et al. 2015

View full text Add to dashboard Cite

Steroid hormone receptor (SHR) expression and changes in SHR expression compared to basal levels, whether upregulated, downregulated, or mutated, form a distinguishing feature of some breast, ovarian, and prostate cancers. These receptors act to induce tumor proliferation. In the imaging context, total expression together with modulation of expression can yield predictive and prognostic information. Currently, biopsy for histologic assessment of SHR expression is routine for breast and prostate cancer; however, the technique is not well suited to the heterogeneous tumor environment and can lead to incorrect receptor expression assignment, which precludes effective treatment. The development of positron emission tomography (PET) radioligands to image receptor expression may overcome the difficulties associated with tumor heterogeneity and facilitate the assessment of metastatic disease.

show abstract

“…In this animal model, uptake in the prostate was proven to be AR-mediated. Prostate uptake was comparable to other 18 F-labeled steroids and twofold higher than [ 18 F]FMDHT uptake in DES-treated rats (Garg et al 2008).…”

Section: Pet Tracers For Androgen Receptorsmentioning

confidence: 60%

PET and SPECT Imaging of Steroid Hormone Receptors in the Brain

Moraga-Amaro

Doorduin

Dierckx

et al. 2020

PET and SPECT of Neurobiological Systems

View full text Add to dashboard Cite

Steroid hormones, like sex hormones and corticosteroids, are involved in normal brain function. They can influence behavior and higher functions via binding to the corresponding hormone receptors. Steroid hormones also play a crucial role in psychiatric disorders by interacting with different neurotransmitter systems in the brain. Most of the studies in this field have been performed on postmortem

show abstract

A remote controlled system for the preparation of 7α-[18F]fluoro-17α-methyl 5α-dihydrotestosterone ([18F]FMDHT) using microwave

Cited by 5 publications

References 14 publications

Selective targeting of melanoma using N-(2-diethylaminoethyl) 4-[18F]fluoroethoxy benzamide (4-[18F]FEBZA): a novel PET imaging probe

Selective targeting of melanoma using N-(2-diethylaminoethyl) 4-[18F]fluoroethoxy benzamide (4-[18F]FEBZA): a novel PET imaging probe

PET Imaging of Steroid Hormone Receptor Expression

PET and SPECT Imaging of Steroid Hormone Receptors in the Brain

Contact Info

Product

Resources

About