Positron emission tomography neuroreceptor imaging as a tool in drug discovery, research and development

Burns, H. Donald; Hamill, Terence G.; Eng, Wai-si; Francis, Barbara; Fioravanti, Christine; Gibson, Raymond E.

doi:10.1016/s1367-5931(99)80059-3

Cited by 46 publications

(23 citation statements)

References 17 publications

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“…Outside of the clinic, small animal PET is widely used in basic biomedical research and development, providing quantitative assays for the study of gene expression, metabolism and signal transduction, and drug biodistribution (15,(17)(18)(19). Preclinical drug screening by PET has been exploited for elucidating small molecule permeability to the blood-brain barrier (20,21), and in human microdosing studies of experimental therapeutics during early clinical development (15,16). In addition, the low-mass dose of radiolabeled PET probes (ie, high specific activity compounds injected at nanomolar concentrations, yielding picomoles of probe/g tissue) allows for detailed biodistribution analysis of target drugs without perturbing normal biological processes (17,18).…”

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confidence: 99%

In vivo imaging of pyrrole-imidazole polyamides with positron emission tomography

Harki

Satyamurthy

Stout

et al. 2008

Proc. Natl. Acad. Sci. U.S.A.

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The biodistribution profiles in mice of two pyrrole-imidazole polyamides were determined by PET. Pyrrole-imidazole polyamides are a class of small molecules that can be programmed to bind a broad repertoire of DNA sequences, disrupt transcription factor-DNA interfaces, and modulate gene expression pathways in cell culture experiments. The 18 F-radiolabeled polyamides were prepared by oxime ligation between 4-[ 18 F]-fluorobenzaldehyde and a hydroxylamine moiety at the polyamide C terminus. Small animal PET imaging of radiolabeled polyamides administered to mice revealed distinct differences in the biodistribution of a 5-ring ␤-linked polyamide versus an 8-ring hairpin, which exhibited better overall bioavailability. In vivo imaging of pyrrole-imidazole polyamides by PET is a minimum first step toward the translation of polyamidebased gene regulation from cell culture to small animal studies.biodistribution ͉ fluorine-18 ͉ oxime ͉ radiosynthesis

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mentioning

confidence: 99%

In vivo imaging of pyrrole-imidazole polyamides with positron emission tomography

Harki

Satyamurthy

Stout

et al. 2008

Proc. Natl. Acad. Sci. U.S.A.

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“…Radiopharmaceuticals with an affinity to the neurotransmitter system have been applied in neurological and psychiatric research, e.g. in Parkinson's disease and other motor disorders, in depression and schizophrenia [74][75][76][77]. Whereas first knowledge about the neurotransmitter system is usually acquired by animal research or post-mortem studies, PET can verify these findings in the human being in vivo.…”

Section: Neurological Petmentioning

confidence: 99%

In vivo functional imaging with SPECT and PET

Herzog

2001

Radiochimica Acta

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Single photon emission computed tomography / Positron emission tomography / Functional imaging / Radiopharmaceuticals / Gamma cameraSummary. Nuclear medicine methods permit the visualisation of a variety of metabolic and physiological processes all over the body. Although planar scintigraphy has been found useful for many questions, detailed spatial information about the diseased organ can only be obtained with tomographic methods. Dependent on the radionuclide involved, two different tomographic procedures are available: single photon emission computed tomography (SPECT) and positron emission tomography (PET). The first part of this paper describes shortly the historical development of these methods as well as their technical and methodological basics. To elucidate the large variety of possible applications, an overview of SPECT and PET procedures utilised in research as well as in clinical practice are presented. Furthermore, both methods are compared and their individual advantages are pointed out.

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“…One useful tool for this is positron emission tomography (PET) which is a non-invasive technique. 16 PET utilizes specifically designed radiotracers with affinity and selectivity for target receptors. Ligand development is the crucial part of PET studies.…”

Section: Introductionmentioning

confidence: 99%

N1'-(p-[18F]Fluorobenzyl)naltrindole (p-[18F]BNTI) as a potential PET imaging agent for DOP receptors

Akgün¹,

Sajjad²,

Portoghese³

2006

J Label Compd Radiopharm

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SummaryThe N1'-(p-fluorobenzyl)naltrindole 5 has been synthesized by reaction of 3-O-benzyl NTI 3 with p-fluorobenzylbromide under phase transfer catalysis. The subsequent 3-O-benzyldeprotection of 4 in HBr/CH 3 COOH gave the target compound 5 in three steps from naltrindole 2. p-FBNTI 5 is a novel delta opioid receptor antagonist (K i =0.00312 nM) and antagonizes the delta opioid (DOP) agonist, DPDPE, with a K e =1.55 nM in the mouse vas deferens preparation. Using the same synthetic strategy the synthesis of p-[18 F]BNTI 10 was undertaken. The final yield was 4% and the specific activity varied in a range of 250-400 mCi/mmol.

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Positron emission tomography neuroreceptor imaging as a tool in drug discovery, research and development

Cited by 46 publications

References 17 publications

In vivo imaging of pyrrole-imidazole polyamides with positron emission tomography

In vivo imaging of pyrrole-imidazole polyamides with positron emission tomography

In vivo functional imaging with SPECT and PET

N1'-(p-[18F]Fluorobenzyl)naltrindole (p-[18F]BNTI) as a potential PET imaging agent for DOP receptors

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