Tactics for preclinical validation of receptor-binding radiotracers.

PubWeight™: 0.75‹?›

🔗 View Article (PMID 27755986)

Published in Nucl Med Biol on September 03, 2016

Authors

Susan Z Lever1, Kuo-Hsien Fan2, John R Lever3

Author Affiliations

1: Department of Chemistry, University of Missouri, Columbia, MO, USA; University of Missouri Research Reactor Center, Columbia, MO, USA. Electronic address: levers@missouri.edu.
2: Department of Chemistry, University of Missouri, Columbia, MO, USA.
3: Department of Radiology, University of Missouri, Columbia, MO, USA; Research Service, Harry S. Truman Memorial Veterans' Hospital, Columbia, MO, USA. Electronic address: leverj@health.missouri.edu.

Articles cited by this

(truncated to the top 100)

Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction. Biochem Pharmacol (1973) 47.81

Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings. Adv Drug Deliv Rev (2001) 36.00

Consensus nomenclature for in vivo imaging of reversibly binding radioligands. J Cereb Blood Flow Metab (2007) 11.79

Policy: NIH to balance sex in cell and animal studies. Nature (2014) 9.15

The effects of morphine- and nalorphine- like drugs in the nondependent and morphine-dependent chronic spinal dog. J Pharmacol Exp Ther (1976) 9.13

Placebo effects mediated by endogenous opioid activity on mu-opioid receptors. J Neurosci (2005) 4.00

Automated design of ligands to polypharmacological profiles. Nature (2012) 3.54

The pharmacology of sigma-1 receptors. Pharmacol Ther (2009) 3.12

A quantitative model for the in vivo assessment of drug binding sites with positron emission tomography. Ann Neurol (1984) 3.11

Structural basis of the drug-binding specificity of human serum albumin. J Mol Biol (2005) 3.00

Relationship between subjective effects of cocaine and dopamine transporter occupancy. Nature (1997) 2.94

Coordinating radiometals of copper, gallium, indium, yttrium, and zirconium for PET and SPECT imaging of disease. Chem Rev (2010) 2.70

A proposal for the classification of sigma binding sites. Trends Pharmacol Sci (1992) 2.65

Medicinal chemical properties of successful central nervous system drugs. NeuroRx (2005) 2.55

Determination of lipophilicity and its use as a predictor of blood-brain barrier penetration of molecular imaging agents. Mol Imaging Biol (2003) 2.40

Sigma receptors: biology and function. Pharmacol Rev (1990) 2.37

Quantifying the chemical beauty of drugs. Nat Chem (2012) 2.36

PET radiotracers: crossing the blood-brain barrier and surviving metabolism. Trends Pharmacol Sci (2009) 2.32

Moving beyond rules: the development of a central nervous system multiparameter optimization (CNS MPO) approach to enable alignment of druglike properties. ACS Chem Neurosci (2010) 2.06

Opiate receptor: autoradiographic localization in rat brain. Proc Natl Acad Sci U S A (1976) 2.01

Calculating receptor number from binding experiments using same compound as radioligand and competitor. Trends Pharmacol Sci (1989) 2.01

Simultaneous assessment of rodent behavior and neurochemistry using a miniature positron emission tomograph. Nat Methods (2011) 1.88

Appropriate use criteria for amyloid PET: a report of the Amyloid Imaging Task Force, the Society of Nuclear Medicine and Molecular Imaging, and the Alzheimer's Association. Alzheimers Dement (2013) 1.87

Transparency in Research involving Animals: The Basel Declaration and new principles for reporting research in BJP manuscripts. Br J Pharmacol (2015) 1.79

Laminin receptor specific therapeutic gold nanoparticles (198AuNP-EGCg) show efficacy in treating prostate cancer. Proc Natl Acad Sci U S A (2012) 1.72

Ligand binding assays at equilibrium: validation and interpretation. Br J Pharmacol (2010) 1.71

Positron emission tomography microdosing: a new concept with application in tracer and early clinical drug development. Eur J Clin Pharmacol (2003) 1.65

The role of coordination chemistry in the development of target-specific radiopharmaceuticals. Chem Soc Rev (2004) 1.60

Gender and age influences on human brain mu-opioid receptor binding measured by PET. Am J Psychiatry (1999) 1.59

Enhanced sphingosine-1-phosphate receptor 2 expression underlies female CNS autoimmunity susceptibility. J Clin Invest (2014) 1.58

Positron emission tomography molecular imaging for drug development. Br J Clin Pharmacol (2012) 1.56

Imaging dopamine receptors in the human brain by positron tomography. Science (1983) 1.55

Anesthesia and other considerations for in vivo imaging of small animals. ILAR J (2008) 1.53

Protein binding: do we ever learn? Antimicrob Agents Chemother (2011) 1.46

Selective sigma-2 ligands preferentially bind to pancreatic adenocarcinomas: applications in diagnostic imaging and therapy. Mol Cancer (2007) 1.46

Calculation of molecular lipophilicity: State-of-the-art and comparison of log P methods on more than 96,000 compounds. J Pharm Sci (2009) 1.45

An admonition when measuring the lipophilicity of radiotracers using counting techniques. Appl Radiat Isot (2001) 1.36

High occupancy of sigma-1 receptors in the human brain after single oral administration of fluvoxamine: a positron emission tomography study using [11C]SA4503. Biol Psychiatry (2007) 1.33

Opinion: Sex inclusion in basic research drives discovery. Proc Natl Acad Sci U S A (2015) 1.32

Radioligand binding methods: practical guide and tips. Am J Physiol (1993) 1.29

The emerging field of neuroepigenetics. Neuron (2013) 1.28

Relationship between psychostimulant-induced "high" and dopamine transporter occupancy. Proc Natl Acad Sci U S A (1996) 1.27

[3H]N-[4-(3,4-dihydro-6,7-dimethoxyisoquinolin-2(1H)-yl)butyl]-2-methoxy-5-methylbenzamide: a novel sigma-2 receptor probe. Eur J Pharmacol (2005) 1.26

Anaesthesia and physiological monitoring during in vivo imaging of laboratory rodents: considerations on experimental outcomes and animal welfare. EJNMMI Res (2012) 1.25

Targeting ligand-operated chaperone sigma-1 receptors in the treatment of neuropsychiatric disorders. Expert Opin Ther Targets (2011) 1.22

In vivo site-directed radiotracers: a mini-review. Nucl Med Biol (2008) 1.19

Quantification of cerebral cannabinoid receptors subtype 1 (CB1) in healthy subjects and schizophrenia by the novel PET radioligand [11C]OMAR. Neuroimage (2010) 1.19

Cannabinoid receptor type 2 (CB2)-selective N-aryl-oxadiazolyl-propionamides: synthesis, radiolabelling, molecular modelling and biological evaluation. Org Med Chem Lett (2012) 1.18

Sigma1 and sigma2 receptor binding affinity and selectivity of SA4503 and fluoroethyl SA4503. Synapse (2006) 1.17

Relationship between brain serotonin transporter binding, plasma concentration and behavioural effect of selective serotonin reuptake inhibitors. Br J Pharmacol (2005) 1.15

Molecular imaging and personalized medicine: an uncertain future. Cancer Biother Radiopharm (2007) 1.15

The σ2 receptor: a novel protein for the imaging and treatment of cancer. J Med Chem (2013) 1.13

Gender-dependent increases with healthy aging of the human cerebral cannabinoid-type 1 receptor binding using [(18)F]MK-9470 PET. Neuroimage (2007) 1.12

Measuring dopamine transporter occupancy by cocaine in vivo: radiotracer considerations. Synapse (1998) 1.10

High occupancy of sigma1 receptors in the human brain after single oral administration of donepezil: a positron emission tomography study using [11C]SA4503. Int J Neuropsychopharmacol (2009) 1.09

Cognition and depression: the effects of fluvoxamine, a sigma-1 receptor agonist, reconsidered. Hum Psychopharmacol (2010) 1.07

Development of molecular probes for imaging sigma-2 receptors in vitro and in vivo. Cent Nerv Syst Agents Med Chem (2009) 1.07

DMSO-related effects in protein characterization. J Biomol Screen (2006) 1.06

Differential sorting of human delta-opioid receptors after internalization by peptide and alkaloid agonists. J Biol Chem (2003) 1.06

CNS drug design: balancing physicochemical properties for optimal brain exposure. J Med Chem (2015) 1.05

Guidance on current good radiopharmacy practice (cGRPP) for the small-scale preparation of radiopharmaceuticals. Eur J Nucl Med Mol Imaging (2010) 1.04

Conformationally-flexible benzamide analogues as dopamine D3 and sigma 2 receptor ligands. Bioorg Med Chem Lett (2004) 1.03

Studying both sexes: a guiding principle for biomedicine. FASEB J (2015) 1.02

On quantitative relationships between drug-like compound lipophilicity and plasma free fraction in monkey and human. J Pharm Sci (2011) 1.02

Opinion: Focus on preclinical sex differences will not address women's and men's health disparities. Proc Natl Acad Sci U S A (2015) 1.01

Characterization of the binding of [3H](+)-pentazocine to sigma recognition sites in guinea pig brain. Eur J Pharmacol (1992) 0.99

Potentials and pitfalls using high affinity radioligands in PET and SPET determinations on regional drug induced D2 receptor occupancy--a simulation study based on experimental data. Neuroimage (2001) 0.98

Suggested pathway to assess radiation safety of 11C-labeled PET tracers for first-in-human studies. Eur J Nucl Med Mol Imaging (2011) 0.98

Binding properties of SA4503, a novel and selective sigma 1 receptor agonist. Eur J Pharmacol (1996) 0.98

[(11)C]-GR89696, a potent kappa opiate receptor radioligand; in vivo binding of the R and S enantiomers. Nucl Med Biol (2002) 0.97

Establishment of in vivo brain imaging method in conscious mice. J Nucl Med (2010) 0.96

Mu opiate receptors are selectively labelled by [3H]carfentanil in human and rat brain. Eur J Pharmacol (1989) 0.96

Considerations in the Development of Reversibly Binding PET Radioligands for Brain Imaging. Curr Med Chem (2016) 0.96

Radiosynthesis of an opiate receptor binding radiotracer: [11C]carfentanil. Int J Appl Radiat Isot (1985) 0.95

Synthesis and in vivo evaluation of 2 high-affinity 76Br-labeled sigma2-receptor ligands. J Nucl Med (2006) 0.95

Imaging the high-affinity state of the dopamine D2 receptor in vivo: fact or fiction? Biochem Pharmacol (2011) 0.94

Imaging opiate receptors in the human brain by positron tomography. J Comput Assist Tomogr (1985) 0.94

MicroPET/SPECT/CT imaging of small animal models of disease. Am J Pathol (2012) 0.94

SA 4503 attenuates cocaine-induced hyperactivity and enhances methamphetamine substitution for a cocaine discriminative stimulus. Pharmacol Biochem Behav (2010) 0.94

Synthesis and pharmacological evaluation of 6-acetyl-3-(4-(4-(4-fluorophenyl)piperazin-1-yl)butyl)benzo[d]oxazol-2(3H)-one (SN79), a cocaine antagonist, in rodents. AAPS J (2011) 0.94

Targeted imaging: an important biomarker for understanding disease progression in the era of personalized medicine. Drug Discov Today (2008) 0.93

Real-time 3D motion tracking for small animal brain PET. Phys Med Biol (2008) 0.93

Dopamine receptor parameters detected by [3H]spiperone depend on tissue concentration: analysis and examples. J Neurochem (1984) 0.93

[3H]nisoxetine: a new radioligand for norepinephrine uptake sites in brain. Eur J Pharmacol (1990) 0.92

Transport of selected PET radiotracers by human P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2): an in vitro screening. J Nucl Med (2011) 0.91

Light autoradiographic localisation of cholinergic muscarinic receptors in rat brain by specific binding of a potent antagonist. Nature (1975) 0.91

Discussion of targeting proteins in vivo: in vitro guidelines. Nucl Med Biol (2006) 0.90

Direct comparison of radiation dosimetry of six PET tracers using human whole-body imaging and murine biodistribution studies. Ann Nucl Med (2013) 0.90

Rat-PET study without anesthesia: anesthetics modify the dopamine D1 receptor binding in rat brain. Synapse (2004) 0.89

Predicting the success of a radiopharmaceutical for in vivo imaging of central nervous system neuroreceptor systems. Mol Imaging Biol (2003) 0.89

How Beyond Rule of 5 Drugs and Clinical Candidates Bind to Their Targets. J Med Chem (2015) 0.89

PET measurement of the in vivo affinity of 11C-(R)-rolipram and the density of its target, phosphodiesterase-4, in the brains of conscious and anesthetized rats. J Nucl Med (2009) 0.88

Radiosyntheses using fluorine-18: the art and science of late stage fluorination. Curr Top Med Chem (2014) 0.88

High affinity dopamine D2 receptor radioligands. 1. Regional rat brain distribution of iodinated benzamides. J Nucl Med (1991) 0.88

Sigma-1 receptor chaperones regulate the secretion of brain-derived neurotrophic factor. Synapse (2012) 0.88

Intrathecal delivery of protein therapeutics to the brain: a critical reassessment. Pharmacol Ther (2014) 0.87

Sigma (σ) receptors as potential therapeutic targets to mitigate psychostimulant effects. Adv Pharmacol (2014) 0.87

Recent advances in metabolic imaging. J Nucl Cardiol (2013) 0.87

In vitro studies on the distribution of probucol among human plasma lipoproteins. Mol Pharmacol (1984) 0.87

Preclinical imaging: an essential ally in modern biosciences. Mol Diagn Ther (2014) 0.86