Positron emission tomography imaging using an inverse agonist radioligand to assess cannabinoid CB1 receptors in rodents.

PubWeight™: 0.99‹?› | Rank: Top 15%

🔗 View Article (PMC 2474463)

Published in Neuroimage on March 18, 2008

Authors

Garth Terry1, Jeih-San Liow, Eyassu Chernet, Sami S Zoghbi, Lee Phebus, Christian C Felder, Johannes Tauscher, John M Schaus, Victor W Pike, Christer Halldin, Robert B Innis

Author Affiliations

1: Molecular Imaging Branch, National Institute of Mental Health, Bethesda, MD 20892-2035, USA.

Articles citing this

Reversible and regionally selective downregulation of brain cannabinoid CB1 receptors in chronic daily cannabis smokers. Mol Psychiatry (2011) 2.03

Quantitation of cannabinoid CB1 receptors in healthy human brain using positron emission tomography and an inverse agonist radioligand. Neuroimage (2009) 1.42

Elevated brain cannabinoid CB1 receptor availability in post-traumatic stress disorder: a positron emission tomography study. Mol Psychiatry (2013) 1.32

Reduced cannabinoid CB1 receptor binding in alcohol dependence measured with positron emission tomography. Mol Psychiatry (2012) 0.94

Brain and whole-body imaging of nociceptin/orphanin FQ peptide receptor in humans using the PET ligand 11C-NOP-1A. J Nucl Med (2012) 0.94

Brain and whole-body imaging in rhesus monkeys of 11C-NOP-1A, a promising PET radioligand for nociceptin/orphanin FQ peptide receptors. J Nucl Med (2011) 0.90

Test-retest reproducibility of cannabinoid-receptor type 1 availability quantified with the PET ligand [¹¹C]MePPEP. Neuroimage (2014) 0.79

Preclinical evaluation and quantification of [¹⁸F]MK-9470 as a radioligand for PET imaging of the type 1 cannabinoid receptor in rat brain. Eur J Nucl Med Mol Imaging (2012) 0.78

Transient changes in the endocannabinoid system after acute and chronic ethanol exposure and abstinence in the rat: a combined PET and microdialysis study. Eur J Nucl Med Mol Imaging (2013) 0.78

Evaluation of cannabinoid type 1 receptor expression in the rat brain using [¹⁸F]MK-9470 microPET. Eur J Nucl Med Mol Imaging (2013) 0.77

Rapid Changes in CB1 Receptor Availability in Cannabis Dependent Males after Abstinence from Cannabis. Biol Psychiatry Cogn Neurosci Neuroimaging (2016) 0.77

18F-MK-9470 PET imaging of the type 1 cannabinoid receptor in prostate carcinoma: a pilot study. EJNMMI Res (2013) 0.75

[(11)C]TASP457, a novel PET ligand for histamine H3 receptors in human brain. Eur J Nucl Med Mol Imaging (2016) 0.75

Articles cited by this

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

Effects of the cannabinoid-1 receptor blocker rimonabant on weight reduction and cardiovascular risk factors in overweight patients: 1-year experience from the RIO-Europe study. Lancet (2005) 8.01

The endocannabinoid system as an emerging target of pharmacotherapy. Pharmacol Rev (2006) 6.80

Biochemical, cellular, and pharmacological aspects of the multidrug transporter. Annu Rev Pharmacol Toxicol (1999) 6.62

P-glycoprotein in the blood-brain barrier of mice influences the brain penetration and pharmacological activity of many drugs. J Clin Invest (1996) 3.75

The 2006 Henry N. Wagner Lecture: Of mice and men (and positrons)--advances in PET imaging technology. J Nucl Med (2006) 2.65

Inverse agonism and neutral antagonism at cannabinoid CB1 receptors. Life Sci (2004) 2.29

Pharmacological profile of the selective FAAH inhibitor KDS-4103 (URB597). CNS Drug Rev (2006) 2.25

PET imaging of the dopamine transporter with 18F-FECNT: a polar radiometabolite confounds brain radioligand measurements. J Nucl Med (2006) 2.20

(R)-methanandamide: a chiral novel anandamide possessing higher potency and metabolic stability. J Med Chem (1994) 1.80

[18F]MK-9470, a positron emission tomography (PET) tracer for in vivo human PET brain imaging of the cannabinoid-1 receptor. Proc Natl Acad Sci U S A (2007) 1.73

Pharmacological activity of the cannabinoid receptor agonist, anandamide, a brain constituent. Eur J Pharmacol (1993) 1.73

An aromatic microdomain at the cannabinoid CB(1) receptor constitutes an agonist/inverse agonist binding region. J Med Chem (2003) 1.43

Assessment of anandamide interaction with the cannabinoid brain receptor: SR 141716A antagonism studies in mice and autoradiographic analysis of receptor binding in rat brain. J Pharmacol Exp Ther (1998) 1.37

Isolation and expression of a mouse CB1 cannabinoid receptor gene. Comparison of binding properties with those of native CB1 receptors in mouse brain and N18TG2 neuroblastoma cells. Biochem Pharmacol (1997) 1.36

The PET radioligand [11C]MePPEP binds reversibly and with high specific signal to cannabinoid CB1 receptors in nonhuman primate brain. Neuropsychopharmacology (2007) 1.34

Large receptor reserve for cannabinoid actions in the central nervous system. J Pharmacol Exp Ther (1999) 1.26

Effect of a P-glycoprotein inhibitor, Cyclosporin A, on the disposition in rodent brain and blood of the 5-HT1A receptor radioligand, [11C](R)-(-)-RWAY. Synapse (2007) 1.15

Characterization and distribution of binding sites for [3H]-SR 141716A, a selective brain (CB1) cannabinoid receptor antagonist, in rodent brain. Life Sci (1996) 1.10

Aversive effects of the synthetic cannabinoid CP 55,940 in rats. Pharmacol Biochem Behav (1996) 1.08

Evaluation of cannabinoid receptor binding and in vivo activities for anandamide analogs. J Pharmacol Exp Ther (1995) 1.05

Use of LC/MS to assess brain tracer distribution in preclinical, in vivo receptor occupancy studies: dopamine D2, serotonin 2A and NK-1 receptors as examples. Life Sci (2005) 1.04

The endocannabinoid system and rimonabant: a new drug with a novel mechanism of action involving cannabinoid CB1 receptor antagonism--or inverse agonism--as potential obesity treatment and other therapeutic use. J Clin Pharm Ther (2007) 1.01

Kinetic analyses for species differences in P-glycoprotein-mediated drug transport. J Pharm Sci (2006) 0.96

Integrity of extracellular loop 1 of the human cannabinoid receptor 1 is critical for high-affinity binding of the ligand CP 55,940 but not SR 141716A. Biochem Pharmacol (2003) 0.94

Pharmacological characterization of endocannabinoid transport and fatty acid amide hydrolase inhibitors. Cell Mol Neurobiol (2006) 0.93

Cannabinoids. Curr Drug Targets CNS Neurol Disord (2005) 0.92

Characterisation of the rat cerebella CB1 receptor using SR141716A, a central cannabinoid receptor antagonist. Neurosci Lett (1996) 0.89

Articles by these authors

Linearized reference tissue parametric imaging methods: application to [11C]DASB positron emission tomography studies of the serotonin transporter in human brain. J Cereb Blood Flow Metab (2003) 3.77

Selective muscarinic receptor agonist xanomeline as a novel treatment approach for schizophrenia. Am J Psychiatry (2008) 3.51

Peripheral cannabinoid-1 receptor inverse agonism reduces obesity by reversing leptin resistance. Cell Metab (2012) 2.76

Strategies to improve neuroreceptor parameter estimation by linear regression analysis. J Cereb Blood Flow Metab (2002) 2.58

Kinetic analysis in healthy humans of a novel positron emission tomography radioligand to image the peripheral benzodiazepine receptor, a potential biomarker for inflammation. Neuroimage (2007) 2.50

Activation and allosteric modulation of a muscarinic acetylcholine receptor. Nature (2013) 2.49

PET imaging of the dopamine transporter with 18F-FECNT: a polar radiometabolite confounds brain radioligand measurements. J Nucl Med (2006) 2.20

Synthesis and evaluation in monkey of two sensitive 11C-labeled aryloxyanilide ligands for imaging brain peripheral benzodiazepine receptors in vivo. J Med Chem (2007) 2.11

Mixed-affinity binding in humans with 18-kDa translocator protein ligands. J Nucl Med (2010) 2.00

Brain and whole-body imaging in nonhuman primates of [11C]PBR28, a promising PET radioligand for peripheral benzodiazepine receptors. Neuroimage (2007) 1.91

Fast and high-yield microreactor syntheses of ortho-substituted [(18)F]fluoroarenes from reactions of [(18)F]fluoride ion with diaryliodonium salts. J Org Chem (2010) 1.91

Increased dopamine transporter availability associated with the 9-repeat allele of the SLC6A3 gene. J Nucl Med (2005) 1.89

Comparison of [(11)C]-(R)-PK 11195 and [(11)C]PBR28, two radioligands for translocator protein (18 kDa) in human and monkey: Implications for positron emission tomographic imaging of this inflammation biomarker. Neuroimage (2009) 1.89

Downregulation of brain phosphodiesterase type IV measured with 11C-(R)-rolipram positron emission tomography in major depressive disorder. Biol Psychiatry (2012) 1.85

Radiation dosimetry and biodistribution in monkey and man of 11C-PBR28: a PET radioligand to image inflammation. J Nucl Med (2007) 1.81

Increase in prefrontal cortex serotonin 2A receptors following estrogen treatment in postmenopausal women. Am J Psychiatry (2003) 1.77

Autoradiographic distribution of serotonin transporters and receptor subtypes in human brain. Hum Brain Mapp (2004) 1.76

Use of M1-M5 muscarinic receptor knockout mice as novel tools to delineate the physiological roles of the muscarinic cholinergic system. Neurochem Res (2003) 1.75

Decreased dopamine D2 receptor binding in the anterior cingulate cortex in schizophrenia. Arch Gen Psychiatry (2002) 1.75

P-glycoprotein function at the blood-brain barrier in humans can be quantified with the substrate radiotracer 11C-N-desmethyl-loperamide. J Nucl Med (2010) 1.62

A genetic polymorphism for translocator protein 18 kDa affects both in vitro and in vivo radioligand binding in human brain to this putative biomarker of neuroinflammation. J Cereb Blood Flow Metab (2012) 1.59

Guideline to regulations for radiopharmaceuticals in early phase clinical trials in the EU. Eur J Nucl Med Mol Imaging (2008) 1.58

In vivo radioligand binding to translocator protein correlates with severity of Alzheimer's disease. Brain (2013) 1.57

New insights into the function of M4 muscarinic acetylcholine receptors gained using a novel allosteric modulator and a DREADD (designer receptor exclusively activated by a designer drug). Mol Pharmacol (2008) 1.57

PET imaging with [11C]PBR28 can localize and quantify upregulated peripheral benzodiazepine receptors associated with cerebral ischemia in rat. Neurosci Lett (2006) 1.56

Fluoxetine administered to juvenile monkeys: effects on the serotonin transporter and behavior. Am J Psychiatry (2014) 1.54

P-glycoprotein function at the blood-brain barrier imaged using 11C-N-desmethyl-loperamide in monkeys. J Nucl Med (2008) 1.53

Approaches to quantify radioligands that wash out slowly from target organs. Eur J Nucl Med Mol Imaging (2010) 1.52

Decreased neurokinin-1 (substance P) receptor binding in patients with panic disorder: positron emission tomographic study with [18F]SPA-RQ. Biol Psychiatry (2009) 1.47

The "specific" P-glycoprotein inhibitor Tariquidar is also a substrate and an inhibitor for breast cancer resistance protein (BCRP/ABCG2). ACS Chem Neurosci (2010) 1.46

Reduced serotonin-1A receptor binding in social anxiety disorder. Biol Psychiatry (2006) 1.46

Fluoxetine, but not other selective serotonin uptake inhibitors, increases norepinephrine and dopamine extracellular levels in prefrontal cortex. Psychopharmacology (Berl) (2002) 1.46

Molecular mechanisms of action and in vivo validation of an M4 muscarinic acetylcholine receptor allosteric modulator with potential antipsychotic properties. Neuropsychopharmacology (2009) 1.45

Syntheses of 11C- and 18F-labeled carboxylic esters within a hydrodynamically-driven micro-reactor. Lab Chip (2004) 1.44

Molecular imaging of the dopaminergic system and its association with human cognitive function. Biol Psychiatry (2006) 1.44

Synthesis and evaluation of [N-methyl-11C]N-desmethyl-loperamide as a new and improved PET radiotracer for imaging P-gp function. J Med Chem (2008) 1.43

Support for dopaminergic hypoactivity in restless legs syndrome: a PET study on D2-receptor binding. Brain (2006) 1.43

Characterization of a novel endocannabinoid, virodhamine, with antagonist activity at the CB1 receptor. J Pharmacol Exp Ther (2002) 1.43

Image-derived input function for brain PET studies: many challenges and few opportunities. J Cereb Blood Flow Metab (2011) 1.42

Quantitation of cannabinoid CB1 receptors in healthy human brain using positron emission tomography and an inverse agonist radioligand. Neuroimage (2009) 1.42

The role of the striatal dopamine transporter in cognitive aging. Psychiatry Res (2005) 1.42

Role of specific muscarinic receptor subtypes in cholinergic parasympathomimetic responses, in vivo phosphoinositide hydrolysis, and pilocarpine-induced seizure activity. Eur J Neurosci (2003) 1.41

Reduced midbrain dopamine transporter binding in male adolescents with attention-deficit/hyperactivity disorder: association between striatal dopamine markers and motor hyperactivity. Biol Psychiatry (2005) 1.40

Application of calibrated image-derived input function to a clinical protocol. Nucl Med Commun (2014) 1.38

11C-loperamide and its N-desmethyl radiometabolite are avid substrates for brain permeability-glycoprotein efflux. J Nucl Med (2008) 1.37

Metabotropic glutamate subtype 5 receptors are quantified in the human brain with a novel radioligand for PET. J Nucl Med (2008) 1.37