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Small animal SPECT and its place in the matrix of molecular imaging technologies
The technology developments and design tradeoffs that led to the current state-of-the-art in SPECT small animal scanning are reviewed and the position SPECT occupies within the matrix of molecular imaging technologies is described.
Comparative Evaluation of the Translocator Protein Radioligands 11C-DPA-713, 18F-DPA-714, and 11C-PK11195 in a Rat Model of Acute Neuroinflammation
In vivo, 18F-DPA-714 appears to be an attractive alternative to 11C-PK11195 because of its increased bioavailability in brain tissue and its reduced nonspecific binding, and its labeling with 18F, the preferred PET isotope for radiopharmaceutical chemistry, favors its dissemination and wide clinical use.
Pharmacology of Valinate and tert-Leucinate Synthetic Cannabinoids 5F-AMBICA, 5F-AMB, 5F-ADB, AMB-FUBINACA, MDMB-FUBINACA, MDMB-CHMICA, and Their Analogues.
In vitro and in vivo data indicate that these SCs act as highly efficacious CB receptor agonists with greater potency than Δ(9)-THC and earlier generations of SCs.
Imaging of Glial Cell Activation and White Matter Integrity in Brains of Active and Recently Retired National Football League Players
The results suggest that localized brain injury and repair, indicated by higher TSPO signal and white matter changes, may be associated with NFL play.
The Translocator Protein
The incomplete characterization of multiple T SPO binding sites and the role of TSPO polymerization suggest that current interpretation of PET data may require further refinement, and this work has highlighted the importance of understanding the interaction of ligands with the protein.
Effects of bioisosteric fluorine in synthetic cannabinoid designer drugs JWH-018, AM-2201, UR-144, XLR-11, PB-22, 5F-PB-22, APICA, and STS-135.
In vitro functional activities of SC designer drugs JWH-018, UR-144, PB-22, and APICA, and their respective terminally fluorinated analogues and in vivo in vivo cannabinoid type 1 receptor binding affinity evaluated in rats showed no consistent trend for increased potency of fluorinated SCs over the corresponding des-fluoro SCs in vivo.
Evaluation of the PBR/TSPO Radioligand [18F]DPA-714 in a Rat Model of Focal Cerebral Ischemia
- Abraham Martín, R. Boisgard, B. Tavitian
- BiologyJournal of cerebral blood flow and metabolism…
- 1 January 2010
Results show that in vivo PET imaging with [18F]DPA-714 provides accurate quantitative information of the time course of PBR/TSPO expression in experimental stroke.
Acute Prosocial Effects of Oxytocin and Vasopressin When Given Alone or in Combination with 3,4-Methylenedioxymethamphetamine in Rats: Involvement of the V1A Receptor
Results show for the first time acute prosocial effects of peripherally injected OT and AVP in laboratory rats, and suggest a commonality of action of OT, AVP, and MDMA in stimulating social behavior that involves V1ARs.
The Nonpeptide Oxytocin Receptor Agonist WAY 267,464: Receptor‐Binding Profile, Prosocial Effects and Distribution of c‐Fos Expression in Adolescent Rats
The results confirm the differential effects of WAY 267,464 and oxytocin and suggest that this may reflect contrasting actions of ways of treating prosocial effects of this drug either through a direct action or through disinhibition of Oxytocin circuitry that is subject to vasopressin inhibitory influences.
DPA-714, a New Translocator Protein–Specific Ligand: Synthesis, Radiofluorination, and Pharmacologic Characterization
The synthesis, radiofluorination, and pharmacologic evaluation of a new TSPO-specific pyrazolopyrimidine, DPA-714, shows promising in vivo properties and is warranting further investigation.