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Histone Deacetylase Inhibitor MS-275 Exhibits Poor Brain Penetration: Pharmacokinetic Studies of [ 11 C]MS-275 using Positron Emission Tomography
(American Chemical Society (ACS), 2010)
MS-275 (entinostat) is a histone deacetylase (HDAC) inhibitor currently in clinical trials for the treatment of several types of cancer. Recent reports have noted that MS-275 can cross the blood−brain barrier (BBB) and ...
Salvinorin A and Derivatives: Protection from Metabolism Does Not Prolong Short-Term, Whole-Brain Residence
(Elsevier BV, 2009)
Salvinorin A (SA) is a potent kappa opioid agonist with a brief duration of action. Consistent with this, our previous positron emission tomography (PET) studies of carbon-11 labeled SA showed that brain levels decrease ...
Characterisation of [11C]PR04.MZ in Papio Anubis Baboon: A Selective High-Affinity Radioligand for Quantitative Imaging of the Dopamine Transporter
(Elsevier BV, 2012)
N-(4-fluorobut-2-yn-1-yl)-2β-carbomethoxy-3β-(4′-tolyl)nortropane (PR04.MZ, 1) is a PET radioligand for the non-invasive exploration of the function of the cerebral dopamine transporter (DAT). A reliable automated process ...
One-Pot, Direct Incorporation of [11 C]CO 2 into Carbamates
(Wiley-Blackwell, 2009)
Why beat about the bush? An operationally simple and mild reaction based on the direct fixation of 11CO2 with 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU) has been developed for the synthesis of 11C-labeled carbamates at 75 °C ...
Radiosynthesis and Bioimaging of the Tuberculosis Chemotherapeutics Isoniazid, Rifampicin and Pyrazinamide in Baboons
(American Chemical Society (ACS), 2010)
The front-line tuberculosis (TB) chemotherapeutics isoniazid (INH), rifampicin (RIF), and pyrazinamide (PZA) have been labeled with carbon-11 and the biodistribution of each labeled drug has been determined in baboons using ...
In Vivo Photoactivation Without “Light”: Use of Cherenkov Radiation to Overcome the Penetration Limit of Light
(Springer Nature, 2011)
Purpose: The poor tissue penetration of visible light has been a major barrier for optical imaging, photoactivatable conversions, and photodynamic therapy for in vivo targets with depths beyond 10 mm. In this report, as a ...
A Simple, Rapid Method for the Preparation of [11 C]Formaldehyde
(Wiley-Blackwell, 2008)
A PET project: A powerful reagent for the synthesis of positron-emitting imaging molecules—[11C]formaldehyde—is accessible from [11C]methyl iodide and trimethylamine N-oxide (TMAO) in high yields and under mild conditions. ...
Pharmacokinetics of the Potent Hallucinogen, Salvinorin A in Primates Parallels the Rapid Onset and Short Duration of Effects in Humans
(Elsevier BV, 2008)
Salvia divinorum, a mint plant originally used by the Mazatecs of Oaxaca, Mexico in spiritual rituals has gained popularity, in smoked form, as a legal hallucinogen in the United States and Europe. Abuse results in rapid ...
Rapid Chemoselective Bioconjugation Through Oxidative Coupling of Anilines and Aminophenols
(American Chemical Society (ACS), 2011)
A highly efficient protein bioconjugation method is described involving addition of anilines to o-aminophenols in the presence of sodium periodate. The reaction takes place in aqueous buffer at pH 6.5 and can reach high ...
Radiosynthesis of C-11 Labeled Auxin (3-Indolyl[1-11C]acetic Acid) and Its Derivatives from Gramine
(Wiley-Blackwell, 2011)
3-Indolylacetic acid (IAA) is the major auxin in higher plants and plays a key role in plant growth and development. We report the rapid radiolabeling of the important plant hormone using carbon-11 (half life: 20.4 min) ...