Quantitative in vivo analysis of benzodiazepine binding sites in the human brain using positron emission tomography

1991 ◽  
Vol 30 (3) ◽  
pp. 207-215 ◽  
Author(s):  
Masaomi Iyo ◽  
Takashi Itoh ◽  
Toshiro Yamasaki ◽  
Hiroshi Fukuda ◽  
Osamu Inoue ◽  
...  
Keyword(s):  
Positron Emission Tomography ◽  
Human Brain ◽  
Binding Sites ◽  
Emission Tomography ◽  
Positron Emission ◽  
Benzodiazepine Binding ◽  
In Vivo Analysis ◽  
Benzodiazepine Binding Sites

Central type benzodiazepine binding sites: A positron emission tomography study in the baboon's brain

1984 ◽  
Vol 48 (2) ◽  
pp. 115-120 ◽  
Author(s):  
Philippe Hantraye ◽  
Mitsunobu Kaijima ◽  
Christian Prenant ◽  
Bernard Guibert ◽  
Jacqueline Sastre ◽  
...  
Keyword(s):  
Positron Emission Tomography ◽  
Binding Sites ◽  
Emission Tomography ◽  
Positron Emission Tomography Study ◽  
Central Type ◽  
Positron Emission ◽  
Benzodiazepine Binding ◽  
Benzodiazepine Binding Sites

Validation of In Vitro Cell-Based Human Blood−Brain Barrier Model Using Clinical Positron Emission Tomography Radioligands To Predict In Vivo Human Brain Penetration

2010 ◽  
Vol 7 (5) ◽  
pp. 1805-1815 ◽  
Author(s):  
Aloïse Mabondzo ◽  
Michel Bottlaender ◽  
Anne-Cécile Guyot ◽  
Katya Tsaouin ◽  
Jean Robert Deverre ◽  
...  
Keyword(s):  
Positron Emission Tomography ◽  
Human Brain ◽  
Human Blood ◽  
Emission Tomography ◽  
Brain Penetration ◽  
Positron Emission ◽  
Blood Brain Barrier Model ◽  
Barrier Model

scholarly journals Blocking of Fatty Acid Amide Hydrolase Activity with PF-04457845 in Human Brain: A Positron Emission Tomography Study with the Novel Radioligand [11C]CURB

2015 ◽  
Vol 35 (11) ◽  
pp. 1827-1835 ◽  
Author(s):  
Isabelle Boileau ◽  
Pablo M Rusjan ◽  
Belinda Williams ◽  
Esmaeil Mansouri ◽  
Romina Mizrahi ◽  
...  
Keyword(s):  
Positron Emission Tomography ◽  
Fatty Acid ◽  
Human Brain ◽  
Fatty Acid Amide Hydrolase ◽  
Acid Amide ◽  
Emission Tomography ◽  
Positron Emission ◽  
Amide Hydrolase ◽  
Fatty Acid Amide

Positron emission tomography with [11C]CURB was recently developed to quantify fatty acid amide hydrolase (FAAH), the enzyme responsible for hydrolyzing the endocannabinoid anandamide. This study investigated the test–retest reliability of [11C]CURB as well as its in vivo specificity and the validity of the kinetic model by using the highly specific FAAH inhibitor, PF-04457845. Five healthy volunteers completed test–retest [11C]CURB scans 1 to 2 months apart and six subjects completed baseline and blocking scans on the same day after PF-04457845 (p.o.) administration (1, 4, or 20 mg; n = 2 each). The composite parameter γ k3 (an index of FAAH activity, γ = K1/ k2) was estimated using an irreversible two-tissue compartment model with plasma input function. There were no clinically observable responses to oral PF-04457845 or [11C]CURB injection. Oral administration of PF-04457845 reduced [11C]CURB binding to a homogeneous level at all three doses, with γ k3 values decreased by ≥91%. Excellent reproducibility and good reliability (test–retest variability = 9%; intraclass correlation coefficient = 0.79) were observed across all regions of interest investigated. Our findings suggest that γ k3/[11C]CURB is a reliable, highly sensitive, and selective tool to measure FAAH activity in human brain in vivo. Moreover, PF-04457845 is a highly potent FAAH inhibitor (>95% inhibition at 1 mg) in living human brain.

In Vivo Measurement of Dopamine Receptors in Human Brain by Positron Emission Tomography Age and Sex Differences

1988 ◽  
Vol 515 (1 Central Deter) ◽  
pp. 203-214 ◽  
Author(s):  
DEAN F. WONG ◽  
EMMANUEL P. BROUSSOLLE ◽  
GARY WAND ◽  
VICTOR VILLEMAGNE ◽  
ROBERT F. DANNALS ◽  
...  
Keyword(s):  
Positron Emission Tomography ◽  
Sex Differences ◽  
Human Brain ◽  
Dopamine Receptors ◽  
Emission Tomography ◽  
In Vivo Measurement ◽  
Positron Emission ◽  
Age And Sex

Histamine H1 receptors in human brain visualized in vivo by [11C]doxepin and positron emission tomography

1992 ◽  
Vol 137 (2) ◽  
pp. 145-148 ◽  
Author(s):  
Kazuhiko Yanai ◽  
Takehiko Watanabe ◽  
Hiroyuki Yokoyama ◽  
Kenichi Meguro ◽  
Jun Hatazawa ◽  
...  
Keyword(s):  
Positron Emission Tomography ◽  
Human Brain ◽  
Emission Tomography ◽  
Positron Emission ◽  
Histamine H1 Receptors
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