Regulation of GPR119 receptor activity with endocannabinoid-like lipids

…, TB Farb, J Ficorilli, AK Chesterfield… - American Journal …, 2012 - journals.physiology.org
The GPR119 receptor plays an important role in the secretion of incretin hormones in
response to nutrient consumption. We have studied the ability of an array of naturally occurring …

[HTML][HTML] The PET radioligand [11C] MePPEP binds reversibly and with high specific signal to cannabinoid CB1 receptors in nonhuman primate brain

…, JM Schaus, LA Phebus, AK Chesterfield… - …, 2008 - nature.com
… Competitive binding was either not significant or had a K i value of >10 μM at the following
receptor, ion channel, or enzyme targets: acetylcholinesterase, CCK1, CCK2, EDG-2, Cox1, …

Synthesis, ex vivo evaluation, and radiolabeling of potent 1, 5-diphenylpyrrolidin-2-one cannabinoid subtype-1 receptor ligands as candidates for in vivo imaging

…, E Chernet, L Phebus, AK Chesterfield… - Journal of medicinal …, 2008 - ACS Publications
We have reported that [methyl- 11 C] (3R,5R)-5-(3-methoxyphenyl)-3-[(R)-1-phenylethylamino]-1-(4-trifluoromethylphenyl)pyrrolidin-2-one
([ 11 C]8, [ 11 C]MePPEP) binds with high …

Pharmacological characterization of LY593093, an M1 muscarinic acetylcholine receptor-selective partial orthosteric agonist

…, DA Schober, S Hitchcock, B Liu, AK Chesterfield… - … of Pharmacology and …, 2011 - ASPET
Alzheimer's disease and schizophrenia are characterized by expression of psychotic, affective,
and cognitive symptoms. Currently, there is a lack of adequate treatment for the cognitive …

[HTML][HTML] The muscarinic acetylcholine receptor agonist BuTAC mediates antipsychotic-like effects via the M4 subtype

…, KM Knitowski, AT Quets, AK Chesterfield… - …, 2013 - nature.com
The generation of muscarinic acetylcholine receptor (mAChR) subtype-selective compounds
has been challenging, requiring use of nonpharmacological approaches, such as …

[HTML][HTML] Cannabinoids biology: the search for new therapeutic targets

…, AK Dickason-Chesterfield… - Molecular …, 2006 - triggered.stanford.clockss.org
Cannabinoids, in the form of marijuana plant extracts, have been used for thousands of years
for a wide variety of medical conditions, ranging from general malaise and mood disorders …

Identification of a high-affinity binding site involved in the transport of endocannabinoids

…, AK Dickason-Chesterfield… - Proceedings of the …, 2005 - National Acad Sciences
Phytocannabinoids, such as the principal bioactive component of marijuana, Δ 9 -tetrahydrocannabinol,
have been used for thousands of years for medical and recreational purposes. Δ …

Methods for the Design and Analysis of Replicate‐Experiment Studies to Establish Assay Reproducibility and the Equivalence of Two Potency Assays

BJ Eastwood, AK Chesterfield… - Pharmaceutical …, 2010 - Wiley Online Library
Statistical parameters estimated in validation studies to establish the reliability of single‐concentration
assays, such as the Signal Window and Z'‐Factor, are well established. These …

Pharmacological characterization of the cannabinoid CB1 receptor PET ligand ortholog,[3H] MePPEP

TM Suter, AK Chesterfield, C Bao, JM Schaus… - European journal of …, 2010 - Elsevier
… [ 3 H]MePPEP binding to human CB 1 /CHO membranes was best fit to a one-phase association
model and yielded a K on value of 1.8 × 10 8 (M − 1 , min − 1 ) (Fig. 3). The dissociation …

Pharmacological characterization of endocannabinoid transport and fatty acid amide hydrolase inhibitors

AK Dickason-Chesterfield, SR Kidd, SA Moore… - Cellular and molecular …, 2006 - Springer
1. The mechanism of anandamide uptake and disposal has been an issue of considerable
debate in the cannabinoid field. Several compounds have been reported to inhibit …