RESEARCH & RELATED - OTHER PROJECT INFORMATION - PROJECT SUMMARY/ABSTRACT This Core B facility will serve as a technical and scientific support unit for the three projects (1, 2, 3) of this Program Project. Its major goals involve: (1) the re-synthesis and scale-up of compounds in sufficient quantifies to address the in vitro and in vivo needs of the research laboratories involved in the four projects; all compounds will be evaluated in silico for their druggability properties as well (2) the testing of all new ligands for their affinities for the CB1 and CB2 cannabinoid receptors; (3) the testing of ligands for their abilities to bind irreversibly to CB1 and CB2; (4) the testing of a class of ligands for their abilities to act as substrates or inhibitors for the endocannabinoid deactivating enzymes, FAAH and MGL; (5) determining the functional properties of successful ligands initially in the cAMP assay; (6) determining the biochemical stabilities of ligands using liver microsomal preparations; (7) evaluation of a select group of novel ligands in mice for bioavailability and their ability to cross the blood brain barrier; and (8) evaluation of CB1 antagonists in vivo (mice) for their ability to antagonize the effects of an agonist. Compounds produced under the auspices of Core B will also be made available to other laboratories identified in this program project whose collaboration is at no cost to the grant.
Showing the most recent 10 out of 196 publications
