443998-69-4Relevant articles and documents
Discovery of a Potent, Selective, and Brain-Penetrant Small Molecule that Activates the Orphan Receptor GPR88 and Reduces Alcohol Intake
Jin, Chunyang,Decker, Ann M.,Makhijani, Viren H.,Besheer, Joyce,Darcq, Emmanuel,Kieffer, Brigitte L.,Maitra, Rangan
, p. 6748 - 6758 (2018/07/25)
The orphan G-protein-coupled receptor GPR88 is highly expressed in the striatum. Studies using GPR88 knockout mice have suggested that the receptor is implicated in alcohol seeking and drinking behaviors. To date, the biological effects of GPR88 activatio
Synthesis, pharmacological characterization, and structure - Activity relationship studies of small molecular agonists for the orphan GPR88 receptor
Jin, Chunyang,Decker, Ann M.,Huang, Xi-Ping,Gilmour, Brian P.,Blough, Bruce E.,Roth, Bryan L.,Hu, Yang,Gill, Joseph B.,Zhang, X. Peter
, p. 576 - 587 (2014/08/05)
GPR88 is an orphan G-protein-coupled receptor (GPCR) enriched in the striatum. Genetic deletion and gene expression studies have suggested that GPR88 plays an important role in the regulation of striatal functions and is implicated in psychiatric disorder
Structurally simple, potent, Plasmodium selective farnesyltransferase inhibitors that arrest the growth of malaria parasites
Glenn, Matthew P.,Chang, Sung-Youn,Hornéy, Carrie,Rivas, Kasey,Yokoyama, Kohei,Pusateri, Erin E.,Fletcher, Steven,Cummings, Christopher G.,Buckner, Frederick S.,Pendyala, Prakash R.,Chakrabarti, Debopam,Sebti, Sa?d M.,Gelb, Michael,Van Voorhis, Wesley C.,Hamilton, Andrew D.
, p. 5710 - 5727 (2007/10/03)
Third world nations require immediate access to inexpensive therapeutics to counter the high mortality inflicted by malaria. Here, we report a new class of antimalarial protein farnesyltransferase (PFT) inhibitors, designed with specific emphasis on simple molecular architecture, to facilitate easy access to therapies based on this recently validated antimalarial target. This novel series of compounds represents the first Plasmodium falciparum selective PFT inhibitors reported (up to 145-fold selectivity), with lead inhibitors displaying excellent in vitro activity (IC50 50 100 nM). Initial studies of absorption, metabolism, and oral bioavailability are reported.
