Synthesis and biological evaluation of a novel series of furans: ligands selective for estrogen receptor α

DS Mortensen, AL Rodriguez, KE Carlson… - Journal of Medicinal …, 2001 - ACS Publications
A variety of nonsteroidal systems can function as ligands for the estrogen receptor (ER), in
some cases showing selectivity for one of the two ER subtypes, ERα or ERβ. We have …

Discovery, characterization, and antiparkinsonian effect of novel positive allosteric modulators of metabotropic glutamate receptor 4

…, CK Jones, Z Xiang, Q Luo, AL Rodriguez… - Molecular …, 2008 - ASPET
Parkinson's disease (PD) is caused by the death of dopamine neurons in the basal ganglia
and results in motor symptoms such as tremor and bradykinesia. Activation of metabotropic …

Discovery of novel allosteric modulators of metabotropic glutamate receptor subtype 5 reveals chemical and functional diversity and in vivo activity in rat behavioral …

AL Rodriguez, MD Grier, CK Jones, EJ Herman… - Molecular …, 2010 - ASPET
Modulators of metabotropic glutamate receptor subtype 5 (mGluR5) may provide novel
treatments for multiple central nervous system (CNS) disorders, including anxiety and …

A selective allosteric potentiator of metabotropic glutamate (mGlu) 2 receptors has effects similar to an orthosteric mGlu2/3 receptor agonist in mouse models …

R Galici, NG Echemendia, AL Rodriguez… - Journal of Pharmacology …, 2005 - ASPET
Recent studies suggest that agonists of group II metabotropic glutamate (mGlu) receptors (mGlu2/3)
have potential utility as novel therapeutic agents for treatment of psychiatric …

An allosteric potentiator of M4 mAChR modulates hippocampal synaptic transmission

…, R Williams, JE Ayala, AL Rodriguez… - Nature chemical …, 2008 - nature.com
Muscarinic acetylcholine receptors (mAChRs) provide viable targets for the treatment of
multiple central nervous system disorders. We have used cheminformatics and medicinal …

Discovery and characterization of novel allosteric potentiators of M1 muscarinic receptors reveals multiple modes of activity

…, EL Days, TM Bridges, Y Xiang, AL Rodriguez… - Molecular …, 2009 - ASPET
Activators of M 1 muscarinic acetylcholine receptors (mAChRs) may provide novel treatments
for schizophrenia and Alzheimer's disease. Unfortunately, the development of M 1 -active …

Design, synthesis, and in vitro biological evaluation of small molecule inhibitors of estrogen receptor α coactivator binding

AL Rodriguez, A Tamrazi, ML Collins… - Journal of medicinal …, 2004 - ACS Publications
Nuclear receptors (NRs) complexed with agonist ligands activate transcription by recruiting
coactivator protein complexes. In principle, one should be able to inhibit the transcriptional …

Functional impact of allosteric agonist activity of selective positive allosteric modulators of metabotropic glutamate receptor subtype 5 in regulating central nervous …

…, HP Cho, E Days, Y Zhou, AL Rodriguez… - Molecular …, 2012 - ASPET
Positive allosteric modulators (PAMs) of metabotropic glutamate receptor subtype 5 (mGlu 5
) have emerged as an exciting new approach for the treatment of schizophrenia and other …

A close structural analog of 2-methyl-6-(phenylethynyl)-pyridine acts as a neutral allosteric site ligand on metabotropic glutamate receptor subtype 5 and blocks the …

AL Rodriguez, Y Nong, NK Sekaran, D Alagille… - Molecular …, 2005 - ASPET
The metabotropic glutamate receptor subtype 5 (mGlu5) activates calcium mobilization via
binding of glutamate, the major excitatory neurotransmitter in the central nervous system. …

Allosteric potentiators of metabotropic glutamate receptor subtype 5 have differential effects on different signaling pathways in cortical astrocytes

Y Zhang, AL Rodriguez, PJ Conn - Journal of Pharmacology and …, 2005 - ASPET
The metabotropic glutamate receptor subtype 5 (mGluR5) activates calcium mobilization
and extracellular signal-regulated kinase 1/2 (ERK1/2) phosphorylation in cortical astrocytes. …