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A Selective Allosteric Potentiator of Metabotropic Glutamate (mGlu) 2 Receptors Has Effects Similar to an Orthosteric mGlu2/3 Receptor Agonist in Mouse Models Predictive of Antipsychotic Activity
- R. Galici, Nicholas G Echemendia, Alice L. Rodriguez, P. Conn
- Biology, PsychologyJournal of Pharmacology and Experimental…
- 1 December 2005
The finding that the effects of an orthosteric mGlu2/3 receptor agonist in these models can be mimicked by a selective allosteric potentiator of mGLU2 suggests that these effects are mediated by the mGlam2 receptor subtype.
An allosteric potentiator of M4 mAChR modulates hippocampal synaptic transmission.
W Whole-cell patch clamp recordings revealed that selective potentiation of M4 with VU10010 increases carbachol-induced depression of transmission at excitatory but not inhibitory synapses in the hippocampus, suggesting that targeting of individual mAChR subtypes could be used to differentially regulate specific aspects of mA ChR modulation of function in this important forebrain structure.
Discovery, Characterization, and Antiparkinsonian Effect of Novel Positive Allosteric Modulators of Metabotropic Glutamate Receptor 4
High-throughput screening found more than 400 novel PAMs of mGluR4, and resolution of the regioisomers of the lead revealed that this compound is a mixed allosteric agonist/PAM of m GluR 4, providing continued support for mGLUR4 as a therapeutic target in PD.
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 Effects of Multiple Allosteric…
- Alice L. Rodriguez, Y. Nong, N. Sekaran, D. Alagille, G. Tamagnan, P. Conn
- Biology, ChemistryMolecular Pharmacology
- 1 December 2005
Three novel compounds that bind to the allosteric 2-methyl-6-(phenylethynyl)-pyridine (MPEP) site on mGlu5 but have only partial inhibition or no functional effects on the mGLU5 response are reported.
Discovery of Novel Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 5 Reveals Chemical and Functional Diversity and In Vivo Activity in Rat Behavioral Models of Anxiolytic and…
Discovery of structurally and functionally diverse allosteric modulators of mGluR5 that demonstrate in vivo efficacy in rodent models of anxiety and antipsychotic activity provide further support for the tremendous diversity of chemical scaffolds and modes of efficacy of mR5 ligands.
Allosteric Potentiators of Metabotropic Glutamate Receptor Subtype 5 Have Differential Effects on Different Signaling Pathways in Cortical Astrocytes
- Yongqin Zhang, Alice L. Rodriguez, P. Conn
- Biology, ChemistryJournal of Pharmacology and Experimental…
- 1 December 2005
Examination of the effects of CPPHA and DFB on mGluR5-induced calcium transients and ERK1/2 phosphorylation in cultured rat cortical astrocytes provides evidence that different allosteric potentiators can differentially modulate coupling of a single receptor to different signaling pathways.
Discovery of a Novel Chemical Class of mGlu5 Allosteric Ligands with Distinct Modes of Pharmacology
We previously discovered a positive allosteric modulator (PAM) of the metabotropic glutamate receptor subtype 5 (mGlu5) termed 4…
Allosteric control of ligand selectivity between estrogen receptors alpha and beta: implications for other nuclear receptors.
The determinants of ligand selectivity between the two estrogen receptor subtypes ERalpha and ERbeta are investigated, demonstrating the importance of long-range interactions in the transmission of information through the ligand binding domain as well as in determining the lig and selectivity of closely related NR receptor sub types.
Investigating Metabotropic Glutamate Receptor 5 Allosteric Modulator Cooperativity, Affinity, and Agonism: Enriching Structure-Function Studies and Structure-Activity Relationships
An operational model of allosterism that allows quantitative estimation of modulator affinity and cooperativity values is validated and can be applied to PAM and NAM potency curves in combination with maximal fold-shift data to derive reliable estimates of modulators affinities.
Discovery and Characterization of Novel Allosteric Potentiators of M1 Muscarinic Receptors Reveals Multiple Modes of Activity
Several novel ligands that potentiated agonist activation of M1 with low micromolar potencies and induced 5-fold or greater leftward shifts of the acetylcholine (ACh) concentration-response curve are identified, suggesting that structurally diverse M1 potentiators may act by distinct mechanisms and differentially regulate receptor coupling to downstream signaling pathways.