In This Section

Leveraging Novel Insights into Allosteric Modulator Pharmacology for CNS Disorders

Saturday April 06, 2019

2:00 pm - 4:00 pm Eastern Time (ET)

Room W205 A


Chair :

Karen Gregory
Monash Institute of Pharmaceutical Sciences

G protein-coupled receptors (GPCRs) are highly tractable drug targets, however, discovery for CNS disorders suffers from high attrition rates. Allosteric modulators offer the potential to fine-tune GPCR activity when and where the endogenous neurotransmitter is present. This symposium showcases research encompassing the continuum of preclinical GPCR allosteric modulator drug discovery, from molecular pharmacology and chemical biology through to in vivo models of CNS disorders and pain. Speakers will present efforts to harness new paradigms of allosteric drug action (biased signaling and light control) to avoid common pitfalls (selectivity, adverse effect liability) and enhance efficacy.


Karen Gregory - Monash Institute of Pharmaceutical Sciences

Biased Allosteric Agonism and Modulation of Class C G Protein-Coupled Receptors

Jerri Rook - Vanderbilt University

Walking the Line Between Cognition Enhancing Efficacy and Adverse Effect Liability of Muscarinic Acetylcholine Receptor Subtype 1 Positive Allosteric Modulators

Cyril Goudet - Institute of Functional Genomics, University of Montpellier

Shedding Light on Pain Neuromodulation Using Photoswitchable Allosteric Ligands

Sophie Bradley - University of Glasgow

From Cognition to Seizures: Exploring the Therapeutic Potential of Allosteric Modulators of M1 Muscarinic Receptors

Kathryn Luderman - NIH/NINDS

Comparative Pharmacology and Structure–Activity Relationships of D1 Dopamine Receptor Positive Allosteric Modulators

Last Updated: August 15, 2019
Key Dates
April 6

ASPET Business Meeting and Awards Presentation

April 6-9

ASPET Annual Meeting at EB 2019