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Leveraging Novel Insights into Allosteric Modulator Pharmacology for CNS Disorders

Saturday April 06, 2019

2:00 pm - 4:00 pm

Room W205 A
Sponsored by the Division for Molecular Pharmacology (MP)
Co-sponsored by the Division for Behavioral Pharmacology (BEH)
Co-sponsored by the Division for Drug Discovery and Development (DDD)

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.

Biased Allosteric Agonism and Modulation of Class C G Protein-Coupled Receptors
Karen Gregory - Monash Institute of Pharmaceutical Sciences

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

Shedding Light on Pain Neuromodulation Using Photoswitchable Allosteric Ligands
Cyril Goudet - Institute of Functional Genomics, University of Montpellier

From Cognition to Seizures: Exploring the Therapeutic Potential of Allosteric Modulators of M1 Muscarinic Receptors
Sophie Bradley - University of Glasgow

Comparative Pharmacology and Structure–Activity Relationships of D1 Dopamine Receptor Positive Allosteric Modulators
Kathryn Luderman - NIH/NINDS

Last Updated: August 15, 2019
Key Dates
April 6

ASPET Business Meeting and Awards Presentation

April 6-9

ASPET Annual Meeting at EB 2019

Thank you to our Annual Meeting partners:

University of Florida
Wake Forest University
Washington State University College of Pharmacy and Pharmaceutical Sciences
University of Wisconsin Molecular and Cellular Pharmacology Training Program
UT Health San Antonio
University of Minnesota

Emory University Pharmacology

PR & P
University of Michigan Medical School Pharmacology