P-21 Design and Synthesis of a Novel Isoxazoline as a Potential PAM-Agonist
Abstract
Progression of Alzheimer’s disease is associated with a loss of M1 receptor activation in the brain. However, a lack of clinical success following attempts to activate the M1 receptor at the orthosteric site has contributed to a transition towards the allosteric pocket of the receptor. Here, positive allosteric modulators (PAMs) interact to potentiate the acetylcholine response. Recent research proposes that optimization of PAM activity at the expense of intrinsic agonism may posit a means to limit adverse side effects. Therefore, this project proposes a design and synthesis of a novel isoxazoline as a potent PAM agent with weak intrinsic agonism.
Location
Buller Hall Lobby
Start Date
3-8-2019 2:30 PM
P-21 Design and Synthesis of a Novel Isoxazoline as a Potential PAM-Agonist
Buller Hall Lobby
Progression of Alzheimer’s disease is associated with a loss of M1 receptor activation in the brain. However, a lack of clinical success following attempts to activate the M1 receptor at the orthosteric site has contributed to a transition towards the allosteric pocket of the receptor. Here, positive allosteric modulators (PAMs) interact to potentiate the acetylcholine response. Recent research proposes that optimization of PAM activity at the expense of intrinsic agonism may posit a means to limit adverse side effects. Therefore, this project proposes a design and synthesis of a novel isoxazoline as a potent PAM agent with weak intrinsic agonism.
Acknowledgments
Supervising Professor: Dr. Lisa Ahlberg