Design and Discovery of 6-[(3S,4S)-4-Methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one …
…, CJ Schmidt, M Vanase-Frawley… - Journal of medicinal …, 2012 - ACS Publications
6-[(3S,4S)-4-Methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one
(PF-04447943) is a novel PDE9A inhibitor …
(PF-04447943) is a novel PDE9A inhibitor …
[PDF][PDF] Biallelic mutations in PDE10A lead to loss of striatal PDE10A and a hyperkinetic movement disorder with onset in infancy
…, V Reinhart, LC James, MA Vanase-Frawley… - The American Journal of …, 2016 - cell.com
Deficits in the basal ganglia pathways modulating cortical motor activity underlie both
Parkinson disease (PD) and Huntington disease (HD). Phosphodiesterase 10A (PDE10A) is …
Parkinson disease (PD) and Huntington disease (HD). Phosphodiesterase 10A (PDE10A) is …
Phosphodiesterase 9A regulates central cGMP and modulates responses to cholinergic and monoaminergic perturbation in vivo
…, DT Stephenson, FD Tingley, M Vanase-Frawley… - … of Pharmacology and …, 2012 - ASPET
Cyclic nucleotides are critical regulators of synaptic plasticity and participate in requisite
signaling cascades implicated across multiple neurotransmitter systems. Phosphodiesterase 9A …
signaling cascades implicated across multiple neurotransmitter systems. Phosphodiesterase 9A …
[HTML][HTML] Dopamine D3 receptor antagonist reveals a cryptic pocket in aminergic GPCRs
The recent increase in the number of X-ray crystal structures of G-protein coupled receptors (GPCRs)
has been enabling for structure-based drug design (SBDD) efforts. These …
has been enabling for structure-based drug design (SBDD) efforts. These …
Pharmacological characterization of 2-methyl-N-((2′-(pyrrolidin-1-ylsulfonyl) biphenyl-4-yl) methyl) propan-1-amine (PF-04455242), a high-affinity antagonist …
…, Y Lu, AW Schmidt, MA Vanase-Frawley… - … of Pharmacology and …, 2011 - ASPET
… Lu, AW Schmidt, MA Vanase-Frawley, A. Sawant-Basak, E. Miller, S. … Participated in
research design: Grimwood, Lu, Schmidt, Vanase-Frawley, Sawant-Basak, McLean, Wong, …
research design: Grimwood, Lu, Schmidt, Vanase-Frawley, Sawant-Basak, McLean, Wong, …
The 5-hydroxytryptamine4 receptor agonists prucalopride and PRX-03140 increase acetylcholine and histamine levels in the rat prefrontal cortex and the power of …
…, E Tseng, LL McDowell, MA Vanase-Frawley… - … of Pharmacology and …, 2012 - ASPET
5-Hydroxytryptamine (5-HT) 4 receptor agonists reportedly stimulate brain acetylcholine (ACh)
release, a property that might provide a new pharmacological approach for treating …
release, a property that might provide a new pharmacological approach for treating …
Application of structure-based drug design and parallel chemistry to identify selective, brain penetrant, in vivo active phosphodiesterase 9A inhibitors
…, S Lui, RJ Kleiman, M Vanase-Frawley… - Journal of medicinal …, 2012 - ACS Publications
Phosphodiesterase 9A inhibitors have shown activity in preclinical models of cognition with
potential application as novel therapies for treating Alzheimer’s disease. Our clinical …
potential application as novel therapies for treating Alzheimer’s disease. Our clinical …
Identification of a brain penetrant PDE9A inhibitor utilizing prospective design and chemical enablement as a rapid lead optimization strategy
…, CJ Schmidt, M Vanase-Frawley… - Journal of medicinal …, 2009 - ACS Publications
… Michelle Vanase-Frawley … Schmidt, Michelle Vanase-Frawley, and Spiros Liras .
Design and Discovery of 6-[(3S,4S)-4-Methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one …
Design and Discovery of 6-[(3S,4S)-4-Methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one …
Design and Discovery of a Selective Small Molecule κ Opioid Antagonist (2-Methyl-N-((2′-(pyrrolidin-1-ylsulfonyl)biphenyl-4-yl)methyl)propan-1-amine, PF-4455242 …
…, AW Schmidt, M Vanase-Frawley… - Journal of medicinal …, 2011 - ACS Publications
By use of parallel chemistry coupled with physicochemical property design, a series of selective
κ opioid antagonists have been discovered. The parallel chemistry strategy utilized key …
κ opioid antagonists have been discovered. The parallel chemistry strategy utilized key …
Identification of Multiple 5-HT4 Partial Agonist Clinical Candidates for the Treatment of Alzheimer's Disease
…, DM Rubitski, MA Vanase-Frawley… - Journal of medicinal …, 2012 - ACS Publications
The cognitive impairments observed in Alzheimer’s disease (AD) are in part a consequence
of reduced acetylcholine (ACh) levels resulting from a loss of cholinergic neurons. …
of reduced acetylcholine (ACh) levels resulting from a loss of cholinergic neurons. …