Possible role of valvular serotonin 5-HT2B receptors in the cardiopathy associated with fenfluramine

…, PR Hartig, GF Hollis, PC Meunier, AJ Robichaud… - Molecular …, 2000 - ASPET
Dexfenfluramine was approved in the United States for long-term use as an appetite suppressant
until it was reported to be associated with valvular heart disease. The valvular changes …

The major brain cholesterol metabolite 24 (S)-hydroxycholesterol is a potent allosteric modulator of N-methyl-D-aspartate receptors

SM Paul, JJ Doherty, AJ Robichaud… - Journal of …, 2013 - Soc Neuroscience
N-methyl-d-aspartate receptors (NMDARs) are glutamate-gated ion channels that are critical
to the regulation of excitatory synaptic function in the CNS. NMDARs govern experience-…

Design and synthesis of 5, 5′-disubstituted aminohydantoins as potent and selective human β-secretase (BACE1) inhibitors

…, RL Magolda, M Pangalos, AJ Robichaud - Journal of medicinal …, 2010 - ACS Publications
The identification of small molecule aminohydantoins as potent and selective human β-secretase
inhibitors is reported. These analogues exhibit low nannomolar potency for BACE1, …

Aminoimidazoles as potent and selective human β-secretase (BACE1) inhibitors

…, K Fan, A Olland, J Bard, AJ Robichaud - Journal of medicinal …, 2009 - ACS Publications
The identification of small molecule aminoimidazoles as potent and selective human β-secretase
inhibitors is reported. These analogues demonstrate low nannomolar potency for …

[HTML][HTML] Preclinical characterization of zuranolone (SAGE-217), a selective neuroactive steroid GABAA receptor positive allosteric modulator

…, E Hoffmann, RS Hammond, AJ Robichaud… - …, 2020 - Elsevier
Zuranolone (SAGE-217) is a novel, synthetic, clinical stage neuroactive steroid GABA A
receptor positive allosteric modulator designed with the pharmacokinetic properties to support …

Use of aza-Cope rearrangement-Mannich cyclization reactions to achieve a general entry to Melodinus and Aspidosperma alkaloids. Stereocontrolled total syntheses …

…, GM Robertson, AJ Robichaud - Journal of the American …, 1991 - ACS Publications
Conclusions The use of hydrogen bond interactions to direct selective mo-lecular recognition
processes of acyclic imides has been demonstrated by studying their cocrystallization …

Discovery of a tetracyclic quinoxaline derivative as a potent and orally active multifunctional drug candidate for the treatment of neuropsychiatric and neurological …

…, AJ Robichaud, T Lee, J Tomesch… - Journal of Medicinal …, 2014 - ACS Publications
We report the synthesis and structure–activity relationships of a class of tetracyclic butyrophenones
that exhibit potent binding affinities to serotonin 5-HT 2A and dopamine D 2 receptors…

Neuroactive Steroids. 2. 3α-Hydroxy-3β-methyl-21-(4-cyano-1H-pyrazol-1′-yl)-19-nor-5β-pregnan-20-one (SAGE-217): A Clinical Next Generation Neuroactive Steroid Positive …

…, E Hoffmann, JJ Doherty, AJ Robichaud - Journal of Medicinal …, 2017 - ACS Publications
Certain classes of neuroactive steroids (NASs) are positive allosteric modulators (PAM) of
synaptic and extrasynaptic GABA A receptors. Herein, we report new SAR insights in a series …

SAGE-718: A First-in-Class N-Methyl-d-Aspartate Receptor Positive Allosteric Modulator for the Potential Treatment of Cognitive Impairment

…, M Lewis, MC Quirk, AJ Robichaud - Journal of medicinal …, 2022 - ACS Publications
N-Methyl-d-aspartate receptor (NMDAR) positive allosteric modulators (PAMs) have received
increased interest as a powerful mechanism of action to provide relief as therapies for CNS …

Rearrangement of 3, 3-disubstituted indolenines and synthesis of 2, 3-substituted indoles

KG Liu, AJ Robichaud, JR Lo, JF Mattes, Y Cai - Organic Letters, 2006 - ACS Publications
Robichaud. One-pot synthesis of highly substituted indolines. Tetrahedron 2010, 66 (3) ,
573-577. … Schechter, Albert J. Robichaud. A regiospecific synthesis of a series of 1-sulfonyl …