Charles R. Yang
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View article: Effects of DPTQ, a novel positive allosteric modulator of the dopamine D1 receptor, on spontaneous eye blink rate and spatial working memory in the nonhuman primate
Effects of DPTQ, a novel positive allosteric modulator of the dopamine D1 receptor, on spontaneous eye blink rate and spatial working memory in the nonhuman primate Open
Rationale Dopamine (DA) signaling through the D1 receptor has been shown to be integral to multiple aspects of cognition, including the core process of working memory. The discovery of positive allosteric modulators (PAMs) of the D1 recept…
View article: CCDC 1944255: Experimental Crystal Structure Determination
CCDC 1944255: Experimental Crystal Structure Determination Open
View article: CCDC 1944256: Experimental Crystal Structure Determination
CCDC 1944256: Experimental Crystal Structure Determination Open
View article: CCDC 1944257: Experimental Crystal Structure Determination
CCDC 1944257: Experimental Crystal Structure Determination Open
View article: Synthesis and Pharmacological Characterization of 2-(2,6-Dichlorophenyl)-1-((1<i>S</i>,3<i>R</i>)-5-(3-hydroxy-3-methylbutyl)-3-(hydroxymethyl)-1-methyl-3,4-dihydroisoquinolin-2(1<i>H</i>)-yl)ethan-1-one (LY3154207), a Potent, Subtype Selective, and Orally Available Positive Allosteric Modulator of the Human Dopamine D1 Receptor
Synthesis and Pharmacological Characterization of 2-(2,6-Dichlorophenyl)-1-((1<i>S</i>,3<i>R</i>)-5-(3-hydroxy-3-methylbutyl)-3-(hydroxymethyl)-1-methyl-3,4-dihydroisoquinolin-2(1<i>H</i>)-yl)ethan-1-one (LY3154207), a Potent, Subtype Selective, and Orally Available Positive Allosteric Modulator of the Human Dopamine D1 Receptor Open
Clinical development of catechol-based orthosteric agonists of the dopamine D1 receptor has thus far been unsuccessful due to multiple challenges. To address these issues, we identified LY3154207 (3) as a novel, potent, and subtype selecti…
View article: Front Cover: The Discovery of LML134, a Histamine H3 Receptor Inverse Agonist for the Clinical Treatment of Excessive Sleep Disorders (ChemMedChem 13/2019)
Front Cover: The Discovery of LML134, a Histamine H3 Receptor Inverse Agonist for the Clinical Treatment of Excessive Sleep Disorders (ChemMedChem 13/2019) Open
The Front Cover shows the therapeutic effect of the H3 receptor inverse agonist LML134 (18b), as expected in narcoleptic patients. Compound 18b results from an extensive optimization of safety and pharmacokinetic properties of several chem…
View article: Intracellular Binding Site for a Positive Allosteric Modulator of the Dopamine D1 Receptor
Intracellular Binding Site for a Positive Allosteric Modulator of the Dopamine D1 Receptor Open
The binding site for DETQ [2-(2,6-dichlorophenyl)-1-((1S,3R)-3-(hydroxymethyl)-5-(2-hydroxypropan-2-yl)-1-methyl-3,4-dihydroisoquinolin-2(1H)-yl)ethan-1-one], a positive allosteric modulator (PAM) of the dopamine D1 re…
View article: Preclinical profile of a dopamine D1 potentiator suggests therapeutic utility in neurological and psychiatric disorders
Preclinical profile of a dopamine D1 potentiator suggests therapeutic utility in neurological and psychiatric disorders Open
DETQ, an allosteric potentiator of the dopamine D1 receptor, was tested in therapeutic models that were known to respond to D1 agonists. Because of a species difference in affinity for DETQ, all rodent experiments used transgenic mice expr…
View article: An Allosteric Potentiator of the Dopamine D1 Receptor Increases Locomotor Activity in Human D1 Knock-In Mice without Causing Stereotypy or Tachyphylaxis
An Allosteric Potentiator of the Dopamine D1 Receptor Increases Locomotor Activity in Human D1 Knock-In Mice without Causing Stereotypy or Tachyphylaxis Open