Design of 4-Oxo-1-aryl-1,4-dihydroquinoline-3-carboxamides as Selective Negative Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 2
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چکیده
منابع مشابه
A family of highly selective allosteric modulators of the metabotropic glutamate receptor subtype 5.
We have identified a family of highly selective allosteric modulators of the group I metabotropic glutamate receptor subtype 5 (mGluR5). This family of closely related analogs exerts a spectrum of effects, ranging from positive to negative allosteric modulation, and includes compounds that do not themselves modulate mGluR5 agonist activity but rather prevent other family members from exerting t...
متن کاملIterative experimental and virtual high-throughput screening identifies metabotropic glutamate receptor subtype 4 positive allosteric modulators.
Activation of metabotropic glutamate receptor subtype 4 has been shown to be efficacious in rodent models of Parkinson's disease. Artificial neural networks were trained based on a recently reported high throughput screen which identified 434 positive allosteric modulators of metabotropic glutamate receptor subtype 4 out of a set of approximately 155,000 compounds. A jury system containing thre...
متن کاملA novel class of positive allosteric modulators of metabotropic glutamate receptor subtype 1 interact with a site distinct from that of negative allosteric modulators.
We recently reported a novel class of compounds, represented by 3-cyano-N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamide (CD-PPB), that act as positive allosteric modulators (potentiators) of metabotropic glutamate receptor (mGluR) subtype 5. Studies of CDPPB analogs revealed that some compounds in this series serve also as positive allosteric modulators of mGluR1. Although CDPPB is selective for mGlu...
متن کاملNegative Allosteric Modulators of Metabotropic Glutamate Receptors Subtype 5 in Addiction: a Therapeutic Window
BACKGROUND Abundant evidence at the anatomical, electrophysiological, and molecular levels implicates metabotropic glutamate receptor subtype 5 (mGluR5) in addiction. Consistently, the effects of a wide range of doses of different mGluR5 negative allosteric modulators (NAMs) have been tested in various animal models of addiction. Here, these studies were subjected to a systematic review to find...
متن کاملIdentification of Glutathione Conjugates of Acetylene- Containing Positive Allosteric Modulators of Metabotropic Glutamate Receptor Subtype
XIAOLIANG ZHUO, XIAOHUA STELLA HUANG, ANDREW P. DEGNAN, LAWRENCE B. SNYDER, FUKANG YANG, HONG HUANG, YUE-ZHONG SHU, BENJAMIN M. JOHNSON Department of Biotransformation (X.Z., B.M.J.), Discovery Analytical Sciences (X.S.H.), Neuroscience Chemistry (A.P.D., L.B.S., F.Y., H.H.), Bristol-Myers Squibb Co., 5 Research Parkway, Wallingford, CT 06492 Department of Biotransformation (Y.-Z.S.), Bristol-M...
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ژورنال
عنوان ژورنال: Journal of Medicinal Chemistry
سال: 2015
ISSN: 0022-2623,1520-4804
DOI: 10.1021/acs.jmedchem.5b01371