Agonists of the γ-aminobutyric acid type B (GABAB) receptor derived from β-hydroxy and β-amino difluoromethyl ketones
نویسندگان
چکیده
منابع مشابه
Activation of the γ-Aminobutyric Acid Type B (GABA(B)) Receptor by Agonists and Positive Allosteric Modulators.
Since the discovery of the GABA(B) agonist and muscle relaxant baclofen, there have been substantial advancements in the development of compounds that activate the GABA(B) receptor as agonists or positive allosteric modulators. For the agonists, most of the existing structure-activity data apply to understanding the role of substituents on the backbone of GABA as well as replacing the carboxyli...
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چکیده ندارد.
Spinally mediated analgesic interaction between γ-aminobutyric acid B receptor agonist and glutamate receptor antagonists in rats
Background. Many mechanisms are involved in pain transmission in the spinal cord. Therefore, combination of drugs acting on different kinds of mechanisms might be useful for analgesia. We investigated the interaction betweenγ-aminobutyric acid （GABA）B receptor agonist, baclofen, and N-methyl-D-aspartate （NMDA） receptor antagonist, AP-5, orα-amino-3-hydroxy-5-methylisoxazole-4-propionic acid ...
متن کاملEfficient synthesis of β’-amino-α,β-unsaturated ketones
A general and simple procedure to access chiral β'-amino-α,β-enones, in seven steps, from an α,β unsaturated ester has been described. The use of a Horner-Wadsworth-Emmons reaction as a key step for generating the β'-amino-α,β-enones, permits access to a range of substrates under mild conditions and in moderate to high yield.
متن کاملP145: The Role of γ-Aminobutyric Acid Receptor in The Social Anxiety Disorder
Social anxiety disorder (SAD) is the one of the most common anxiety disorders. Despite its high prevalence, the disorder is still considerably undiagnosed and untreated. The disease places a massive burden on patient’s lives, affecting not only their social interactions but also their educational and professional activities, thereby constituting a severe disability. γ-aminobutyric acid (GABA) s...
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ژورنال
عنوان ژورنال: Bioorganic & Medicinal Chemistry Letters
سال: 2018
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2018.04.003