Bioisosteric determinants for subtype selectivity of ligands for heteromeric GABAA receptors

Bioorganic & Medicinal Chemistry Letters
2001.0

Abstract

The potency and efficacy of a series of bioisosterically modified GABA analogues were determined electrophysiologically using heteromeric GABA(A) receptors expressed in Xenopus oocytes. These agonist parameters were shown to be strongly dependent on the receptor subunit combination. On the other hand, the antagonist potencies of the classical GABA(A) antagonists SR 95531 (7) and BMC (8) and also of 5g and the phosphinic acid bioisosteres of 5a, compounds 5f and 6, were essentially independent of the receptor subunit combinations.

Knowledge Graph

Similar Paper

Bioisosteric determinants for subtype selectivity of ligands for heteromeric GABAA receptors
Bioorganic & Medicinal Chemistry Letters 2001.0
Five-Membered N-Heterocyclic Scaffolds as Novel Amino Bioisosteres at γ-Aminobutyric Acid (GABA) Type A Receptors and GABA Transporters
Journal of Medicinal Chemistry 2019.0
Use of bicuculline, a GABA antagonist, as a template for the development of a new class of ligands showing positive allosteric modulation of the GABAA receptor
Bioorganic & Medicinal Chemistry Letters 2000.0
Hydroxy-1,2,5-oxadiazolyl Moiety as Bioisoster of the Carboxy Function. Synthesis, Ionization Constants, and Pharmacological Characterization of γ-Aminobutyric Acid (GABA) Related Compounds
Journal of Medicinal Chemistry 2006.0
Structure and molecular modeling of GABAA receptor antagonists
Journal of Medicinal Chemistry 1992.0
Novel γ-Aminobutyric Acid ρ<sub>1</sub>Receptor Antagonists; Synthesis, Pharmacological Activity and Structure−Activity Relationships
Journal of Medicinal Chemistry 2008.0
Synthesis and Biological Evaluation of 4-(Aminomethyl)-1-hydroxypyrazole Analogues of Muscimol as γ-Aminobutyric Acid<sub>A</sub> Receptor Agonists
Journal of Medicinal Chemistry 2013.0
5-Substituted Imidazole-4-acetic Acid Analogues:  Synthesis, Modeling, and Pharmacological Characterization of a Series of Novel γ-Aminobutyric Acid<sub>C</sub>Receptor Agonists
Journal of Medicinal Chemistry 2007.0
Biological activity of 3-aminopropyl (methyl) phosphinic acid, a potent and selective GABAB agonist with CNS activity
Bioorganic &amp; Medicinal Chemistry Letters 1993.0
A Novel Class of Potent 3-Isoxazolol GABA<sub>A</sub>Antagonists:  Design, Synthesis, and Pharmacology
Journal of Medicinal Chemistry 2000.0