Stereoselective synthesis of γ-amino acids

M Ordonez, C Cativiela - Tetrahedron: Asymmetry, 2007 - Elsevier
γ-Amino acids have attracted considerable attention as biologically active compounds in the
central nervous system (CNS) of mammals. Over the last few years, significant interest in the …

GABA‐ρ receptors: distinctive functions and molecular pharmacology

MM Naffaa, S Hung, M Chebib… - British Journal of …, 2017 - Wiley Online Library
The homomeric GABA‐ρ ligand‐gated ion channels (also known as GABAC or GABAA‐ρ
receptors) are similar to heteromeric GABAA receptors in structure, function and mechanism …

The enantiomers of syn-2, 3-difluoro-4-aminobutyric acid elicit opposite responses at the GABA C receptor

I Yamamoto, MJT Jordan, N Gavande… - Chemical …, 2012 - pubs.rsc.org
The conformational behaviour and GABA receptor activity of the different stereoisomers of 2,
3-difluoro-4-aminobutyric acid are described. Two enantiomeric GABAC-active ligands are …

Neurochemicals for the Investigation of GABAC Receptors

GAR Johnston, M Chebib, JR Hanrahan… - Neurochemical …, 2010 - Springer
GABA C receptors are being investigated for their role in many aspects of nervous system
function including memory, myopia, pain and sleep. There is evidence for functional GABA C …

Multi-functional diarylurea small molecule inhibitors of TRPV1 with therapeutic potential for neuroinflammation

Z Feng, LV Pearce, Y Zhang, C Xing, BKA Herold… - The AAPS journal, 2016 - Springer
Transient receptor potential vanilloid type 1 (TRPV1), a heat-sensitive calcium channel
protein, contributes to inflammation as well as to acute and persistent pain. Since TRPV1 …

Medicinal Chemistry of ρ GABAC Receptors

CKL Ng, H Kim, N Gavande, I Yamamoto… - Future medicinal …, 2011 - Taylor & Francis
The inhibitory neurotransmitter, GABA, is a low-molecular-weight molecule that can achieve
many low-energy conformations, which are recognized by GABA receptors and transporters …

A Molecular Basis for Agonist and Antagonist Actions at GABAC Receptors

H Abdel‐Halim, JR Hanrahan, DE Hibbs… - Chemical biology & …, 2008 - Wiley Online Library
We modelled the N‐terminal ligand‐binding domain of the ρ1 GABAC receptor based on the
Lymnaea stagnalis acetylcholine‐binding protein (L‐AChBP) crystal structure using …

Scope, limitations and classification of lactamases

Z Assaf, K Faber, M Hall - Journal of Biotechnology, 2016 - Elsevier
The hydrolysis of amide bonds is a ubiquitous process in nature and is catalyzed by various
enzymes: Whereas N-unsubstituted amides are cleaved by amidases (EC 3.5. 1.4) …

Agonist responses of (R)-and (S)-3-fluoro-γ-aminobutyric acids suggest an enantiomeric fold for GABA binding to GABA C receptors

I Yamamoto, GP Deniau, N Gavande… - Chemical …, 2011 - pubs.rsc.org
The enantiomers of 3F-GABA were evaluated on GABAC receptors. Both enantiomers were
agonists, with the (R)-enantiomer being an order of magnitude more potent. This result is …

A conformationally restricted GABA analogue based on octahydro-1H-cyclopenta[b]pyridine scaffold

KP Melnykov, DM Volochnyuk, SV Ryabukhin… - Amino Acids, 2019 - Springer
An approach to rel-(4a S, 6 R, 7a R)-octahydro-1 H-cyclopenta [b] pyridine-6-carboxylic acid—
a bicyclic conformationally restricted γ-aminobutyric acid (GABA) analogue was developed …