Related Experiment Video

Updated: May 7, 2026

Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission
07:16

Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission

Published on: August 16, 2018

Development of allosteric modulators of GPCRs for treatment of CNS disorders

Hilary Highfield Nickols1, P Jeffrey Conn

  • 1Division of Neuropathology, Department of Pathology, Microbiology and Immunology, Vanderbilt University, USA.

Neurobiology of Disease
|October 1, 2013
PubMed

Keywords:
(+)-6-(2,4-dimethylphenyl)-2-ethyl-6,7-dihydrobenzo[d]oxazol-4(5H)-one(1-(4-cyano-4-(pyridine-2-yl)piperidine-1-yl)methyl-4-oxo-4H-quinolizine-3-carboxylic acid)(1S,2S)-N(1)-(3,4-dichlorophenyl)cyclohexane-1,2-dicarboxamide(1S,3R,4S)-1-aminocyclo-pentane-1,3,4-tricarboxylic acid(3,4-dihydro-2H-pyrano[2,3]b quinolin-7-yl)(cis-4-methoxycyclohexyl) methanone(3aS,5S,7aR)-methyl 5-hydroxy-5-(m-tolylethynyl)octahydro-1H-indole-1-carboxylate1-(1′-(2-methylbenzyl)-1,4′-bipiperidin-4-yl)-1H-benzo[d]imidazol-2(3H)-one1-[3-(4-butyl-1-piperidinyl)propyl]-3,4-dihydro-2(1H)-quinolinone1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine2-(2-(3-methoxyphenyl)ethynyl)-5-methylpyridine2-chloro-4-((2,5-dimethyl-1-(4-(trifluoromethoxy)phenyl)-1Himidazol-4-yl)ethynyl)pyridine2-methyl-6-(2-phenylethenyl)pyridine2-methyl-6-(phenylethynyl)-pyridine3-cyano-N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamide3-cyclohexyl-5-fluoro-6-methyl-7-(2-morpholin-4-ylethoxy)-4H-chromen-4-one3[(2-methyl-1,3-thiazol-4-yl)ethylnyl]pyridine4-((E)-styryl)-pyrimidin-2-ylamine4-[1-(2-fluoropyridin-3-yl)-5-methyl-1H-1,2,3-triazol-4-yl]-N-isopropyl-N-methyl-3,6-dihydropyridine-1(2H)-carboxamide4-n-butyl-1-[4-(2-methylphenyl)-4-oxo-1-butyl]-piperidine5-methyl-6-(phenylethynyl)-pyridine5MPEP6-(4-methoxyphenyl)-5-methyl-3-(4-pyridinyl)-isoxazolo[4,5-c]pyridin-4(5H)-one6-OHDA6-hydroxydopamine6-methyl-2-(phenylazo)-3-pyridinol77-LH-28-17TMRAC-42ACPT-1AChEADADX71743AFQ056APPAllosteric modulatorAlzheimer's diseaseBINABQCACDPPBCFMMCCNSCPPHACTEPDADFBDHPGDrug discoveryERK1/2FMRPFTIDCFXSFragile X syndromeGABAGPCRJNJ16259685L-AP4L-DOPALu AF21934Lu AF32615M-5MPEPMMPIPMPEPMPTPMTEPMetabotropic glutamate receptorMuscarinic acetylcholine receptorN-[4-chloro-2[(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl]phenyl]-2-hydrobenzamideN-methyl-d-aspartateN-phenyl-7-(hydroxylimino)cyclopropa[b]chromen-1a-carboxamideNAMNMDAPAMPCPPDPD-LIDPETPHCCCPQCAParkinson's diseaseParkinson's disease levodopa-induced dyskinesiaSAMSIB-1757SIB-1893TBPB[(3-fluorophenyl)methylene]hydrazone-3-fluorobenzaldehydeacetylcholinesteraseamyloid precursor proteinbenzylquinolone carboxylic acidcentral nervous systemdihydroxyphenylglycinedopamineextracellular signal-regulated kinase 1/2fragile X mental retardation proteinl-(+)-2-amino-4-phosphonobutyric acidl-3,4-dihydroxyphenylalaninemGlumetabotropic glutamate receptornegative allosteric modulatorphencyclidinepositive allosteric modulatorpositron emission tomographypotassium 30-([(2-cyclopentyl-6-7-dimethyl-1-oxo-2,3-dihydro-1H-inden-5yl)oxy]methyl)biphenyl l-4-carboxylateseven transmembrane receptorsilent allosteric modulatorγ-aminobutyric acid

More Related Videos

A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators07:41

A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators

Published on: February 20, 2018

Monitoring GPCR-β-arrestin1/2 Interactions in Real Time Living Systems to Accelerate Drug Discovery08:21

Monitoring GPCR-β-arrestin1/2 Interactions in Real Time Living Systems to Accelerate Drug Discovery

Published on: June 28, 2019

Related Concept Videos

G Protein-coupled Receptors01:15

G Protein-coupled Receptors

G Protein-Coupled Receptors or GPCRs are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to sensory stimuli such as light, odors, hormones, cytokines, or neurotransmitters.
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
G Protein-coupled Receptors01:15

G Protein-coupled Receptors

G Protein-Coupled Receptors or GPCRs are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to sensory stimuli such as light, odors, hormones, cytokines, or neurotransmitters.
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
Ligand-Gated Ion Channel Receptor: Gating Mechanism01:30

Ligand-Gated Ion Channel Receptor: Gating Mechanism

Ligand-gated ion channels are transmembrane proteins that play a vital role in intercellular communication and functions of the nervous system. They allow the influx of ions across the membrane once the neurotransmitter binds, allowing the subsequent transmission of electrical excitation across the neurons. Other ligand-gated ion channels, like the γ-aminobutyric acid (GABA) receptor, permit anions like chloride into the cells on the binding of the GABA molecule. Their entry into the cell...
GPCRs Regulate Adenylyl Cylase Activity01:09

GPCRs Regulate Adenylyl Cylase Activity

Some GPCRs transmit signals through adenylyl cyclase (AC), a transmembrane enzyme. AC helps synthesize second messenger cyclic adenosine monophosphate (cAMP). AC catalyzes cyclization reaction and converts ATP to cAMP by releasing a pyrophosphate. The pyrophosphate is further hydrolyzed to phosphate by the enzyme pyrophosphatase, which drives cAMP synthesis to completion. However, cAMP is rapidly degraded to 5′ AMP by the enzymes phosphodiesterase (PDE), preventing overstimulation of cells.
Two...
Transducer Mechanism: G Protein–Coupled Receptors01:30

Transducer Mechanism: G Protein–Coupled Receptors

G Protein–Coupled Receptors (GPCRs) are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to various stimuli. GPCRs regulate critical physiological pathways and are excellent drug targets for treating diseases such as diabetes, cancer, obesity, depression, or Alzheimer's. Nearly 35% of approved drugs implement their therapeutic effects by selectively interacting with specific GPCRs.
GPCRs are also called heptahelical, 7TM, or...
Pharmacogenomics: Identification of New Drug Targets01:29

Pharmacogenomics: Identification of New Drug Targets

Advances in genomics have profoundly influenced drug discovery by increasing both the speed and accuracy of pharmaceutical development. Pharmacogenomics, which examines how genetic variation influences drug response, facilitates the identification of novel therapeutic targets and enables patient stratification for personalized treatment. These strategies contribute to improved drug efficacy, minimized adverse effects, and more efficient clinical trial design.Mapping genetic differences...