A thieno[2,3-d]pyrimidine scaffold is a novel negative allosteric modulator of the dopamine D2 receptor
Recently, a novel negative allosteric modulator (NAM) of the D 2-like dopamine receptors 1 was identified through virtual ligand screening. This ligand comprises a thieno[2,3-d]pyrimidine scaffold that does not feature in known dopaminergic ligands. Herein, we provide pharmacological validation of a...
| Main Authors: | Fyfe, Tim J., Zarzycka, Barbara, Lim, Herman D., Kellam, Barrie, Mistry, Shailesh N., Katrich, Vsevolod, Scammells, Peter J., Lane, J. Robert, Capuano, Ben |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
American Chemical Society
2018
|
| Online Access: | https://eprints.nottingham.ac.uk/51343/ |
Similar Items
Discovery of a novel class of negative allosteric modulator of the dopamine D2 receptor through fragmentation of a bitopic ligand
by: Mistry, Shailesh N., et al.
Published: (2015)
by: Mistry, Shailesh N., et al.
Published: (2015)
Medicinal Chemistry & Chemical Biology Approaches to Investigate Prospective Treatments for CNS Diseases: Dopamine D1 Receptor Positive Allosteric Modulators, Dopamine D2 Receptor Positive & Negative Allosteric Modulators, Dopamine D2 Receptor-Ligand Kinetics
by: Fyfe, Tim
Published: (2019)
by: Fyfe, Tim
Published: (2019)
Structure–activity study of N-((trans)-4-(2-(7-cyano-3,4-dihydroisoquinolin-2(1H)-yl)ethyl)cyclohexyl)-1H-indole-2-carboxamide (SB269652), a bitopic ligand that acts as a negative allosteric modulator of the dopamine D2 receptor
by: Shonberg, Jeremy, et al.
Published: (2015)
by: Shonberg, Jeremy, et al.
Published: (2015)
Novel fused arylpyrimidinone based allosteric modulators of the M1 muscarinic acetylcholine receptor
by: Mistry, Shailesh N., et al.
Published: (2016)
by: Mistry, Shailesh N., et al.
Published: (2016)
4-Phenylpyridin-2-one derivatives: a novel class of positive allosteric modulator of the M1 muscarinic acetylcholine receptor
by: Mistry, Shailesh N., et al.
Published: (2015)
by: Mistry, Shailesh N., et al.
Published: (2015)
Synthesis and pharmacological profiling of analogues of benzyl quinolone carboxylic acid (BQCA) as allosteric modulators of the M1 muscarinic receptor
by: Mistry, Shailesh N., et al.
Published: (2013)
by: Mistry, Shailesh N., et al.
Published: (2013)
Mechanistic insights into allosteric structure-function relationships at the M1 muscarinic acetylcholine receptor
by: Abdul-Ridha, Alaa, et al.
Published: (2014)
by: Abdul-Ridha, Alaa, et al.
Published: (2014)
Extrapyramidal side effects of antipsychotics are linked to their association kinetics at dopamine D2 receptors
by: Sykes, David A., et al.
Published: (2017)
by: Sykes, David A., et al.
Published: (2017)
The dopamine D3-preferring D2/D3 dopamine receptor partial agonist, cariprazine, reverses behavioral changes in a rat neurodevelopmental model for schizophrenia
by: Watson, David J.G., et al.
Published: (2016)
by: Watson, David J.G., et al.
Published: (2016)
Assessment of the molecular mechanisms of action of novel 4-phenylpyridine-2-one and 6-phenylpyrimidin-4-one allosteric modulators at the M1 muscarinic acetylcholine receptors
by: van der Westhuizen, Emma T., et al.
Published: (2018)
by: van der Westhuizen, Emma T., et al.
Published: (2018)
D-amphetamine and antipsychotic drug effects on latent
inhibition in mice lacking dopamine D2 receptors
by: Bay-Richter, C., et al.
Published: (2013)
by: Bay-Richter, C., et al.
Published: (2013)
Determination of agonist intrinsic efficacies at the dopamine D2 receptor
by: Stott, Lisa Alice
Published: (2017)
by: Stott, Lisa Alice
Published: (2017)
Kinetic studies of dopamine D2 receptor molecular pharmacology
by: Keen, Alastair C.
Published: (2021)
by: Keen, Alastair C.
Published: (2021)
Biased allosteric modulation at the CaS receptor engendered by structurally diverse calcimimetics
by: Cook, A.E., et al.
Published: (2014)
by: Cook, A.E., et al.
Published: (2014)
4-Hydrazino-1-methylpyrazolo[3,4-d]pyrimidine.
by: Dolzhenko, Anton, et al.
Published: (2009)
by: Dolzhenko, Anton, et al.
Published: (2009)
Molecular determinants of allosteric modulation at the M1 muscarinic acetylcholine receptor
by: Abdul-Ridha, Alaa, et al.
Published: (2014)
by: Abdul-Ridha, Alaa, et al.
Published: (2014)
Allosteric interactions at adenosine A1 and A3 receptors: new insights into the role of small molecules and receptor dimerization
by: Hill, Stephen J., et al.
Published: (2014)
by: Hill, Stephen J., et al.
Published: (2014)
Dopamine D1 receptor involvement in latent inhibition and overshadowing
by: Nelson, Andrew J.D., et al.
Published: (2012)
by: Nelson, Andrew J.D., et al.
Published: (2012)
Positive allosteric modulation of the muscarinic M1 receptor improves efficacy of antipsychotics in mouse glutamatergic deficit models of behavior
by: Choy, Kwok H.C., et al.
Published: (2016)
by: Choy, Kwok H.C., et al.
Published: (2016)
Discovery Of New Potential Pyrido[2,3-D]Pyrimidin-7-One Based Cdk4 Inhibitors Using Molecular Modelling Approaches
by: Al Attraqchi, Omar Husham Ahmed
Published: (2023)
by: Al Attraqchi, Omar Husham Ahmed
Published: (2023)
Two conformational polymorphs of a bioactive pyrazolo[3,4-d]pyrimidine
by: Tan, Sang Loon *, et al.
Published: (2023)
by: Tan, Sang Loon *, et al.
Published: (2023)
Thermoanalytical behaviour of 2-amino- and 2-oxo-Substituted Pyrimidines
by: Shah, S. W., et al.
Published: (2001)
by: Shah, S. W., et al.
Published: (2001)
Kinetic analysis of antagonist-occupied adenosine-A3 receptors within membrane microdomains of individual cells provides evidence of receptor dimerization and allosterism
by: Corriden, Ross, et al.
Published: (2014)
by: Corriden, Ross, et al.
Published: (2014)
The role of dopamine D2 and neuregulin-1 receptors in schizophrenia relevant phenotypes of cognition, attention and memory
by: Mathur, Naina
Published: (2012)
by: Mathur, Naina
Published: (2012)
Corticosterone and dopamine D2/D3 receptors mediate the
motivation for voluntary wheel running in C57BL/6J mice
by: Ebada, Mohamed Elsaed Elsayed, et al.
Published: (2016)
by: Ebada, Mohamed Elsaed Elsayed, et al.
Published: (2016)
Effects of dopamine D1 modulation of the anterior cingulate cortex in a fear conditioning procedure
by: Pezze, Marie A., et al.
Published: (2015)
by: Pezze, Marie A., et al.
Published: (2015)
Photosensitized dimerization in pyrimidine-based thin solid films
by: Patra, A., et al.
Published: (2011)
by: Patra, A., et al.
Published: (2011)
Water solubility enhancement of pyrazolo[3,4-d]pyrimidine derivatives via miniaturized polymer-drug microarrays
by: Sanna, Monica, et al.
Published: (2018)
by: Sanna, Monica, et al.
Published: (2018)
Controlled dopamine (D1) receptor stimulation using photo-responsive substrates
by: Rajput, Sunil
Published: (2019)
by: Rajput, Sunil
Published: (2019)
Dopamine 2 Receptor Genes Are Associated with Raised Blood Glucose in Schizophrenia
by: Lawford, B., et al.
Published: (2016)
by: Lawford, B., et al.
Published: (2016)
Three-component microwave-assisted synthesis of 3,5-disubstituted pyrazolo[3,4-d]pyrimidin-4-ones
by: Ng, Jia Hui, et al.
Published: (2022)
by: Ng, Jia Hui, et al.
Published: (2022)
Potentiation of latent inhibition by haloperidol and clozapine is attenuated in Dopamine D2 receptor (Drd-2) deficient mice: Do antipsychotics influence learning to ignore irrelevant stimuli via both Drd-2 and non-Drd-2 mechanisms?
by: O'Callaghan, M.J., et al.
Published: (2014)
by: O'Callaghan, M.J., et al.
Published: (2014)
Dopamine D1 receptor stimulation modulates the formation and retrieval of novel object recognition memory: role of the prelimbic cortex
by: Pezze, Marie A., et al.
Published: (2015)
by: Pezze, Marie A., et al.
Published: (2015)
Investigations into β2-adrenoceptor pharmacology: kinetic analysis, mechanotransduction and allosteric modulation
by: Cullum, Sean A.
Published: (2024)
by: Cullum, Sean A.
Published: (2024)
Photochemistry of 3H-furo[3,4-c]pyrazoles and 3H-thieno[3,4-c] pyrazoles
by: Payne, Alan
Published: (2013)
by: Payne, Alan
Published: (2013)
3,4-Diaminopyrazolo[3,4-d]pyrimidines: a new three-component microwave-assisted synthesis and anti-leukemic properties
by: Ng, Jia Hui, et al.
Published: (2023)
by: Ng, Jia Hui, et al.
Published: (2023)
Dopamine D1-like receptor signalling in the hippocampus and amygdala modulates the acquisition of contextual fear conditioning
by: Heath, Florence C., et al.
Published: (2015)
by: Heath, Florence C., et al.
Published: (2015)
5-Propyl-6-(p-tolylsulfanyl)pyrimidine-2,4(1H,3H)-dione
by: A. M. Al-Omary, Fatmah, et al.
Published: (2014)
by: A. M. Al-Omary, Fatmah, et al.
Published: (2014)
Design, Synthesis, and Development of Novel Intracellular Allosteric Modulators of CXC Chemokine Receptor 1 and 2
by: Francis, Rhys
Published: (2024)
by: Francis, Rhys
Published: (2024)
Design, Synthesis, and Development of Novel Fluorescently Labelled Allosteric Probes for the Human Beta2-Adrenoceptor
by: Tuzer, Cemre
Published: (2023)
by: Tuzer, Cemre
Published: (2023)
Similar Items
-
Discovery of a novel class of negative allosteric modulator of the dopamine D2 receptor through fragmentation of a bitopic ligand
by: Mistry, Shailesh N., et al.
Published: (2015) -
Medicinal Chemistry & Chemical Biology Approaches to Investigate Prospective Treatments for CNS Diseases: Dopamine D1 Receptor Positive Allosteric Modulators, Dopamine D2 Receptor Positive & Negative Allosteric Modulators, Dopamine D2 Receptor-Ligand Kinetics
by: Fyfe, Tim
Published: (2019) -
Structure–activity study of N-((trans)-4-(2-(7-cyano-3,4-dihydroisoquinolin-2(1H)-yl)ethyl)cyclohexyl)-1H-indole-2-carboxamide (SB269652), a bitopic ligand that acts as a negative allosteric modulator of the dopamine D2 receptor
by: Shonberg, Jeremy, et al.
Published: (2015) -
Novel fused arylpyrimidinone based allosteric modulators of the M1 muscarinic acetylcholine receptor
by: Mistry, Shailesh N., et al.
Published: (2016) -
4-Phenylpyridin-2-one derivatives: a novel class of positive allosteric modulator of the M1 muscarinic acetylcholine receptor
by: Mistry, Shailesh N., et al.
Published: (2015)