Distinct profiles of α7 nAChR positive allosteric modulation revealed by structurally diverse chemotypes
JH Grønlien, M Håkerud, H Ween… - Molecular …, 2007 - ASPET
Selective modulation of α7 nicotinic acetylcholine receptors (nAChRs) is thought to regulate
processes impaired in schizophrenia, Alzheimer's disease, and other dementias. One …
processes impaired in schizophrenia, Alzheimer's disease, and other dementias. One …
An allosteric modulator of the α7 nicotinic acetylcholine receptor possessing cognition-enhancing properties in vivo
DB Timmermann, JH Grønlien, KL Kohlhaas… - … of Pharmacology and …, 2007 - ASPET
Augmentation of nicotinic α7 receptor function is considered to be a potential therapeutic
strategy aimed at ameliorating cognitive and mnemonic dysfunction in relation to debilitating …
strategy aimed at ameliorating cognitive and mnemonic dysfunction in relation to debilitating …
Broad-spectrum efficacy across cognitive domains by α7 nicotinic acetylcholine receptor agonism correlates with activation of ERK1/2 and CREB phosphorylation …
…, JH Gronlien, E Gubbins, J Li, J Malysz… - Journal of …, 2007 - Soc Neuroscience
The α7 nicotinic acetylcholine receptor (nAChR) plays an important role in cognitive processes
and may represent a drug target for treating cognitive deficits in neurodegenerative and …
and may represent a drug target for treating cognitive deficits in neurodegenerative and …
Role of channel activation in cognitive enhancement mediated by α7 nicotinic acetylcholine receptors
CA Briggs, JH Grønlien, P Curzon… - British journal of …, 2009 - Wiley Online Library
Background and purpose: Several agonists of the α7 nicotinic acetylcholine receptor (nAChR)
have been developed for treatment of cognitive deficits. However, agonist efficacy in vivo …
have been developed for treatment of cognitive deficits. However, agonist efficacy in vivo …
In vitro pharmacological characterization of a novel allosteric modulator of α7 neuronal acetylcholine receptor, 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1 …
J Malysz, JH Grønlien, DJ Anderson, M Håkerud… - … of Pharmacology and …, 2009 - ASPET
Targeting α7 neuronal acetylcholine receptors (nAChRs) with selective agonists and positive
allosteric modulators (PAMs) is considered a therapeutic approach for managing cognitive …
allosteric modulators (PAMs) is considered a therapeutic approach for managing cognitive …
Preclinical characterization of A‐582941: A novel α7 neuronal nicotinic receptor agonist with broad spectrum cognition‐enhancing properties
…, RM Fryer, GB Fox, JH Gronlien… - CNS neuroscience & …, 2008 - Wiley Online Library
Among the diverse sets of nicotinic acetylcholine receptors (nAChRs), the α7 subtype is
highly expressed in the hippocampus and cortex and is thought to play important roles in a …
highly expressed in the hippocampus and cortex and is thought to play important roles in a …
Discovery of 4-(5-(4-Chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a Novel Positive Allosteric Modulator of the α7 Nicotinic …
…, JH Gronlien, J Malysz… - Journal of medicinal …, 2009 - ACS Publications
The discovery of a series of pyrrole-sulfonamides as positive allosteric modulators (PAM) of
α7 nAChRs is described. Optimization of this series led to the identification of 19 (A-867744), …
α7 nAChRs is described. Optimization of this series led to the identification of 19 (A-867744), …
Stimulation of dopamine release by nicotinic acetylcholine receptor ligands in rat brain slices correlates with the profile of high, but not low, sensitivity α4β2 subunit …
DJ Anderson, J Malysz, JH Grønlien… - Biochemical …, 2009 - Elsevier
α4β2 neuronal nicotinic receptors (nAChRs) can exist in high and low sensitivity states
possibly due to distinct stoichiometries during subunit assembly: (α4) 2 (β2) 3 pentamer (high …
possibly due to distinct stoichiometries during subunit assembly: (α4) 2 (β2) 3 pentamer (high …
Importance of M2–M3 loop in governing properties of genistein at the α7 nicotinic acetylcholine receptor inferred from α7/5-HT3A chimera
JH Grønlien, H Ween, K Thorin-Hagene… - European journal of …, 2010 - Elsevier
Genistein and 5-hydroxyindole (5-HI) potentiate the α7 nicotinic acetylcholine receptor
current by primarily increasing peak amplitude, a property of type I α7 positive allosteric …
current by primarily increasing peak amplitude, a property of type I α7 positive allosteric …
α3* and α7 nAChR-mediated Ca2+ transient generation in IMR-32 neuroblastoma cells
…, K Thorin-Hagene, E Andersen, JH Grønlien… - Neurochemistry …, 2010 - Elsevier
α3-Containing (α3*) and α7 nicotinic acetylcholine receptors (nAChRs) are expressed in
human IMR-32 neuroblastoma cells and implicated in Ca 2+ signaling. In this study, we …
human IMR-32 neuroblastoma cells and implicated in Ca 2+ signaling. In this study, we …