Results 301 to 310 of about 195,829 (332)

Transcranial Direct Current Stimulation of the Temporoparietal Junction in Autism Spectrum Disorder: Results of a Phase‐IIa Randomized, Double‐Blind, Sham‐Controlled Feasibility Study

Autism Research, EarlyView.
ABSTRACT Activation of the temporoparietal junction (TPJ) is reduced in autism spectrum disorder (ASD) during social cognitive tasks. Therefore, anodal transcranial direct current stimulation (tDCS) of the TPJ may enhance social cognitive abilities in autistic individuals. In a multicenter, randomized, sham‐controlled, double‐blind parallel‐group Phase‐
Christina Luckhardt, Magdalena Schütz, Andreas M. Mühlherr, Sara Boxhoorn, Christine Ecker, Hanna Mössinger, Julia Siemann, Fabienne Schlechter, Miguel Castelo‐Branco, Helena C. Pereira, Marianne Latinus, Camille Ricou, Frederique Bonnet‐Brilhault, Ricardo Salvador, Giulio Ruffini, Rafal Nowak, Michael Siniatchkin, Astrid Dempfle, Christine M. Freitag   +18 more
wiley   +1 more source

A Frank Assessment of SHANK: Impacts of Pathogenic Variations in SHANK3 on Preclinical Models of Phelan McDermid Syndrome

Autism Research, EarlyView.
ABSTRACT Although there are as many as 40 preclinical models of the neurodevelopmental disorder Phelan McDermid syndrome (PMS, or 22q13.3 deletion syndrome), detailed phenotypic analyses to compare the effects of different pathogenic variants and inform treatment design are lacking.
Vic Lin, Samantha M. Matta, Julia E. Dallman, Suzanne Hosie, Manon Moreau, Ashley E. Franks, Thomas Bourgeron, Elisa L. Hill‐Yardin   +7 more
wiley   +1 more source

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Specific GABA_A agonists and partial agonists

The Chemical Record, 2002
AbstractThe GABAA receptor system is implicated in a number of neurological and psychiatric diseases, making GABAA receptor ligands interesting as potential therapeutic agents. Only a few different classes of structures are currently known as ligands for the GABA recognition site on the hetero‐pentameric GABAA receptor complex, reflecting the very ...
Krogsgaard-Larsen, Povl, Frølund, Bente, Liljefors, Tommy   +2 more
openaire   +4 more sources

Partial agonists and acetylcholine liberation

European Journal of Pharmacology, 1970
Abstract The effects of cooling, tetrodotoxin, cocaine, atropine, dibenamine and of a mixture of tetrodotoxin, cocaine and hexamethonium on the actions of cholinesters, alkyltrimethylammonium salts and dimethylaminoethanol derivatives were tested on the guinea pig small intestine.
Keijiro Takagi, Fukutaro Taga, Issei Takayanagi   +2 more
openaire   +3 more sources

Partial agonists go molecular

Trends in Pharmacological Sciences, 2021
Single-channel analysis previously revealed a key role for a short-lived 'flipped' state during glycine receptor activation by partial agonists. Structures solved by Yu and colleagues now reveal a surprising mechanism involving a partially activated agonist-bound closed state that is too long-lived to be considered the flipped state.
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Design of a partial PPARδ agonist

Bioorganic & Medicinal Chemistry Letters, 2007
Structure based ligand design was used in order to design a partial agonist for the PPARdelta receptor. The maximum activation in the transactivation assay was reduced from 87% to 39%. The crystal structure of the ligand binding domain of the PPARdelta receptor in complex with compound 2 was determined in order to understand the structural changes ...
Miroslav Havranek, Marek Korínek, John Patrick Mogensen, Søren Ebdrup, Ingrid Pettersson, Eva Johansson, Pavel Pihera, Claus Bekker Jeppesen, Per Sauerberg   +8 more
openaire   +3 more sources

Partial Agonist Activity of Celiprolol

Journal of Cardiovascular Pharmacology, 1993
Celiprolol given intravenously (i.v.) to pithed rats in the dose range of 0.1-10,000 micrograms/g produced a dose-dependent increase in heart rate (HR) which was greatest (123 beats/min) at 1,000-3,000 micrograms/kg. This partial agonist effect was blocked by the selective beta 1-adrenoceptor antagonist CGP 20712A.
William J. Louis, Dimitrios Iakovidis, L.-H. Tung, B Campbell, Simon N S Louis, Graham P Jackman   +5 more
openaire   +3 more sources

A2A adenosine receptor agonists, antagonists, inverse agonists and partial agonists

2023
The Gs-coupled A2A adenosine receptor (A2AAR) has been explored extensively as a pharmaceutical target, which has led to numerous clinical trials. However, only one selective A2AAR agonist (regadenoson, Lexiscan) and one selective A2AAR antagonist (istradefylline, Nouriast) have been approved by the FDA, as a pharmacological agent for myocardial ...
Kenneth A, Jacobson, R Rama, Suresh, Paola, Oliva   +2 more
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Agonists, partial agonists, antagonists, inverse agonists and agonist/antagonists?

Trends in Pharmacological Sciences, 1987
The label placed on a drug influences its ultimate use. But interpretation ofin-vivo data has complicated the simple receptor theory of agonists and antagonists for certain classes of drugs.Terry Kenakin argues that clarification of such data — described in an extremely complex system — at a molecular level, will either obviate the need for terms such ...
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Partial agonists, full agonists, antagonists: dilemmas of definition

Trends in Pharmacological Sciences, 1993
The absence of selective antagonists makes receptor characterization difficult, and largely dependent on the use of agonists. However, there has been considerable debate as to whether certain drugs acting at G protein-coupled receptors are better described as agonists, partial agonists or antagonists. Indeed many agonists tend to display differences in
Hendrikus Boddeke, Daniel Hoyer
openaire   +3 more sources