In vitro and in vivo pharmacological characterization of SSD114, a novel GABAB positive allosteric modulator

2016 ◽  
Vol 791 ◽  
pp. 115-123 ◽  
Author(s):  
Alessandra Porcu ◽  
Carla Lobina ◽  
Daniela Giunta ◽  
Maurizio Solinas ◽  
Claudia Mugnaini ◽  
...  
Keyword(s):  
Allosteric Modulator ◽  
Positive Allosteric Modulator ◽  
Pharmacological Characterization

In vitro and in vivo characterization of PheTQS, a novel α7 nAChR positive allosteric modulator

2009 ◽  
Vol 78 (7) ◽  
pp. 913 ◽  
Author(s):  
James N.C. Kew ◽  
Selina Mok ◽  
Annette Weil ◽  
Caterina Virginio ◽  
Laura Castelletti ◽  
...  
Keyword(s):  
Allosteric Modulator ◽  
Positive Allosteric Modulator ◽  
Α7 Nachr ◽  
In Vivo Characterization

In vitro and in vivo characterization of the novel GABAB receptor positive allosteric modulator, 2-{1-[2-(4-chlorophenyl)-5-methylpyrazolo[1,5-a]pyrimidin-7-yl]-2-piperidinyl}ethanol (CMPPE)

2011 ◽  
Vol 61 (5-6) ◽  
pp. 957-966 ◽  
Author(s):  
Elisabetta Perdona’ ◽  
Vivian J.A. Costantini ◽  
Michela Tessari ◽  
Prisca Martinelli ◽  
Corrado Carignani ◽  
...  
Keyword(s):  
Gabab Receptor ◽  
Allosteric Modulator ◽  
The Novel ◽  
Positive Allosteric Modulator ◽  
In Vivo Characterization

In vitro pharmacological characterization of ABT-779, a novel positive allosteric modulator of α7 nAChRs

2011 ◽  
Vol 82 (8) ◽  
pp. 1030 ◽  
Author(s):  
John Malysz ◽  
Jens Halvard Gronlien ◽  
Clark A. Briggs ◽  
David J. Anderson ◽  
Rachid El-Kouhen ◽  
...  
Keyword(s):  
Allosteric Modulator ◽  
Positive Allosteric Modulator ◽  
Pharmacological Characterization ◽  
Α7 Nachrs

scholarly journals Molecular and functional characterization of somatostatin-type signalling in a deuterostome invertebrate

Open Biology ◽  
2020 ◽  
Vol 10 (9) ◽  
pp. 200172
Author(s):  
Ya Zhang ◽  
Luis Alfonso Yañez Guerra ◽  
Michaela Egertová ◽  
Cleidiane G. Zampronio ◽  
Alexandra M. Jones ◽  
...  
Keyword(s):  
Functional Characterization ◽  
The Body ◽  
Pharmacological Characterization ◽  
Cardiac Stomach ◽  
Physiological Processes ◽  
Pharmacological Tests ◽  
The Central Nervous System

Somatostatin (SS) and allatostatin-C (ASTC) are structurally and evolutionarily related neuropeptides that act as inhibitory regulators of physiological processes in mammals and insects, respectively. Here, we report the first molecular and functional characterization of SS/ASTC-type signalling in a deuterostome invertebrate—the starfish Asterias rubens (phylum Echinodermata). Two SS/ASTC-type precursors were identified in A. rubens (ArSSP1 and ArSSP2) and the structures of neuropeptides derived from these proteins (ArSS1 and ArSS2) were analysed using mass spectrometry. Pharmacological characterization of three cloned A. rubens SS/ASTC-type receptors (ArSSR1–3) revealed that ArSS2, but not ArSS1, acts as a ligand for all three receptors. Analysis of ArSS2 expression in A. rubens using mRNA in situ hybridization and immunohistochemistry revealed stained cells/fibres in the central nervous system, the digestive system (e.g. cardiac stomach) and the body wall and its appendages (e.g. tube feet). Furthermore, in vitro pharmacological tests revealed that ArSS2 causes dose-dependent relaxation of tube foot and cardiac stomach preparations, while injection of ArSS2 in vivo causes partial eversion of the cardiac stomach. Our findings provide new insights into the molecular evolution of SS/ASTC-type signalling in the animal kingdom and reveal an ancient role of SS-type neuropeptides as inhibitory regulators of muscle contractility.

scholarly journals P2-065: IN VITRO PHARMACOLOGICAL CHARACTERIZATION OF S68890, AN ALLOSTERIC MODULATOR OF ALPHA7 NICOTINIC RECEPTORS

2019 ◽  
Vol 15 ◽  
pp. P595-P596
Author(s):  
Laurence Danober ◽  
Kumiko Kambara ◽  
Sonia Bertrand ◽  
Daniel Bertrand ◽  
Alain Benoist ◽  
...  
Keyword(s):  
Nicotinic Receptors ◽  
Allosteric Modulator ◽  
Pharmacological Characterization

P2-311: In vitro characterization of s44858: A positive allosteric modulator of ampa receptors and GluN2B selective non-competitive nmda receptors antagonist

2015 ◽  
Vol 11 (7S_Part_13) ◽  
pp. P612-P613
Author(s):  
Laurence Danober ◽  
Jean-Yves Thomas ◽  
Sylvie Challal ◽  
Nathalie Rogez ◽  
Karine Albinet ◽  
...  
Keyword(s):  
Nmda Receptors ◽  
Ampa Receptors ◽  
Allosteric Modulator ◽  
Positive Allosteric Modulator ◽  
In Vitro Characterization
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