scholarly journals The In Vivo Effects of the CB1-Positive Allosteric Modulator GAT229 on Intraocular Pressure in Ocular Normotensive and Hypertensive Mice

2017 ◽  
Vol 33 (8) ◽  
pp. 582-590 ◽  
Author(s):  
Elizabeth A. Cairns ◽  
Anna-Maria Szczesniak ◽  
Alex J. Straiker ◽  
Pushkar M. Kulkarni ◽  
Roger G. Pertwee ◽  
...  
Keyword(s):  
Intraocular Pressure ◽  
Allosteric Modulator ◽  
Positive Allosteric Modulator ◽  
In Vivo Effects

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

scholarly journals In Silico Identification and Experimental Validation of (−)-Muqubilin A, a Marine Norterpene Peroxide, as PPARα/γ-RXRα Agonist and RARα Positive Allosteric Modulator

Marine Drugs ◽  
2019 ◽  
Vol 17 (2) ◽  
pp. 110 ◽  
Author(s):  
Enrico D’Aniello ◽  
Fabio Iannotti ◽  
Lauren Falkenberg ◽  
Andrea Martella ◽  
Alessandra Gentile ◽  
...  
Keyword(s):  
Binding Mode ◽  
Allosteric Modulator ◽  
Positive Allosteric Modulator ◽  
Full Agonist ◽  
Synergistic Enhancement ◽  
Pharmacological Targets ◽  
In Vivo Analysis ◽  
Dynamics Simulations ◽  
Micromolar Range

The nuclear receptors (NRs) RARα, RXRα, PPARα, and PPARγ represent promising pharmacological targets for the treatment of neurodegenerative diseases. In the search for molecules able to simultaneously target all the above-mentioned NRs, we screened an in-house developed molecular database using a ligand-based approach, identifying (−)-Muqubilin (Muq), a cyclic peroxide norterpene from a marine sponge, as a potential hit. The ability of this compound to stably and effectively bind these NRs was assessed by molecular docking and molecular dynamics simulations. Muq recapitulated all the main interactions of a canonical full agonist for RXRα and both PPARα and PPARγ, whereas the binding mode toward RARα showed peculiar features potentially impairing its activity as full agonist. Luciferase assays confirmed that Muq acts as a full agonist for RXRα, PPARα, and PPARγ with an activity in the low- to sub-micromolar range. On the other hand, in the case of RAR, a very weak agonist activity was observed in the micromolar range. Quite surprisingly, we found that Muq is a positive allosteric modulator for RARα, as both luciferase assays and in vivo analysis using a zebrafish transgenic retinoic acid (RA) reporter line showed that co-administration of Muq with RA produced a potent synergistic enhancement of RARα activation and RA signaling.

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

scholarly journals A 5-mer peptide derived from hinge region of hFSHR can function as positive allosteric modulator in vivo

2021 ◽  
Vol 1863 (1) ◽  
pp. 183492
Author(s):  
Kaushiki S. Prabhudesai ◽  
Muthu Sankar Aathi ◽  
Vikas Dighe ◽  
Susan Idicula-Thomas
Keyword(s):  
Hinge Region ◽  
Allosteric Modulator ◽  
Positive Allosteric Modulator

[P4-036]: THE NOVEL AMPA RECEPTOR POSITIVE ALLOSTERIC MODULATOR S 47445 RESCUES IN VIVO CA3-CA1 LONG-TERM POTENTIATION AND STRUCTURAL SYNAPTIC CHANGES IN MIDDLE-AGED MICE

2017 ◽  
Vol 13 (7S_Part_26) ◽  
pp. P1270-P1270
Author(s):  
Sylvie Bretin ◽  
Albert Giralt ◽  
María Ángeles Gómez-Climent ◽  
Rafael Alcalá ◽  
Jose Maria Delgado-Garcia ◽  
...  
Keyword(s):  
Ampa Receptor ◽  
Long Term Potentiation ◽  
Allosteric Modulator ◽  
The Novel ◽  
Positive Allosteric Modulator ◽  
Aged Mice ◽  
Term Potentiation ◽  
Synaptic Changes

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
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