Pharmacological characterization of CRTh2 antagonist LAS191859: Long receptor residence time translates into long-lasting in vivo efficacy

2016 ◽  
Vol 111 ◽  
pp. 208-216 ◽  
Author(s):  
Marta Calbet ◽  
Miriam Andrés ◽  
Clara Armengol ◽  
Mónica Bravo ◽  
Peter Eichhorn ◽  
...  
Keyword(s):  
Residence Time ◽  
Pharmacological Characterization ◽  
In Vivo Efficacy

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.

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 vivo pharmacological characterization of the structurally novel, potent, selective mGlu2/3 receptor agonist LY404039 in animal models of psychiatric disorders

2007 ◽  
Vol 193 (1) ◽  
pp. 121-136 ◽  
Author(s):  
Linda M. Rorick-Kehn ◽  
Bryan G. Johnson ◽  
Karen M. Knitowski ◽  
Craig R. Salhoff ◽  
Jeffrey M. Witkin ◽  
...  
Keyword(s):  
Animal Models ◽  
Psychiatric Disorders ◽  
Receptor Agonist ◽  
Pharmacological Characterization

Pharmacological characterization of novel tissue kallikrein inhibitors in vivo

1996 ◽  
Vol 32 (1-3) ◽  
pp. 111-114 ◽  
Author(s):  
Luciana Bizeto ◽  
Edson Antunes ◽  
Fernanda C.V. Portaro ◽  
Maria Aparecida Juliano ◽  
Luiz Juliano ◽  
...  
Keyword(s):  
Tissue Kallikrein ◽  
Pharmacological Characterization ◽  
Kallikrein Inhibitors
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