Pharmacological Characterization of the Competitive GLUK5 Receptor Antagonist Decahydroisoquinoline LY466195 in Vitro and in Vivo

2006 ◽  
Vol 318 (2) ◽  
pp. 772-781 ◽  
Author(s):  
Brianne Weiss ◽  
Andrew Alt ◽  
Ann Marie Ogden ◽  
Mary Gates ◽  
Donna K. Dieckman ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Pharmacological Characterization

In vitro and in vivo pharmacological characterization of Pronetupitant, a prodrug of the neurokinin 1 receptor antagonist Netupitant

Peptides ◽  
2015 ◽  
Vol 69 ◽  
pp. 26-32 ◽  
Author(s):  
Chiara Ruzza ◽  
Anna Rizzi ◽  
Davide Malfacini ◽  
Stefano Molinari ◽  
Claudio Giuliano ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Pharmacological Characterization ◽  
Neurokinin 1 Receptor ◽  
Neurokinin 1

Pharmacological characterization of the TRPV1 receptor antagonist JYL1421 (SC0030) in vitro and in vivo in the rat

2005 ◽  
Vol 517 (1-2) ◽  
pp. 35-44 ◽  
Author(s):  
Balázs Jakab ◽  
Zsuzsanna Helyes ◽  
Angelika Varga ◽  
Kata Bölcskei ◽  
Árpád Szabó ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Pharmacological Characterization ◽  
Trpv1 Receptor

In vitro and in vivo pharmacological characterization of J-113397, a potent and selective non-peptidyl ORL1 receptor antagonist

2000 ◽  
Vol 402 (1-2) ◽  
pp. 45-53 ◽  
Author(s):  
Satoshi Ozaki ◽  
Hiroshi Kawamoto ◽  
Yoshiki Itoh ◽  
Mitsuru Miyaji ◽  
Tomoko Azuma ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Pharmacological Characterization ◽  
Orl1 Receptor

scholarly journals In Vitro and in Vivo Pharmacological Characterization of the Neuropeptide S Receptor Antagonist [d-Cys(tBu)5]Neuropeptide S

2008 ◽  
Vol 328 (2) ◽  
pp. 549-555 ◽  
Author(s):  
Valeria Camarda ◽  
Anna Rizzi ◽  
Chiara Ruzza ◽  
Silvia Zucchini ◽  
Giuliano Marzola ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Neuropeptide S ◽  
Pharmacological Characterization

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
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