Pharmacological Characterization Of The A2C-adrenoceptor Agonist Compound A In Binding, In Vitro And In Vivo Assays

2010 ◽  
Author(s):  
Michel R. Corboz ◽  
Maria A. Rivelli ◽  
Gissela Lieber ◽  
Yanlin Jia ◽  
Robbie L. McLeod ◽  
...  
Keyword(s):  
Pharmacological Characterization ◽  
Compound A ◽  
In Vivo Assays ◽  
Adrenoceptor Agonist

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.

Pharmacological Characterization of a Novel α2C-Adrenoceptor Agonist N-[3,4-dihydro-4-(1H-imidazol-4-ylmethyl)-2H-1, 4-benzoxazin-6-yl]-N-ethyl-N′-methylurea (Compound A)

2011 ◽  
Vol 337 (1) ◽  
pp. 256-266 ◽  
Author(s):  
Michel R. Corboz ◽  
Maria A. Rivelli ◽  
Kevin D. McCormick ◽  
Yuntao Wan ◽  
Himanshu Shah ◽  
...  
Keyword(s):  
Pharmacological Characterization ◽  
Compound A ◽  
Adrenoceptor Agonist

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

Pharmacological Characterization of the New Stable Antiarrhythmic Peptide Analog Ac-d-Tyr-d-Pro-d-Hyp-Gly-d-Ala-Gly-NH2 (ZP123): In Vivo and in Vitro Studies

2003 ◽  
Vol 306 (3) ◽  
pp. 1191-1199 ◽  
Author(s):  
Anne Louise Kjølbye ◽  
Carsten Boye Knudsen ◽  
Trine Jepsen ◽  
Bjarne Due Larsen ◽  
Jørgen Søberg Petersen
Keyword(s):  
In Vitro Studies ◽  
Pharmacological Characterization ◽  
Peptide Analog ◽  
Antiarrhythmic Peptide

scholarly journals In Vitro and In Vivo Pharmacological Characterization of Galanin and Galnon

2006 ◽  
Vol 20 (4) ◽  
Author(s):  
Johannes Rajarao ◽  
Lisa Potestio ◽  
Jessica Malberg ◽  
Corey Bender ◽  
Bart Nieuwenhuijsen ◽  
...  
Keyword(s):  
Pharmacological Characterization

In vitro and in vivo pharmacological characterization of SB 201993, an eicosanoid-like LTB4receptor antagonist with anti-inflammatory activity

1999 ◽  
Vol 61 (1) ◽  
pp. 55-64 ◽  
Author(s):  
H.M. Sarau ◽  
J.J. Foley ◽  
D.B. Schmidt ◽  
L.D. Martin ◽  
E.F. Webb ◽  
...  
Keyword(s):  
Inflammatory Activity ◽  
Pharmacological Characterization ◽  
Anti Inflammatory

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
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