Pharmacological Characterization of a Novel 5-HT4 Receptor Agonist, TS-951, in vitro

Pharmacology ◽  
2001 ◽  
Vol 63 (1) ◽  
pp. 8-16 ◽  
Author(s):  
Sumiyo Kajita ◽  
Chika Ito ◽  
Reiko Kawamura ◽  
Shoji Yasuda ◽  
Yoshihiko Isobe ◽  
...  
Keyword(s):  
Receptor Agonist ◽  
Pharmacological Characterization

scholarly journals Pharmacological characterization of a novel 5-HT4 receptor agonist, TS-951 in vitro.

1999 ◽  
Vol 79 ◽  
pp. 206
Author(s):  
Sumiyo Kajita ◽  
Chika Ito ◽  
Yoshihiko Isobe ◽  
Kiyomi Fukushima
Keyword(s):  
Receptor Agonist ◽  
Pharmacological Characterization

Pharmacological Characterization of Postjunctional α-Adrenoceptors in Human Nasal Mucosa

2005 ◽  
Vol 19 (5) ◽  
pp. 495-502 ◽  
Author(s):  
Michel R. Corboz ◽  
Maria A. Rivelli ◽  
Lori Varty ◽  
Jennifer Mutter ◽  
Mark Cartwright ◽  
...  
Keyword(s):  
Nasal Mucosa ◽  
Isometric Force ◽  
Ringer Solution ◽  
Predominant Role ◽  
Pharmacological Characterization ◽  
Human Nasal Mucosa ◽  
Force Transducers ◽  
Arteries And Veins

Background Functional α1- and α2-adrenoreceptor subtype pharmacology was characterized in an in vitro human nasal mucosa contractile bioassay. Methods Nasal mucosa was obtained from 49 donor patients and mucosal strips were placed in chambers filled with Krebs–Ringer solution and attached to isometric force transducers. Results Nonselective α-adrenoreceptor agonists epinephrine, norepinephrine, and oxymetazoline produced concentration-dependent contractions of isolated human nasal mucosa (pD2= 5.2, 4.9, and 6.5, respectively). The α2-adrenoreceptor agonist BHT-920 (10 μM)–induced contractions were blocked by yohimbine (0.01–1 μM) and prazosin (0.01–1 μM) inhibited the contractile response to the α1-adrenoreceptor agonist phenylephrine (10 μM). Histological analysis showed that phenylephrine and BHT-920 differentially contracted the arteries and veins of human nasal mucosa, respectively. Conclusion Our results indicate that functional α1- and α2-adrenoceptors are present and functional in human nasal mucosa. The a 2-adrenoceptors display a predominant role in contracting the veins and the α1-adrenoceptors appear to preferentially constrict the human nasal arteries.

Synthesis and pharmacological characterization of a new benzoxazole derivative as a potent 5-HT 3 receptor agonist

2003 ◽  
Vol 11 (13) ◽  
pp. 2709-2714 ◽  
Author(s):  
Pedro Luis López-Tudanca ◽  
Luis Labeaga ◽  
Ana Innerárity ◽  
Luisa Alonso-Cires ◽  
Inés Tapia ◽  
...  
Keyword(s):  
Receptor Agonist ◽  
Pharmacological Characterization

Pharmacological Characterization of PD151832, an M1 Muscarinic Receptor Agonist

1997 ◽  
pp. 311-315
Author(s):  
Roy D. Schwarz ◽  
Michael J. Callahan ◽  
Robert E. Davis ◽  
Mark R. Emmerling ◽  
Juan C. Jaen ◽  
...  
Keyword(s):  
Muscarinic Receptor ◽  
Receptor Agonist ◽  
Pharmacological Characterization ◽  
M1 Muscarinic

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.

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