scholarly journals Prostaglandin FP receptor antagonists: discovery, pharmacological characterization and therapeutic utility

2018 ◽  
Vol 176 (8) ◽  
pp. 1059-1078 ◽  
Author(s):  
Najam A Sharif ◽  
Peter G Klimko
Keyword(s):  
Receptor Antagonists ◽  
Pharmacological Characterization ◽  
Fp Receptor ◽  
Therapeutic Utility

Pharmacological characterization of human NPFF1 and NPFF2 receptors expressed in CHO cells by using NPY Y1 receptor antagonists

2002 ◽  
Vol 451 (3) ◽  
pp. 245-256 ◽  
Author(s):  
Catherine Mollereau ◽  
Honoré Mazarguil ◽  
Delphine Marcus ◽  
Isabelle Quelven ◽  
Masato Kotani ◽  
...  
Keyword(s):  
Cho Cells ◽  
Receptor Antagonists ◽  
Pharmacological Characterization ◽  
Y1 Receptor

Pharmacological characterization of H3 receptor antagonists with imidazole, thioimidazole and thioimidazoline polar groups in the side chain

2000 ◽  
Vol 49 (S1) ◽  
pp. 62-63 ◽  
Author(s):  
E. Barocelli ◽  
V. Ballabeni ◽  
M. Chiavarini ◽  
S. Bertoni ◽  
M. Mor ◽  
...  
Keyword(s):  
Side Chain ◽  
Receptor Antagonists ◽  
Pharmacological Characterization ◽  
Polar Groups ◽  
H3 Receptor

A new convenient synthetic method and preliminary pharmacological characterization of triazinediones as prokineticin receptor antagonists

2014 ◽  
Vol 81 ◽  
pp. 334-340 ◽  
Author(s):  
Cenzo Congiu ◽  
Valentina Onnis ◽  
Alessandro Deplano ◽  
Severo Salvadori ◽  
Veronica Marconi ◽  
...  
Keyword(s):  
Synthetic Method ◽  
Receptor Antagonists ◽  
Pharmacological Characterization

Prevention of reflex natriuresis after acute unilateral nephrectomy by melanocortin receptor antagonists

1998 ◽  
Vol 274 (4) ◽  
pp. R931-R938 ◽  
Author(s):  
Xi-Ping Ni ◽  
Robert A. Kesterson ◽  
Shubh D. Sharma ◽  
Victor J. Hruby ◽  
Roger D. Cone ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Urinary Sodium Excretion ◽  
Melanocortin Receptor ◽  
Unilateral Nephrectomy ◽  
Sprague Dawley ◽  
Receptor Antagonists ◽  
Pharmacological Characterization ◽  
Melanocyte Stimulating Hormone ◽  
Sprague Dawley Rats

γ-Melanocyte-stimulating hormone (γ-MSH), atrial natriuretic peptide (ANP), and oxytocin have been identified as candidate hormonal mediators of the reflex natriuresis that follows acute unilateral nephrectomy (AUN). Pharmacological characterization of the third melanocortin receptor (MC3-R) indicates that it uniquely responds to physiological concentrations of γ-MSH. We tested the roles of γ-MSH, ANP, and oxytocin in the postnephrectomy natriuresis by carrying out AUN during continuous intrarenal infusion of specific antagonists for their cognate receptors. In anesthetized Sprague-Dawley rats, urinary sodium excretion (UNaV) increased from 0.34 ± 0.04 to 1.12 ± 0.11 μeq/min 90 min after AUN ( P < 0.001). No change in UNaV occurred in rats undergoing a sham AUN procedure. Plasma immunoreactive γ-MSH concentration was 53 ± 8 fmol/ml after sham AUN but 112 ± 17 fmol/ml after AUN ( P < 0.01). SHU-9119 and SHU-9005 are substituted derivatives of α-MSH with potent antagonism at the MC3-R in vitro. Infusion of these compounds at 5 pmol/min completely blocked the natriuretic response to AUN despite a similar elevation in plasma γ-MSH (111 ± 12 vs. 49 ± 8 fmol/ml in sham rats, P < 0.01). Intrarenal infusion of the ANP receptor antagonist A-71915 (5 pmol/min) or the oxytocin receptor antagonist [d(CH2)5 1, Tyr(Me)2,Orn8] vasotocin (10 pmol/min) effectively inhibited the natriuresis induced by intravenous infusion of ANP or oxytocin (each at 1 pmol/min), respectively, but did not block the natriuresis after AUN. Plasma immunoreactivity of these peptides was not increased after AUN. These results indicate that reflex natriuresis after AUN is accompanied by an increase in plasma γ-MSH but not ANP or oxytocin concentration and is prevented by intrarenal infusion of receptor antagonists with selectivity for MC3-R. The data indicate that γ-MSH or a closely related peptide mediates postnephrectomy natriuresis and provide further support for the possibility that γ-MSH may play a wider role in sodium homeostasis.

Identification and Pharmacological Characterization of Domains Involved in Binding of CGRP Receptor Antagonists to the Calcitonin-like Receptor

Biochemistry ◽  
2006 ◽  
Vol 45 (6) ◽  
pp. 1881-1887 ◽  
Author(s):  
Christopher A. Salvatore ◽  
John J. Mallee ◽  
Ian M. Bell ◽  
C. Blair Zartman ◽  
Theresa M. Williams ◽  
...  
Keyword(s):  
Cgrp Receptor ◽  
Receptor Antagonists ◽  
Pharmacological Characterization ◽  
Cgrp Receptor Antagonists
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