Reciprocal Regulation of Agonist and Inverse Agonist Signaling Efficacy upon Short-Term Treatment of the Human δ-Opioid Receptor with an Inverse Agonist

2004 ◽  
Vol 67 (1) ◽  
pp. 336-348 ◽  
Author(s):  
Graciela Piñeyro ◽  
Mounia Azzi ◽  
André deLéan ◽  
Peter W. Schiller ◽  
Michel Bouvier
2020 ◽  
Vol 20 (31) ◽  
pp. 2889-2902 ◽  
Author(s):  
Shigeto Hirayama ◽  
Hideaki Fujii

The discovery of δ opioid receptor inverse agonist activity induced by ICI-174,864, which was previously reported as an δ opioid receptor antagonist, opened the door for the investigation of inverse agonism/constitutive activity of the receptors. Various peptidic or non-peptidic δ opioid receptor inverse agonists have since been developed. Compared with the reports dealing with in vitro inverse agonist activities of novel compounds or known compounds as antagonists, there have been almost no publications describing the in vivo pharmacological effects induced by a δ opioid receptor inverse agonist. After the observation of anorectic effects with the δ opioid receptor antagonism was discussed in the early 2000s, the short-term memory improving effects and antitussive effects have been very recently reported as possible pharmacological effects induced by a δ opioid receptor inverse agonist. In this review, we will survey the developed δ opioid receptor inverse agonists and summarize the possible in vivo pharmacological effects by δ opioid receptor inverse agonists. Moreover, we will discuss important issues involved in the investigation of the in vivo pharmacological effects produced by a δ opioid receptor inverse agonist.


Author(s):  
TRISNI UNTARI DEWI ◽  
INSTIATY . ◽  
RUDIANTO SEDONO ◽  
GESTINA ALISKA ◽  
MUHAMMAD KHIFZHON AZWAR ◽  
...  

Objective: This study sought to determine the correlation between trough plasma amikacin concentrations and urinary normalized kidney injurymolecule-1 (KIM-1) concentrations as an early biomarker of nephrotoxicity in patients with sepsis who are hospitalized in an intensive care unit.Methods: In this pilot study, 12 patients with sepsis were treated with amikacin 1000 mg/day between May 2015 and September 2015. The correlationbetween trough plasma amikacin concentrations measured after the third dose and the elevation of urinary normalized KIM-1 concentrations afterthe third amikacin dose relative to the first/second dose was evaluated.Results: In total, three patients had trough plasma amikacin concentrations exceeding the safe level (>10 μg/ml). Furthermore, eight patientsdisplayed higher normalized KIM-1 concentrations after third dose than after the first/second dose; however, there was no correlation betweentrough amikacin concentrations and the elevation of urinary normalized KIM-1 concentrations (r=0.3, p=0.3).Conclusion: The study results illustrated that short-term treatment with an amikacin dose of 1000 mg/day was generally safe in patients with sepsis.


1997 ◽  
Vol 6 (4) ◽  
pp. 9-16 ◽  
Author(s):  
Alison Behrman ◽  
Robert F. Orlikoff

Sophisticated, computer-based instrumentation has become increasingly available to the voice clinician. Yet substantial questions remain regarding its clinical necessity and usefulness. A theoretical model based on the scientific method is developed as a framework that can be used to guide the clinician in the selection and application of instrumental measures. Using the process of hypothesis testing, instrumentation is presented as an integral component of clinical practice. The uses of instrumental measures, and their relevance to long- and short-term treatment goals, are addressed. Clinical examples are presented to illustrate the incorporation of instrumentation and the scientific method into assessment and treatment.


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