Development and validation of an assay for a novel ghrelin receptor inverse agonist PF-5190457 and its major hydroxy metabolite (PF-6870961) by LC-MS/MS in human plasma

2019 ◽  
Vol 1130-1131 ◽  
pp. 121820
Author(s):  
Sravani Adusumalli ◽  
Rohitash Jamwal ◽  
Lorenzo Leggio ◽  
Fatemeh Akhlaghi
Keyword(s):  
Human Plasma ◽  
Inverse Agonist ◽  
Ghrelin Receptor ◽  
Development And Validation ◽  
Receptor Inverse Agonist ◽  
Hydroxy Metabolite

scholarly journals Role of Molybdenum-Containing Enzymes in the Biotransformation of the Novel Ghrelin Receptor Inverse Agonist PF-5190457: A Reverse Translational Bed-to-Bench Approach

2019 ◽  
Vol 47 (8) ◽  
pp. 874-882 ◽  
Author(s):  
Sravani Adusumalli ◽  
Rohitash Jamwal ◽  
R. Scott Obach ◽  
Tim F. Ryder ◽  
Lorenzo Leggio ◽  
...  
Keyword(s):  
Inverse Agonist ◽  
The Novel ◽  
Ghrelin Receptor ◽  
Receptor Inverse Agonist

scholarly journals Pharmacokinetics and pharmacodynamics of PF-05190457: The first oral ghrelin receptor inverse agonist to be profiled in healthy subjects

2016 ◽  
Vol 83 (2) ◽  
pp. 326-338 ◽  
Author(s):  
William S. Denney ◽  
Gabriele E. Sonnenberg ◽  
Santos Carvajal-Gonzalez ◽  
Theresa Tuthill ◽  
V. Margaret Jackson
Keyword(s):  
Healthy Subjects ◽  
Inverse Agonist ◽  
Pharmacokinetics And Pharmacodynamics ◽  
Ghrelin Receptor ◽  
Receptor Inverse Agonist

scholarly journals Discovery of PF-5190457, a Potent, Selective, and Orally Bioavailable Ghrelin Receptor Inverse Agonist Clinical Candidate

2014 ◽  
Vol 5 (5) ◽  
pp. 474-479 ◽  
Author(s):  
Samit K. Bhattacharya ◽  
Kim Andrews ◽  
Ramsay Beveridge ◽  
Kimberly O. Cameron ◽  
Chiliu Chen ◽  
...  
Keyword(s):  
Inverse Agonist ◽  
Ghrelin Receptor ◽  
Orally Bioavailable ◽  
Receptor Inverse Agonist ◽  
Clinical Candidate

C-terminus of a hexapeptidic ghrelin receptor inverse agonist can switch peptide behavior from inverse agonism to agonism

Biopolymers ◽  
2016 ◽  
Vol 106 (1) ◽  
pp. 101-108 ◽  
Author(s):  
Sylvia Els-Heindl ◽  
Kathrin Bellmann-Sickert ◽  
Annette G. Beck-Sickinger
Keyword(s):  
Inverse Agonist ◽  
Ghrelin Receptor ◽  
Inverse Agonism ◽  
C Terminus ◽  
Receptor Inverse Agonist

LC–MS/MS method for the quantification of SUVN-G3031, a novel H3 receptor inverse agonist for narcolepsy treatment

Bioanalysis ◽  
2020 ◽  
Vol 12 (8) ◽  
pp. 533-544 ◽  
Author(s):  
Ramakrishna Nirogi ◽  
Devender Reddy Ajjala ◽  
Naga Surya Prakash Padala ◽  
Ilayaraja Kalaikadhiban ◽  
Lakshmi Prasanna Rayapati ◽  
...  
Keyword(s):  
Healthy Volunteers ◽  
Human Plasma ◽  
Human Study ◽  
Inverse Agonist ◽  
Clinical Development ◽  
Protein Precipitation ◽  
Esi Ms ◽  
H3 Receptor ◽  
Receptor Inverse Agonist

Background: A LC–MS/MS method was validated for the quantification of SUVN-G3031, a novel H3 receptor inverse agonist in clinical development for the treatment of patients with narcolepsy, with and without cataplexy. Methodology: SUVN-G3031 was extracted from plasma following acetonitrile protein precipitation, separated by Ultra HPLC and quantified using positive ESI–MS/MS. Results: The method was linear across the range of 0.1–100 ng ml-1 in plasma. Results for intra and inter-day accuracy were from 99.8 to 104% and precision (%CV) was ≤10.6%. Conclusion: The method was applied to a first-in-human study in healthy volunteers. The method is precise, accurate and highly selective for the quantification of SUVN-G3031 in human plasma.

scholarly journals Development of a ghrelin receptor inverse agonist for positron emission tomography

Oncotarget ◽  
2021 ◽  
Vol 12 (5) ◽  
pp. 450-474
Author(s):  
Ralf Bergmann ◽  
Constance Chollet ◽  
Sylvia Els-Heindl ◽  
Martin Ullrich ◽  
Nicole Berndt ◽  
...  
Keyword(s):  
Positron Emission Tomography ◽  
Inverse Agonist ◽  
Emission Tomography ◽  
Ghrelin Receptor ◽  
Positron Emission ◽  
Receptor Inverse Agonist
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