Plasma and cerebrospinal fluid (CSF) pharmacokinetics of CP-457,920, a selective alpha 5 GABA-A receptor inverse agonist in young, healthy volunteers

2004 ◽  
Vol 75 (2) ◽  
pp. P30 ◽  
Author(s):  
M Bednar
Keyword(s):  
Cerebrospinal Fluid ◽  
Healthy Volunteers ◽  
Inverse Agonist ◽  
Gaba A ◽  
Csf Pharmacokinetics ◽  
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.

High specific activity tritiation of the pyridazin-3-one histamine H3 receptor inverse agonist CEP-27088

2012 ◽  
Vol 70 (3) ◽  
pp. 512-514 ◽  
Author(s):  
Joseph R. Andrews ◽  
Crist N. Filer ◽  
Mario Maniscalco ◽  
Nadine C. Becknell ◽  
Robert L. Hudkins
Keyword(s):  
Specific Activity ◽  
High Specific Activity ◽  
Inverse Agonist ◽  
Histamine H3 Receptor ◽  
H3 Receptor ◽  
Receptor Inverse Agonist ◽  
Histamine H3

scholarly journals P2-026: SUVN-G3031, a Potent and Selective H3 Receptor Inverse Agonist: Safety, Tolerability and Pharmacokinetics in Humans

2016 ◽  
Vol 12 ◽  
pp. P618-P619 ◽  
Author(s):  
Gopinadh Bhyrapuneni ◽  
Koteshwara Mudigonda ◽  
Kiran Kumar Penta ◽  
Veera Raghava Chowdary Palacharla ◽  
NageswaraRao Muddana ◽  
...  
Keyword(s):  
Inverse Agonist ◽  
H3 Receptor ◽  
Receptor Inverse Agonist

scholarly journals Cognitive Improvements in Children with Prader-Willi Syndrome Following Pitolisant Treatment—Patient Reports

2019 ◽  
Vol 24 (2) ◽  
pp. 166-171 ◽  
Author(s):  
Lara C. Pullen ◽  
Maria Picone ◽  
Litjen Tan ◽  
Charles Johnston ◽  
Holger Stark
Keyword(s):  
Daytime Sleepiness ◽  
Therapeutic Option ◽  
Case Series ◽  
Poor Quality ◽  
Inverse Agonist ◽  
Prader Willi Syndrome ◽  
Cognitive Disability ◽  
Patient Reports ◽  
Nighttime Sleep ◽  
Receptor Inverse Agonist

While children with Prader-Willi Syndrome (PWS), a rare genetic disease with an incidence of 1:15,000, typically present with hypotonia and hyperphagia, their lives are made more difficult by an ever-present sleepiness as well as multiple neuro-cognitive dysfunctions, including cognitive defects. We describe a case series of 3 children who were treated with the histamine 3 receptor inverse agonist pitolisant. While this first-in-class inverse agonist is approved for another orphan disease (i.e., narcolepsy with or without cataplexy), we have observed that pediatric patients with PWS prescribed pitolisant demonstrate decreased daytime sleepiness and improved cognition, as evidenced by increased processing speed and improved mental clarity. Pitolisant may represent a novel therapeutic option that might relieve substantial PWS disease burden, including cognitive disability, excessive daytime sleepiness, and poor-quality nighttime sleep.

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