scholarly journals The mGluR2 Positive Allosteric Modulator, AZD8529, and Cue-Induced Relapse to Alcohol Seeking in Rats

2016 ◽  
Vol 41 (12) ◽  
pp. 2932-2940 ◽  
Author(s):  
Eric Augier ◽  
Russell S Dulman ◽  
Caroline Rauffenbart ◽  
Gaëlle Augier ◽  
Alan J Cross ◽  
...  
Keyword(s):  
Allosteric Modulator ◽  
Positive Allosteric Modulator ◽  
Alcohol Seeking

scholarly journals The GABAB Positive Allosteric Modulator ADX71441 Attenuates Alcohol Self-Administration and Relapse to Alcohol Seeking in Rats

2017 ◽  
Vol 42 (9) ◽  
pp. 1789-1799 ◽  
Author(s):  
Eric Augier ◽  
Russell S Dulman ◽  
Ruslan Damadzic ◽  
Andrew Pilling ◽  
J Paul Hamilton ◽  
...  
Keyword(s):  
Allosteric Modulator ◽  
Self Administration ◽  
Positive Allosteric Modulator ◽  
Alcohol Seeking

Correction: Structural modeling and role of HAX-1 as a positive allosteric modulator of human serine protease HtrA2

2020 ◽  
Vol 477 (2) ◽  
pp. 459-459
Author(s):  
Lalith K. Chaganti ◽  
Shubhankar Dutta ◽  
Raja Reddy Kuppili ◽  
Mriganka Mandal ◽  
Kakoli Bose
Keyword(s):  
Serine Protease ◽  
Structural Modeling ◽  
Allosteric Modulator ◽  
Positive Allosteric Modulator

scholarly journals Discovery of BNC375, a Potent, Selective, and Orally Available Type I Positive Allosteric Modulator of α7 nAChRs

2019 ◽  
Vol 10 (5) ◽  
pp. 754-760 ◽  
Author(s):  
Andrew J. Harvey ◽  
Thomas D. Avery ◽  
Laurent Schaeffer ◽  
Christophe Joseph ◽  
Belinda C. Huff ◽  
...  
Keyword(s):  
Allosteric Modulator ◽  
Type I ◽  
Positive Allosteric Modulator ◽  
Α7 Nachrs

scholarly journals Comparison of pregnenolone sulfate, pregnanolone and estradiol levels between patients with menstrually-related migraine and controls: an exploratory study

2021 ◽  
Vol 22 (1) ◽  
Author(s):  
Cecilia Rustichelli ◽  
Elisa Bellei ◽  
Stefania Bergamini ◽  
Emanuela Monari ◽  
Flavia Lo Castro ◽  
...  
Keyword(s):  
Exploratory Study ◽  
Serum Levels ◽  
Enzyme Linked Immunosorbent Assay ◽  
Control Group ◽  
Allosteric Modulator ◽  
Positive Allosteric Modulator ◽  
Pregnenolone Sulfate ◽  
Menstrually Related Migraine ◽  
History Of ◽  
Estradiol Levels

Abstract Background Neurosteroids affect the balance between neuroexcitation and neuroinhibition but have been little studied in migraine. We compared the serum levels of pregnenolone sulfate, pregnanolone and estradiol in women with menstrually-related migraine and controls and analysed if a correlation existed between the levels of the three hormones and history of migraine and age. Methods Thirty women (mean age ± SD: 33.5 ± 7.1) with menstrually-related migraine (MM group) and 30 aged- matched controls (mean age ± SD: 30.9 ± 7.9) participated in the exploratory study. Pregnenolone sulfate and pregnanolone serum levels were analysed by liquid chromatography-tandem mass spectrometry, while estradiol levels by enzyme-linked immunosorbent assay. Results Serum levels of pregnenolone sulfate and pregnanolone were significantly lower in the MM group than in controls (pregnenolone sulfate: P = 0.0328; pregnanolone: P = 0.0271, Student’s t-test), while estradiol levels were similar. In MM group, pregnenolone sulfate serum levels were negatively correlated with history of migraine (R2 = 0.1369; P = 0.0482) and age (R2 = 0.2826, P = 0.0025) while pregnenolone sulfate levels were not age-related in the control group (R2 = 0.04436, P = 0.4337, linear regression analysis). Conclusion Low levels of both pregnanolone, a positive allosteric modulator of the GABAA receptor, and pregnenolone sulfate, a positive allosteric modulator of the NMDA receptor, involved in memory and learning, could contribute either to headache pain or the cognitive dysfunctions reported in migraine patients. Overall, our results agree with the hypothesis that migraine is a disorder associated with a loss of neurohormonal integrity, thus supporting the therapeutic potential of restoring low neurosteroid levels in migraine treatment.

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