Results 71 to 80 of about 47,360 (258)

Automated Synthesis of [18F]Flumazenil Application in GABAA Receptor Neuroimaging Availability for Rat Model of Anxiety [PDF]

, 2023
Shiou‐Shiow Farn, Kai-Hung Cheng, Yuan-Ruei Huang, Shih-Ying Lee, Jenn-Tzong Chen, Kang‐Wei Chang   +5 more
openalex   +1 more source

Novel approaches for drug development against chronic primary pain: A systematic review

British Journal of Pharmacology, EarlyView.
Abstract Chronic primary pain (CPP) persisting for more than 3 months, associated with significant emotional distress without any known underlying cause, is an unmet medical need. Traditional or adjuvant analgesics do not provide satisfactory pain relief for a great proportion of these patients.
Valéria Tékus, Éva Borbély, Andreas Goebel, Ralf Baron, Zsófia Hajna, Zsuzsanna Helyes   +5 more
wiley   +1 more source

Preclinical pharmacology of alogabat: a novel GABAA-α5 positive allosteric modulator targeting neurodevelopmental disorders with impaired GABAA signaling

Frontiers in Pharmacology
BackgroundAlterations in the GABAergic system contribute to the pathophysiology of neurodevelopmental disorders, including autism spectrum disorder (ASD) and Angelman syndrome (AS), particularly in cases involving large deletions in the 15q11–13 region ...
Giuseppe Cecere, Theresa M. Ballard, Frederic Knoflach, Michael Honer, Joerg F. Hipp, Pilar Garces, Thomas Mueggler, Basil Künnecke, Andreas Bruns, Eric P. Prinssen, Philipp Schoenenberger, Philipp Janz, Roger Redondo, Barbara Biemans, Henner Knust, Andrés Olivares-Morales, Alessandro Brigo, Jan Michael Schulz, Daniel Bertrand, Michael Saxe, Eoin C. O’Connor, Maria-Clemencia Hernandez   +21 more
doaj   +1 more source

Cannabigerol reverses mechanical allodynia through α2A‐adrenergic modulation of thalamocortical signaling in chemotherapy‐induced neuropathy

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Chemotherapy‐induced peripheral neuropathy (CIPN) is a prevalent and treatment‐resistant side effect of platinum‐based chemotherapy, characterised by mechanical allodynia. Cannabigerol (CBG), a non‐psychoactive cannabinoid, has shown antinociceptive potential, but its site and mechanism of action remain unclear.
Quinn W. Wade, Nathan Morris, Diana E. Sepulveda, Alonso Cortez‐Resendiz, Christopher Brandl, Jennifer E. Lausch, Mariya Starostina, Nicholas M. Graziane   +7 more
wiley   +1 more source

Synaptic recruitment of gephyrin regulates surface GABAA receptor dynamics for the expression of inhibitory LTP [PDF]

, 2014
Enrica Maria Petrini, Tiziana Ravasenga, Torben J. Hausrat, Giuliano Iurilli, Umberto Olcese, Victor Racine, Jean‐Baptiste Sibarita, Tija C. Jacob, Stephen J. Moss, Fabio Benfenati, Paolo Medini, Matthias Kneussel, Andrea Barberis   +12 more
openalex   +1 more source

Evaluation of preclinical antipsychotic models used to support first‐in‐human clinical trials

British Journal of Pharmacology, EarlyView.
Abstract Schizophrenia is regarded as a complex and heterogeneous psychiatric disorder, characterised by diverse symptoms and comorbidities, which complicate both clinical management and drug development. Current pharmacological treatment, primarily based on dopamine D2 receptor antagonism or partial agonism, which has not markedly progressed since the
Thi Viet Ha Nguyen, Declan P. McKernan, John P. Kelly   +2 more
wiley   +1 more source

Increased motor-impairing effects of the neuroactive steroid pregnanolone in mice with targeted inactivation of the GABAA receptor gamma2 subunit in the cerebellum

Frontiers in Pharmacology, 2016
Endogenous neurosteroids and neuroactive steroids have potent and widespread actions on the brain via inhibitory GABAA receptors. In recombinant receptors and genetic mouse models their actions depend on the alpha, beta and delta subunits of the receptor,
Elli Leppä, Anni-Maija Tuulikki Linden, M. Isabel Aller, Peer Wulff, Olga Vekovischeva, Bernhard Lüscher, Hartmut Lüddens, William Wisden, Esa R Korpi   +8 more
doaj   +1 more source

A PK/PD study on antihyperalgesia by an α2/3‐GABAA receptor PAM in mice: Lack of tolerance liability and potential involvement of γ1‐GABAA receptors

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose GABAA receptors (GABAARs) are heteropentameric ion channels that control almost all CNS functions, including spinal nociception. Most GABAARs contain a γ2 subunit but differ in their α and β subunit composition. TPA023B is an α2/α3 subtype selective, non‐sedative, positive allosteric modulator (PAM) with antihyperalgesic
Elena Neumann, Mariana O. Popa, Karen T. Elvers, Misa Oyama, Daniel Ulrich, Marcus Hanley, Gui Jie Feng, Thomas Hathaway, William T. Ralvenius, Thomas Grampp, Dietmar Benke, John R. Atack, Hanns Ulrich Zeilhofer   +12 more
wiley   +1 more source

Generation of recombinant antibodies to rat GABAA receptor subunits by affinity selection on synthetic peptides.

PLoS ONE, 2014
The abundance and physiological importance of GABAA receptors in the central nervous system make this neurotransmitter receptor an attractive target for localizing diagnostic and therapeutic biomolecules.
Sujatha P Koduvayur, Hélène A Gussin, Rajni Parthasarathy, Zengping Hao, Brian K Kay, David R Pepperberg   +5 more
doaj   +1 more source

A Pharmacogenetic ‘Restriction-of-Function’ Approach Reveals Evidence for Anxiolytic-Like Actions Mediated by α5-Containing GABAA Receptors in Mice [PDF]

, 2016
Lauren M Behlke, Rachel A Foster, Jing Liu, Dietmar Benke, Rebecca S. Benham, Anna Nathanson, Benjamin K. Yee, Hanns Ulrich Zeilhofer, Elif Engin, Uwe Rudolph   +9 more
openalex   +1 more source