Negative Allosteric Modulation of Nicotinic Acetylcholine Receptors Blocks Nicotine Self-Administration in Rats
- R. Yoshimura, D. Hogenkamp, K. Gee
- Biology, ChemistryJournal of Pharmacology and Experimental…
- 1 December 2007
UCI-30002 represents validation of the concept that negative allosteric modulators may have significant benefits as a strategy for treating nicotine addiction and encourages the development of subtype-selective modulators.
First in human trial of a type I positive allosteric modulator of alpha7-nicotinic acetylcholine receptors: Pharmacokinetics, safety, and evidence for neurocognitive effect of AVL-3288
- K. Gee, A. Olincy, R. Freedman
- Psychology, BiologyJournal of Psychopharmacology
- 15 February 2017
The trial demonstrates that a type I PAM can be safely administered to humans and that it has potential positive neurocognitive effects in central nervous system (CNS) disorders.
Allosteric modulation of nicotinic and GABAA receptor subtypes differentially modify autism-like behaviors in the BTBR mouse model
- R. Yoshimura, M. Tran, K. Gee
- Psychology, BiologyNeuropharmacology
- 1 November 2017
Pharmacological profile of a 17β-heteroaryl-substituted neuroactive steroid
- D. Hogenkamp, M. Tran, R. Yoshimura, T. Johnstone, R. Kanner, K. Gee
- Biology, ChemistryPsychopharmacology
- 28 February 2014
UCI-50027 is an orally active neuroactive steroid with pharmacological activity consistent with a gamma-aminobutyric acid(A) receptor PAM that has an improved separation between anticonvulsant/anxiolytic and rotarod effects, potent activity as an anticonVulsant and anxIOlytic when compared to ganaxolone.
Modifying quinolone antibiotics yields new anxiolytics
- T. Johnstone, D. Hogenkamp, K. Gee
- BiologyNature Network Boston
- 2004
Patients taking fluoroquinolone antibiotics such as norfloxacin exhibit a low incidence of convulsions and anxiety. These side effects probably result from antagonism of the neurotransmitter…
Limiting Activity at β1-Subunit-Containing GABAA Receptor Subtypes Reduces Ataxia
- K. Gee, M. Tran, E. R. Whittemore
- BiologyJournal of Pharmacology and Experimental…
- 1 March 2010
These findings provide an alternative strategy for designing anxioselective allosteric modulators of the GABAAR with BZ-like anxiolytic efficacy by reducing or eliminating activity at β1-subunit-containing GABAARs.
Reversible lipidization for the oral delivery of leu-enkephalin
- Jeffrey R. Wang, D. Hogenkamp, K. Gee
- Biology, ChemistryJournal of drug targeting (Print)
- 1 January 2006
The results indicate that like its disulfide-based counterpart, amine-based REAL may be an enabling technology which can be applied to enhance metabolic stability, increase oral absorption, and preserve and possibly prolong the pharmacological activity of peptide drugs.
Allosteric Modulation of Related Ligand-Gated Ion Channels Synergistically Induces Long-Term Potentiation in the Hippocampus and Enhances Cognition
- T. Johnstone, Z. Gu, K. Gee
- BiologyJournal of Pharmacology and Experimental…
- 1 March 2011
Combined transient application of two allosteric modulators that individually inhibit α5 GABAARs and enhance α7 nAChRs causes long-term potentiation of mossy fiber stimulation-induced excitatory postsynaptic currents (EPSC) from CA1 pyramidal neurons of rat hippocampal slices.
Melanin Concentrating Hormone Signaling Deficits in Schizophrenia: Association With Memory and Social Impairments and Abnormal Sensorimotor Gating
- M. Vawter, Anton Schulmann, A. Alachkar
- Psychology, BiologyInternational Journal of Neuropsychopharmacology
- 30 September 2019
This study indicates that early disruption of the melanin concentrating hormone system interferes with neurodevelopmental processes, which may contribute to the pathogenesis of schizophrenia.
Prenatal one-carbon metabolism dysregulation programs schizophrenia-like deficits
- A. Alachkar, L. Wang, O. Civelli
- Psychology, MedicineMolecular Psychiatry
- 1 February 2018
The data support the validity of MET mice as a model for schizophrenia, and uncover methionine metabolism as a potential preventive and/or therapeutic target.
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