Nootropic α7 nicotinic receptor allosteric modulator derived from GABAA receptor modulators
- Herman J Ng, E. R. Whittemore, K. Gee
- Biology, PsychologyProceedings of the National Academy of Sciences
- 8 May 2007
A selective α7 nAChR-positive allosteric modulator (PAM) from a library of GABAA receptor PAMs is generated, which corrects sensory-gating deficits and improves working memory, effects consistent with cognitive enhancement in rodent models.
1,1-Dicyano-2-[6-(dimethylamino)naphthalen-2-yl]propene (DDNP): A Solvent Polarity and Viscosity Sensitive Fluorophore for Fluorescence Microscopy⊥
1,1-Dicyano-2-[6-(dimethylamino)naphthalen-2-yl]propene (II, DDNP) has been synthesized as a fluorescent dye whose intramolecular rotational relaxation is solvent polarity and viscosity dependent.…
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
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.
Realising the therapeutic potential of neuroactive steroid modulators of the GABAA receptor
The monoamine oxidase (MAO) inhibitor tranylcypromine enhances nicotine self-administration in rats through a mechanism independent of MAO inhibition
Allosteric modulation of nicotinic and GABAA receptor subtypes differentially modify autism-like behaviors in the BTBR mouse model
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
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
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.