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Negative Allosteric Modulation of Nicotinic Acetylcholine Receptors Blocks Nicotine Self-Administration in Rats

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.
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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.
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Allosteric modulation of nicotinic and GABAA receptor subtypes differentially modify autism-like behaviors in the BTBR mouse model

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Pharmacological profile of a 17β-heteroaryl-substituted neuroactive steroid

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.
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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…
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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.
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Reversible lipidization for the oral delivery of leu-enkephalin

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.
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Allosteric Modulation of Related Ligand-Gated Ion Channels Synergistically Induces Long-Term Potentiation in the Hippocampus and Enhances Cognition

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.
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Melanin Concentrating Hormone Signaling Deficits in Schizophrenia: Association With Memory and Social Impairments and Abnormal Sensorimotor Gating

This study indicates that early disruption of the melanin concentrating hormone system interferes with neurodevelopmental processes, which may contribute to the pathogenesis of schizophrenia.
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Prenatal one-carbon metabolism dysregulation programs schizophrenia-like deficits

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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