Nootropic 7 nicotinic receptor allosteric modulator derived from GABAA receptor modulators
نویسندگان
چکیده
منابع مشابه
Nootropic alpha7 nicotinic receptor allosteric modulator derived from GABAA receptor modulators.
Activation of brain alpha7 nicotinic acetylcholine receptors (alpha7 nAChRs) has broad therapeutic potential in CNS diseases related to cognitive dysfunction, including Alzheimer's disease and schizophrenia. In contrast to direct agonist activation, positive allosteric modulation of alpha7 nAChRs would deliver the clinically validated benefits of allosterism to these indications. We have genera...
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Both preclinical evidence and clinical evidence suggest that a7 nicotinic acetylcholine receptor activation (a7nAChR) improves cognitive function, the decline of which is associated with conditions such as Alzheimer’s disease and schizophrenia. Moreover, allosteric modulation of a7nAChR is an emerging therapeutic strategy in an attempt to avoid the rapid desensitization properties associated wi...
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Ivermectin is a macrocyclic lactone that acts as a positive allosteric modulator of alpha7 nicotinic acetylcholine receptors (nAChRs) but has no modulatory activity on 5-hydroxytryptamine (5-HT) type 3 (5-HT(3)) receptors. By examining the influence of ivermectin on subunit chimeras containing domains from the nAChR alpha7 subunit and the 5-HT3A subunit, we have concluded that the transmembrane...
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The receptor for TSH (TSHR) has captured our interest and imagination since it was first demonstrated to be a major human antigen in autoimmune thyroid disease. The original realization that the immunoglobulin fraction of sera from patients with Graves’ disease incorporated unique human autoantibodies to the TSHR led to the unraveling of the great complexity that the TSHR exhibits in comparison...
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Rationale: Current first-line treatments for stress-related disorders such as major depressive disorder (MDD) act on monoaminergic systems and take weeks to achieve a therapeutic effect with poor response and low remission rates. Recent research has implicated the GABAergic system in the pathophysiology of depression, including deficits in interneurons targeting the dendritic compartment of cor...
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ژورنال
عنوان ژورنال: Proceedings of the National Academy of Sciences
سال: 2007
ISSN: 0027-8424,1091-6490
DOI: 10.1073/pnas.0701321104