Galanthamine and other Amaryllidaceae related alkaloids are inhibitors of α7, α4β2 and α3β4 nicotinic acetylcholine receptors
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چکیده
منابع مشابه
Identification of a Negative Allosteric Site on Human α4β2 and α3β4 Neuronal Nicotinic Acetylcholine Receptors
Acetylcholine-based neurotransmission is regulated by cationic, ligand-gated ion channels called nicotinic acetylcholine receptors (nAChRs). These receptors have been linked to numerous neurological diseases and disorders such as Alzheimer's disease, Parkinson's disease, and nicotine addiction. Recently, a class of compounds has been discovered that antagonize nAChR function in an allosteric fa...
متن کاملChanges in Temperature Have Opposing Effects on Current Amplitude in α7 and α4β2 Nicotinic Acetylcholine Receptors
We have examined the effect of temperature on the electrophysiological properties of three neuronal nicotinic acetylcholine receptor (NACHR) subtypes: the rapidly desensitizing homomeric α7 nAChR, the more slowly desensitizing heteromeric α4β2 nAChR and on α7 nAChRs containing a transmembrane mutation (L247T) that results in dramatically reduced desensitization. In all cases, the functional pro...
متن کاملTherapeutic Potential of α7 Nicotinic Acetylcholine Receptors.
Progress in the fields of neuroscience and molecular biology has identified the forebrain cholinergic system as being important in many higher order brain functions. Further analysis of the genes encoding the nicotinic acetylcholine receptors (nAChRs) has highlighted, in particular, the role of α7 nAChRs in these higher order brain functions as evidenced by their peculiar physiologic and pharma...
متن کاملKinetic properties and open probability of α7 nicotinic acetylcholine receptors.
The alpha7 nicotinic acetylcholine receptor (nAChR) has some peculiar kinetic properties. From the literature of α7 nAChR-mediated currents we concluded that experimentally measured kinetic properties reflected properties of the solution exchange system, rather than genuine kinetic properties of the receptors. We also concluded that all experimentally measured EC50 values for agonists must inhe...
متن کاملMenthol Binding and Inhibition of α7-Nicotinic Acetylcholine Receptors
Menthol is a common compound in pharmaceutical and commercial products and a popular additive to cigarettes. The molecular targets of menthol remain poorly defined. In this study we show an effect of menthol on the α7 subunit of the nicotinic acetylcholine (nACh) receptor function. Using a two-electrode voltage-clamp technique, menthol was found to reversibly inhibit α7-nACh receptors heterolog...
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ژورنال
عنوان ژورنال: Revista Brasileira de Farmacognosia
سال: 2019
ISSN: 0102-695X
DOI: 10.1016/j.bjp.2019.04.003