scholarly journals Galantamine is not a positive allosteric modulator of human α4β2 or α7 nicotinic acetylcholine receptors

2018 ◽  
Vol 175 (14) ◽  
pp. 2911-2925 ◽  
Author(s):  
Natalia M Kowal ◽  
Philip K Ahring ◽  
Vivian W Y Liao ◽  
Dinesh C Indurti ◽  
Benjamin S Harvey ◽  
...  
Keyword(s):  
Nicotinic Acetylcholine Receptors ◽  
Acetylcholine Receptors ◽  
Allosteric Modulator ◽  
Positive Allosteric Modulator ◽  
Nicotinic Acetylcholine ◽  
Α7 Nicotinic Acetylcholine Receptors

3-Furan-2-yl-N-p-tolyl-acrylamide, a highly selective positive allosteric modulator of α7 nicotinic receptors, produces anxiolytic-like activity in mice

2019 ◽  
Vol 33 (5) ◽  
pp. 558-567 ◽  
Author(s):  
Katarzyna M Targowska-Duda ◽  
Barbara Budzynska ◽  
Agnieszka Michalak ◽  
Krzysztof Jozwiak ◽  
Grazyna Biala ◽  
...  
Keyword(s):  
Nicotinic Acetylcholine Receptors ◽  
Acetylcholine Receptors ◽  
Acute Treatment ◽  
Elevated Plus Maze ◽  
Allosteric Modulator ◽  
Positive Allosteric Modulator ◽  
Nicotinic Acetylcholine ◽  
Plus Maze ◽  
Α7 Nicotinic Acetylcholine Receptors ◽  
First Time

Background: Several lines of investigations support the idea that nicotinic acetylcholine receptors modulate neuronal pathways involved in anxiety and depression. Aims: The purpose of this study was to determine whether 3-furan-2-yl-N-p-tolyl-acrylamide, a highly selective positive allosteric modulator of α7 nicotinic acetylcholine receptors, influences anxiety-like behaviour in mice, and to determine the modulatory activity of 3-furan-2-yl-N-p-tolyl-acrylamide on mice pretreated with either nicotine or selective α7-agonists (i.e. PNU-282987 or (2.4)-dimethoxybenzylidene anabaseine dihydrochloride). Methods: The elevated plus maze and novelty suppressed feeding tests were selected to evaluate 3-furan-2-yl-N-p-tolyl-acrylamide and other nicotinic ligands on anxiety-like behaviour in mice. Results: The results indicated that: (a) 3-furan-2-yl-N-p-tolyl-acrylamide induces anxiolytic-like activity at 0.5 (elevated plus maze) and 1.0 (novelty suppressed feeding) mg/kg, respectively, after acute treatment, whereas its efficacy is increased after chronic treatments (i.e. active at 0.1 mg/kg; elevated plus maze). This is the first time showing anxiolytic-like activity elicited by 3-furan-2-yl-N-p-tolyl-acrylamide, contrary to the lack of activity for PNU-120596 (0.1 mg/kg); (b) the anxiolytic-like activity of 0.5 mg/kg 3-furan-2-yl-N-p-tolyl-acrylamide is inhibited by methyllycaconitine, a selective α7-antagonist, suggesting that α7 nicotinic acetylcholine receptors are involved in this process; (c) 0.5 mg/kg 3-furan-2-yl-N-p-tolyl-acrylamide reverses the anxiogenic effects induced by 0.1 mg/kg nicotine but not by 10.0 mg/kg PNU-282987; and (d) inactive doses of both 3-furan-2-yl-N-p-tolyl-acrylamide (0.1 mg/kg) and (2.4)-dimethoxybenzylidene anabaseine dihydrochloride (1.0 mg/kg) produce anxiolytic-like effects, suggesting drug interactions, probably synergistic. Conclusions: Our findings indicated that anxiolytic-like activity is mediated by α7 nicotinic acetylcholine receptors, supporting the concept that these receptors modulate anxiety processes. The results indicating that the chronic treatment with 3-furan-2-yl-N-p-tolyl-acrylamide is more efficient than the acute treatment in eliciting anxiolytic-like activity, and that 3-furan-2-yl-N-p-tolyl-acrylamide reverses the anxiogenic effects induced by nicotine, might be of therapeutic importance during smoking cessation.

scholarly journals In silico Investigation of Curcumin as a Positive Allosteric Modulator of a7‐Nicotinic Acetylcholine Receptors

2020 ◽  
Vol 34 (S1) ◽  
pp. 1-1
Author(s):  
Tatiana Prytkova ◽  
Mirue Kang ◽  
Tri Ngoc Quang Tran ◽  
Jiwoo You ◽  
Younji Jeong ◽  
...  
Keyword(s):  
Nicotinic Acetylcholine Receptors ◽  
In Silico ◽  
Acetylcholine Receptors ◽  
Allosteric Modulator ◽  
Positive Allosteric Modulator ◽  
Nicotinic Acetylcholine
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