The non-competitive acetylcholinesterase inhibitor APS12-2 is a potent antagonist of skeletal muscle nicotinic acetylcholine receptors

2012 ◽  
Vol 265 (2) ◽  
pp. 221-228 ◽  
Author(s):  
Marjana Grandič ◽  
Romulo Aráoz ◽  
Jordi Molgó ◽  
Tom Turk ◽  
Kristina Sepčić ◽  
...  
Keyword(s):  
Skeletal Muscle ◽  
Nicotinic Acetylcholine Receptors ◽  
Acetylcholine Receptors ◽  
Acetylcholinesterase Inhibitor ◽  
Nicotinic Acetylcholine ◽  
Potent Antagonist

A novel alpha conotoxin (α-PIB) isolated from C. purpurascens is selective for skeletal muscle nicotinic acetylcholine receptors

Toxicon ◽  
2007 ◽  
Vol 49 (8) ◽  
pp. 1193-1199 ◽  
Author(s):  
Estuardo López-Vera ◽  
Richard B. Jacobsen ◽  
Michael Ellison ◽  
Baldomero M. Olivera ◽  
Russell W. Teichert
Keyword(s):  
Skeletal Muscle ◽  
Nicotinic Acetylcholine Receptors ◽  
Acetylcholine Receptors ◽  
Nicotinic Acetylcholine

Infraterminal spreading and extrajunctional expression of nicotinic acetylcholine receptors in denervated rat skeletal muscle

1999 ◽  
Vol 125 (4) ◽  
pp. 426-434 ◽  
Author(s):  
Bertalan Csillik ◽  
János Nemcsók ◽  
Bruce Chase ◽  
Anita E. Csillik ◽  
Elizabeth Knyihár-Csillik
Keyword(s):  
Skeletal Muscle ◽  
Nicotinic Acetylcholine Receptors ◽  
Acetylcholine Receptors ◽  
Rat Skeletal Muscle ◽  
Nicotinic Acetylcholine

scholarly journals The Dinoflagellate Toxin 20-Methyl Spirolide-G Potently Blocks Skeletal Muscle and Neuronal Nicotinic Acetylcholine Receptors

Toxins ◽  
2016 ◽  
Vol 8 (9) ◽  
pp. 249 ◽  
Author(s):  
Aurélie Couesnon ◽  
Rómulo Aráoz ◽  
Bogdan Iorga ◽  
Evelyne Benoit ◽  
Morgane Reynaud ◽  
...  
Keyword(s):  
Skeletal Muscle ◽  
Nicotinic Acetylcholine Receptors ◽  
Acetylcholine Receptors ◽  
Neuronal Nicotinic Acetylcholine Receptors ◽  
Nicotinic Acetylcholine

Two Novel α-Neurotoxins Isolated from the Taipan Snake,Oxyuranus scutellatus, Exhibit Reduced Affinity for Nicotinic Acetylcholine Receptors in Brain and Skeletal Muscle†

Biochemistry ◽  
1996 ◽  
Vol 35 (24) ◽  
pp. 7910-7916 ◽  
Author(s):  
Fernando Zamudio ◽  
Kathleen M. Wolf ◽  
Brian M. Martin ◽  
Lourival D. Possani ◽  
Vincent A. Chiappinelli
Keyword(s):  
Skeletal Muscle ◽  
Nicotinic Acetylcholine Receptors ◽  
Acetylcholine Receptors ◽  
Nicotinic Acetylcholine

scholarly journals Action of Carvacrol on Parascaris sp. and Antagonistic Effect on Nicotinic Acetylcholine Receptors

2021 ◽  
Vol 14 (6) ◽  
pp. 505
Author(s):  
Sasa M. Trailovic ◽  
Milan Rajkovic ◽  
Djordje S. Marjanovic ◽  
Cédric Neveu ◽  
Claude L. Charvet
Keyword(s):  
Nicotinic Acetylcholine Receptors ◽  
Mode Of Action ◽  
Acetylcholine Receptors ◽  
Muscle Flap ◽  
Antagonistic Effect ◽  
Nicotinic Acetylcholine ◽  
Antiparasitic Drugs ◽  
Potent Antagonist

Parascaris sp. is the only ascarid parasitic nematode in equids and one of the most threatening infectious organisms in horses. Only a limited number of compounds are available for treatment of horse helminthiasis, and Parascaris sp. worms have developed resistance to the three major anthelmintic families. In order to overcome the appearance of resistance, there is an urgent need for new therapeutic strategies. The active ingredients of herbal essential oils are potentially effective antiparasitic drugs. Carvacrol is one of the principal chemicals of essential oil from Origanum, Thymus, Coridothymus, Thymbra, Satureja and Lippia herbs. However, the antiparasitic mode of action of carvacrol is poorly understood. Here, the objective of the work was to characterize the activity of carvacrol on Parascaris sp. nicotinic acetylcholine receptor (nAChR) function both in vivo with the use of worm neuromuscular flap preparations and in vitro with two-electrode voltage-clamp electrophysiology on nAChRs expressed in Xenopus oocytes. We developed a neuromuscular contraction assay for Parascaris body flaps and obtained acetylcholine concentration-dependent contraction responses. Strikingly, we observed that 300 µM carvacrol fully and irreversibly abolished Parascaris sp. muscle contractions elicited by acetylcholine. Similarly, carvacrol antagonized acetylcholine-induced currents from both the nicotine-sensitive AChR and the morantel-sensitive AChR subtypes. Thus, we show for the first time that body muscle flap preparation is a tractable approach to investigating the pharmacology of Parascaris sp. neuromuscular system. Our results suggest an intriguing mode of action for carvacrol, being a potent antagonist of muscle nAChRs of Parascaris sp. worms, which may account for its antiparasitic potency.

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