Allosteric interaction of the anticholinergic drug [N-(4-phenyl)-phenacyl-l-hyoscyamine] (Phenthonium) with nicotinic receptors of post-ganglionic sympathetic neurons of the rat vas deferens.

Author: De LimaThereza C M, LapaAntonio J, Lima-LandmanMaria Teresa R, MunhozEgberto, SouccarCaden

Paper Details 
Original Abstract of the Article :
Phenthonium (Phen), a quaternary analog of hyoscyamine, is a blocker of muscarinic activity and an allosteric blocker of alpha(1)2betagammaepsilon nicotinic receptors. Specifically, Phenthonium increases the spontaneous release of acetylcholine at the motor endplate without depolarizing the muscle o...See full text at original site
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引用元:
https://doi.org/10.1016/j.ejphar.2009.06.007

データ提供:米国国立医学図書館(NLM)

Phenthonium: An Allosteric Dance at the Nicotinic Receptor

Oh, the intricate dance of neurotransmitters! This study explores the fascinating interaction of the drug phenthonium with nicotinic receptors in the rat vas deferens. Phenthonium, a unique molecule, acts as an allosteric blocker, influencing the activity of these receptors without directly binding to their active site. It's like a skilled dancer who subtly changes the rhythm of the dance without ever stepping onto the dance floor.

Phenthonium: A Unique Modulator of Cholinergic Synapses

The study revealed that phenthonium inhibits transmitter release and depresses muscle contractions without affecting the response to other chemicals. It also demonstrated that phenthonium's effects on nicotinic receptors are not related to its antimuscarinic or K(+)-channel opening activities. This suggests that phenthonium may have a unique mode of action, acting as a novel modulator of cholinergic synapses. This could be a significant discovery, opening up new avenues for understanding and manipulating neuronal communication.

Allosteric Modulation: A New Frontier in Drug Development

This study emphasizes the potential of allosteric modulation as a new frontier in drug development. By targeting allosteric sites, we can achieve more specific and targeted effects, minimizing side effects and maximizing therapeutic benefits. This is like finding a new oasis in the vast desert of drug discovery, offering a more precise and personalized approach to treating various conditions. This research is paving the way for a new era of drug development, where we can tailor treatments to individual needs and achieve better outcomes.

Dr.Camel's Conclusion

This study showcases the intriguing allosteric interactions of phenthonium with nicotinic receptors, revealing a novel modulator of cholinergic synapses. This discovery highlights the potential of allosteric modulation as a promising strategy for drug development, potentially leading to more targeted and effective therapies for a wide range of conditions.

Date :
  1. Date Completed 2009-10-19
  2. Date Revised 2015-11-19
Further Info :

Pubmed ID

19540221

DOI: Digital Object Identifier

10.1016/j.ejphar.2009.06.007

Related Literature

SNS
PICO Info
in preparation
Languages

English

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