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Lophotoxins: Irreversible active‐site‐directed inhibitors of nicotinic acetylcholine receptors
Author(s) -
Abramson Stewart N.,
Fenical William,
Taylor Palmer
Publication year - 1991
Publication title -
drug development research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.582
H-Index - 60
eISSN - 1098-2299
pISSN - 0272-4391
DOI - 10.1002/ddr.430240402
Subject(s) - nicotinic agonist , acetylcholine , acetylcholine receptor , ganglion type nicotinic receptor , cholinergic , alpha 4 beta 2 nicotinic receptor , receptor , muscarinic acetylcholine receptor m5 , chemistry , nicotinic acetylcholine receptor , neuromuscular junction , biochemistry , nicotinic antagonist , pharmacology , muscarinic acetylcholine receptor m3 , biology , neuroscience
The lophotoxins are a family of structurally‐related neurotoxins that can be isolated from various species of marine soft coral. Like many other naturally occurring neurotoxins, they inhibit nicotinic acetylcholine receptors, resulting in neuromuscular paralysis. However, they are unlike other nicotinic acetylcholine receptor antagonists in several respects. For instance, they do not contain a positive charge common to most cholinergic antagonists; they are conformationally constrained; they react covalently with a specific amino acid (Tyr 190 ) in the a‐subunit of the receptor; and they inhibit both neuronal and muscle subtypes of the receptor. These features make the lophotoxins useful probes for understanding the structure and function of neuronal and muscle nicotinic acetylcholine receptors. Their unique activity may also prove to be useful in a variety of clinical applications.