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The Chemistry and Pharmacology of Anatoxin-a and Related Homotropanes with respect to Nicotinic Acetylcholine Receptors
Mar. Drugs 2006, 4(3), 255-273; doi:10.3390/md403255
Review

The Nemertine Toxin Anabaseine and Its Derivative DMXBA (GTS-21): Chemical and Pharmacological Properties

1,* , 1, 1, 1, 1, 3, 4 and 2
1 Department of Pharmacology and Therapeutics, University of Florida, College of Medicine, Gainesville, FL 32610-0267, USA 2 Department of Pharmaceutical Sciences, College of Pharmacy, Western University of Health Sciences, Pomona, CA 91766-1854, USA 3 College of Life Science and Technology, Shanghai Jiaotong University, Minhang District Shanghai, 200240, China 4 Gordon Life Science Institute, San Diego, CA 92130, USA
* Author to whom correspondence should be addressed.
Received: 10 January 2006 / Accepted: 4 April 2006 / Published: 6 April 2006
(This article belongs to the Special Issue Marine Drugs and Ion Channels)
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Abstract

Nemertines are a phylum of carnivorous marine worms that possess a variety of alkaloidal, peptidic or proteinaceous toxins that serve as chemical defenses against potential predators. The hoplonemertines additionally envenomate their prey with a mixture of proboscis alkaloids delivered with the help of a calcareous stylet that punctures the skin of the victim. Anabaseine, the first of these alkaloids to be identified, stimulates a wide variety of animal nicotinic acetylcholine receptors (AChRs), especially the neuromuscular [e.g., α12β1γδ (embryogenic) or α12β1γε (adult)] and α7 AChRs that are inhibited by the snake peptide α-bungarotoxin. A synthetic derivative, 3-(2,4-Dimethoxybenzylidene)-Anabaseine (DMXBA; also called GTS-21), improves memory in experimental animals and humans and is currently in clinical trials to determine whether it can ameliorate cognitive problems associated with schizophrenia. Here we summarize present knowledge concerning the chemistry and mechanisms of action of these two substances (anabaseine and DMXBA) on AChRs, especially those found in the mammalian brain.
Keywords: Anabaseine; Cognition; DMXBA; GTS-21; Nemertine; Nicotinic receptors Anabaseine; Cognition; DMXBA; GTS-21; Nemertine; Nicotinic receptors
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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Kem, W.; Soti, F.; Wildeboer, K.; LeFrancois, S.; MacDougall, K.; Wei, D.-Q.; Chou, K.-C.; Arias, H.R. The Nemertine Toxin Anabaseine and Its Derivative DMXBA (GTS-21): Chemical and Pharmacological Properties. Mar. Drugs 2006, 4, 255-273.

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