Talk:Homotaurine/Archive 1

Alzheimers
This content too is not appropriately sourced. moving here for now...

Homotaurine has also been investigated as a potential treatment for Alzheimer's disease. It binds to soluble amyloid beta and inhibits the formation of neurotoxic aggregates that lead to amyloid plaque deposition in the brain. However, clinical trials failed to show improvement compared to placebo.

- Jytdog (talk) 21:19, 9 March 2016 (UTC)
 * You have also restored this without discussing or fixing the sources. This is not reliable content because the source are not MEDRS. Jytdog (talk) 22:18, 9 March 2016 (UTC)
 * I have fixed this now. Jytdog (talk) 01:16, 10 March 2016 (UTC)

activities
OK, let's discuss this:

It is a GABAb receptor antagonist and reversed the catatonia induced by baclofen in rats. Moreover, Homotaurine suppress ethanol-stimulated dopamine release, ethanol intake and preference in rats similar to acamprosate (Acetylated homotaurine analogue).

The sources here are both old and primary. This is not how we should be sourcing WP content. These kinds of papers often turn out to be incorrect. If they are correct and valuable, they are discussed in reviews. Where are the secondary sources supporting this content? Jytdog (talk) 21:18, 9 March 2016 (UTC)

Response:

The entire document is accesible, and "it has GABAergic effects and may be useful as an anticonvulsant.[2]" has a old source too. Another source: http://naturaldatabase.therapeuticresearch.com/nd/PrintVersion.aspx?id=1251&AspxAutoDetectCookieSupport=1

https://books.google.es/books?id=4oXFr_aHRAwC&pg=PA169&lpg=PA169&dq=homotaurine+gabab&source=bl&ots=cvlQ4Y07ea&sig=QfMyPpg-40d1hCNINjqlHMhK7n0&hl=es&sa=X&ved=0ahUKEwjgzcyPx7TLAhXThhoKHT2jCGw4ChDoAQhLMAY#v=onepage&q=homotaurine%20gabab&f=false

http://tauruspet.med.yale.edu/staff/edm42/IUPUI-website/emorris.tar/emorris/emorris/PETjournalCLub/ideas%20for%20ntPET%20studies/Effects%20of%20acamporsate%20-%20delay%20of%20DA%20Olve%20EJPharm%202001.pdf

is 2002 an old source? OK, lets go to erase all of "old" sources. — Preceding unsigned comment added by Fonsy74 (talk • contribs) 21:36, 9 March 2016 (UTC)


 * this is not a response. where are the reviews discussing this? Jytdog (talk) 21:48, 9 March 2016 (UTC)
 * OK, I finally had time to go look for reveiws myself - here is the search. I added three reviews from that seach:
 * Caltagirone C et al. The potential protective effect of tramiprosate (homotaurine) against Alzheimer's disease: a review. Aging Clin Exp Res. 2012 Dec;24(6):580-7.
 * Herrmann N et al. Current and emerging drug treatment options for Alzheimer's disease: a systematic review. Drugs. 2011 Oct 22;71(15):2031-65. Review.
 * Aisen PS Alzhemed: a potential treatment for Alzheimer's disease. Curr Alzheimer Res. 2007 Sep;4(4):473-8.
 * None of these recent reviews mentions that GABA binding data. This appears to be not something that the field finds true or relevant - we cannot know which.  This is why we rely on reviews, and not the primary literature.  I have again removed this content, as MEDRS-compliant sources do not support it. Jytdog (talk) 01:16, 10 March 2016 (UTC)


 * Its impossible homotaurine be antagonist if it mimick gaba! Error and unsourced. Evicence says that is a gaba ionotropic agonist and gaba metrabotropic low efficacy agonist (antagonist) — Preceding unsigned comment added by 81.60.45.17 (talk) 12:08, 10 March 2016 (UTC)
 * No. it is a common drug discovery strategy.  There are many reviews discussing this.  The idea is that a small molecule drug candidate is similar enough to the endogenous ligand to bind the receptor and block it, but not have the same effect (activating or inactivating) as the the endogenous ligand.  You have just made it clear that you lack competence in the science here, as well lacking competence in Wikipedia's policies and guidelines. Please see WP:CIR.  Again, I would be happy to work with you but you need to work within Wikipedia's system. Jytdog (talk) 15:59, 10 March 2016 (UTC)


 * The Jytdog version has a few sources and No source for say homotaurine is a gaba antagonist mimicking gaba. Current evicence shows that homotaurine is an agonist at GABA a ionotropic and a partial low efficacy agonist of gabab receptors, who compite with gaba and baclofen, more potents agonists — Preceding unsigned comment added by 81.60.45.17 (talk • contribs) 12:22, 10 March 2016 (UTC)
 * The source at the end of the paragraph, was for the whole two-sentence paragraph. I added it after the 1st sentence to deal with your objection.  everything is sourced.  The source is Daniel Lednicer, The Organic Chemistry of Drug Synthesis. John Wiley & Sons, 2007 ISBN 9780470180662. Page 15  If you have a more recent secondary source on this, that would be great.  Jytdog (talk) 16:16, 10 March 2016 (UTC)


 * there are dispute resolution processes here in Wikipedia, but we cannot use them if you will not actually talk, and base the discussion on Wikipedia's policies and guidelines. Will you please agree to use one of the dispute resolution procedures?  There is a whole community here we can tap, and well established ways to work out content disputes.  I can walk you through them. Jytdog (talk)  18:48, 10 March 2016 (UTC)

Nicely formatted content, originally added by SOCKING blocked editor
Moving this here for now, this was added by obvious sock.

Because of its similarity in structure to the neurotransmitter gamma-aminobutyric acid (GABA), it has GABAergic effects and may be useful as an anticonvulsant.
 * from the 1st paragraph)


 * Animal studies

Homotaurine reversed the catatonia induced by baclofen in rats. Homotaurine also suppress ethanol-stimulated dopamine release, ethanol intake and preference in rats similar to acamprosate (an acetylated homotaurine analogue). Acamprosate, enhance NMDA currents and inhibited GABAB receptor too.

Homotaurine has shown activity in animal models of alcoholism, and a GABAB receptor partial agonist with low efficacy, becoming an antagonist and displacing full agonist as GABA or baclofen. Homotaurine produces analgesia via GABAB receptor, effect that is abolished when applied CGP 35348, a GABAB receptor antagonist.

- Jytdog (talk) 21:30, 10 March 2016 (UTC)

It is the active molecule in ALZ-801
Could mention ? or just say it is known as ALZ-801 for Alzheimers trials ? - Rod57 (talk) 17:21, 17 April 2017 (UTC)